Skip to main content

Biosynthetic Inhibitors and Receptor Antagonists to Platelet Activating Factor

  • Chapter
Book cover Platelets and Their Factors

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 126))

  • 165 Accesses

Abstract

Platelet activating factor (PAF) is now a quarter of a century old. As a mediator of inflammation, it still enjoys the focus of intensive studies ranging from preclinical pharmacology to clinical studies related to pathological involvements. Since its discovery as a soluble substance released from IgE-stimulated basophils (Benveniste et al. 1972) and its subsequent structural identification, PAF has been referred to as “antihypertensive polar renal medullary lipid” (APRL; Blank et al. 1979), “acetyl glyceryl ether phosphorylcholine” (AGEPC; Demopolus et al. 1979) or by the founding name of “Pafacether” (Benveniste et al. 1979). Currently, there is no accepted international nomenclature that describes the autocoid PAF family (Pinckard et al. 1994).

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 84.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 109.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Adamus WS, Heuer H, Meade CJ (1989) PAF-induced platelet aggregation ex vivo as a method for monitoring pharmacological activity in healthy volunteers. Methods Find Exp Clin Pharmacol 11:415–420

    PubMed  CAS  Google Scholar 

  • Adamus WS, Heuer HO, Meade CJ, Schilling JC (1990) Inhibitory effects of the new PAF acether antagonist WEB 2886 on pharmacological changes induced by PAF inhalation in human beings. Clin Pharmacol Ther 47:456–462

    Article  PubMed  CAS  Google Scholar 

  • Albert DH, Snyder F (1983) Biosynthesis of 1-alkyl 2-acetyl sn-glycero-3-phosphocholine (platelet activating factor) from of 1-alkyl 2-acyl sn-glycero-3-phosphocholine by rat alveolar macrophages. J Biol Chem 258:97–102

    PubMed  CAS  Google Scholar 

  • Anagnostopulos H, Bartlett RR, Elben U, Stoll P (1989) Synthesis of basic substituted pyridines: a new class of antiasthmatic-antiallergic agents. Eur J Chem 24:227–232

    CAS  Google Scholar 

  • Anderson GP, White HL, Fennessy MR (1988) Increased airways responsiveness to histamine induced by platelet activating factor in the guinea pig: possible role of lipoxygenase metabolites. Agents Actions 24:1–7

    Article  PubMed  CAS  Google Scholar 

  • Arnout J, VanHecken A, De Lepeleire I, Miyamoto Y, Holmes I, DeSchepper P, Vermylem J (1988) Effectiveness and tolerability of CV 3988, a selective PAF antagonist, after intravenous administration in man. Br J Clin Pharmacol 25:445–454

    PubMed  CAS  Google Scholar 

  • Arnoux A, Denjean A, Page CP, Nolibe D, Morley J, Benveniste J (1988) Accumulation of platelets and eosinophils in baboon lung after Paf-acether challenge. Am Rev Respir Dis 137:855–860

    PubMed  CAS  Google Scholar 

  • Barnes PJ, Chung KF (1987) PAF closely mimics pathology of asthma. Trends Pharmacol Sci 8:285–287

    Article  CAS  Google Scholar 

  • Batt JP, Lamouri A, Tavet F, Heymans F, Dive G, Godfroid JJ (1991) New hypothesis on the conformation of the PAF receptor from studies on the geometry of selected platelet activating factor antagonists. J Lipid Mediat 4:343–346

    PubMed  CAS  Google Scholar 

  • Bel EH, De Smet M, Rossing TH, Timmers MC, Dijkman JH, Sterk PJ (1991) The effect of a specific PAF antagonist, MK-287, on antigen-induced early and late asthmatic reactions in man. Am Rev Respir Dis 143:A811

    Google Scholar 

  • Benveniste J, Henson PM, Cochrane GC (1972) leukocyte dependent histamine release from rabbit platelets: the role of IgE-basophils and platelet activating factor. J Exp Med 136:1356–1368

    Article  PubMed  CAS  Google Scholar 

  • Benveniste J, Tence M, Varenne P, Bidault J, Boullet C, Polonsky J (1979) Semi-syntheses et structure proposee du facteur activant les plaquettes (P.A.F.): PAF-aceteher, un alkyl ether analogue de la lysophatidylcholine. CR Acad Sci III 289D:1037–1041

    Google Scholar 

  • Betz S, Lotner GZ, Henson PM (1980) Production and release of platelet activating factor (PAF): dissociation from degranulation and Superoxide production in the human neutrophil. J Immunol 125:2749–2763

    PubMed  CAS  Google Scholar 

  • Billah MM, Chapman RW, Egan RW, Gilchrest H, Piwinski JJ, Sherwood J, Siegel MI, West REJ, Dreutner W (1990) Sch 37370: a potent, orally active, dual antagonist of platelet activating factor and histamine. J Pharmacol Exp Ther 252:1090–1096

    PubMed  CAS  Google Scholar 

  • Billah MM, Gilchrest H, Eckel SP, Granzow CA, Lawton PJ, Radwanskii E, Brannan MD, Affrime MB, Christopher JD, Richard W, Siegel MI (1992) Differential plasma duration of anti-platelet activating factor and antihistamine activities of oral Sch 37370 in humans. Clin Pharmacol Ther 52:151–159

    Article  PubMed  CAS  Google Scholar 

  • Bitterman H, Lefer D, Lefer A (1987) Beneficial actions of RO 15–1788, a benzodiazepine receptor antagonist, in hemorrhagic shock. Methods Find Exp Clin Pharmacol 9:341–347

    PubMed  CAS  Google Scholar 

  • Blank ML, Synder F, Byers LW, Brooks B, Muirhead EE (1979) Antihypertensive activity of an alkyl ether analog of phosphatidylcholine. Biochem Biophys Res Commun 90:1194–1200

    Article  PubMed  CAS  Google Scholar 

  • Blank ML, Smith ZL, Fitzgerald V, Snyder F (1995) The CoA-independent transacylase in PAF biosynthesis: tissue distribution and molecular species selectivity. Biochem Biophys Acta 1254:295–301

    PubMed  Google Scholar 

  • Burhop KE, Van Der Zee H, Bizios R, Kaplan JE, Malik AB (1986) Pulmonary vascular response to platelet activating factor in awake sheep and the role of cyclooxygenase metabolites. Am Rev Respir Dis 134:548–554

    PubMed  CAS  Google Scholar 

  • Bussolino F, Gremo F, Tetta C, Pescarmona G, Camussi G (1986) Production of platelet activating factor by chick retina. J Boil Chem 261:16502–16508

    CAS  Google Scholar 

  • Cai X, Hussoin S, Killan D, Scannel R, Yaeger D, Eckman J, Hwang SB, Libertine-Barahan L, Qian C, Yeh C, Ip S (1994) Synthesis of substituted hydroxyurieidyl diaryltetrahydrofurans, a potent class of inhibitors of 5-lipoxygenase and platelet activating factor. In: 207th National Meeting of the American Chemical Society, MEDI 123

    Google Scholar 

  • Camussi G, Neilsen N, Tetta C, Saunders RN, Milgrom F (1987) Release of platelet activating factor from rabbit heart perfused in vitro by sera with transplantation alloantibodies. Transplantation 44:113–118

    Article  PubMed  CAS  Google Scholar 

  • Carceller E, Merlos M, Giral M, Almansa C, Bartrolli J, Garcia-Rafaneel J, Forn J (1993) Synthesis and structure-activity relationships of l-acyl-4-[(methyl-3-pyridyl) cyanomethyl] piperazines as PAF antagonists. J Med Chem 36:2984–2997

    Article  PubMed  CAS  Google Scholar 

  • Casals-Stenzel J (1987a) Effects of WEB 2086, a novel antagonist to platelet activating factor in active and passive anaphylaxis. Immunopharmacology 13:117–124

    Article  PubMed  CAS  Google Scholar 

  • Casals-Stenzel J (1987b) Triazolodiazepines are potent antagonists of platelet activating factor (PAF) in vitro and in vivo. Arch Pharmacol 335:351–355

    Article  CAS  Google Scholar 

  • Casals-Stenzel J (1987c) Protective effect of WEB 2086, a novel antagonist of platelet activating factor, in endotoxin shock. Eur J Pharmacol 135:117–122

    Article  PubMed  CAS  Google Scholar 

  • Casals-Stenzel J, Weber KH (1987) Triazolodiazepines: dissociation of their Paf (platelet activating factor) antagonistic and CNS activity. Br J Pharmacol 90:139–146

    PubMed  CAS  Google Scholar 

  • Casals-Stenzel J, Franke J, Friedrich T, Lichey J (1987a) Bronchial and vascular effects of Paf in the rate isolated lung are completely blocked by WEB 2086, a novel specific Paf antagonist. Br J Pharmacol 91:799–802

    PubMed  CAS  Google Scholar 

  • Casals-Stenzel J, Muacevic G, Weber KH (1987b) Pharmacological actions of WEB 2086, a new specific antagonist of platelet activating factor. J Pharmacol Exp Ther 241:974–981

    PubMed  CAS  Google Scholar 

  • Chang SW, Feddersen CO, Henson PM, Voelkel NF (1987) Platelet activating factor mediates hemodynamic changes and lung injury in endotoxin treated rats. J Clin Invest 79:1498–1509

    Article  PubMed  CAS  Google Scholar 

  • Chignard M, Le Couedic JP, Vargaftig BB, Benveniste J (1980) Platelet activating factor (PAF-acether) secretion from platelets: effect of aggregating agents. Br J Haematol 46:455–464

    Article  PubMed  CAS  Google Scholar 

  • Christman BW, Lefferts PL, Snapper JR (1987) Effect of platelet activating factor on aerosol histamine responsiveness in awake sheep. Am Rev Respir Dis 135:1267–1270

    PubMed  CAS  Google Scholar 

  • Christman BW, Lefferts PL, King GA, Snapper JR (1988) Role of circulating platelets and granulocytes in platelet activating factor (PAF)-induced pulmonary dysfunction in awake sheep. J Appl Physiol 64:2033–2041

    PubMed  CAS  Google Scholar 

  • Chung KF, Barnes PJ (1988) PAF antagonists: their potential therapeutic role in asthma. Drugs 35:93–103

    Article  PubMed  CAS  Google Scholar 

  • Chung KF, Barnes PJ (1989) Effects of platelet activating factor on airway caliber, airway responsiveness, and circulating cells in asthmatic subjects. Thorax 44:108–115

    Article  PubMed  CAS  Google Scholar 

  • Chung KF, Aizawa H, Becker AB, Frick O, Gold WM, Nadel JA (1986) Inhibition of antigen-induced airway hyperresponsiveness by a thromboxane synthetase inhibitor (OKY-046) in allergic dogs. Am Rev Respir Dis 134:258–261

    PubMed  CAS  Google Scholar 

  • Chung KF, Dent G, McCusker M, Guinot PH, Page CP, Barnes PJ (1987) Effect of a ginkgolide mixture (BN 52063) in antagonising skin and platelet responses to platelet activating factor in man. Lancet 1:248–251

    Article  PubMed  CAS  Google Scholar 

  • Coeffier E, Borrel MC, Lefort J, Chignard M, Broquet C, Heymans F, Godfroid JJ, Vargaftig BB (1986) Effects of Paf-acether and structural analogues on platelet activation and bronchoconstriction in guinea pigs. Eur J Pharmacol 131:179–188

    Article  PubMed  CAS  Google Scholar 

  • Colditz IG, Topper EK (1991) The effect of systemic treatment with platelet activating factor on the migration of eosinophils to the lung, pleural and peritoneal cavities in the guinea pig. Int Arch Allergy Appl Immunol 95:94–96

    Article  PubMed  CAS  Google Scholar 

  • Cooper K, Fray MJ, Richardson K, Steele J (1992) The discovery of UK-74505: a potent and selective4 PAF antagonist. In: 203rd National Meeting of the American Chemical Society, MEDI 182

    Google Scholar 

  • Coyle AJ, Spina D, Page CP (1990) PAF-induced bronchial hyperresponsiveness in the rabbit: contribution of platelets and airway smooth muscle. Br J Pharmacol 101:31–38

    PubMed  CAS  Google Scholar 

  • Cox CP (1986) Effects of CV-3988, an antagonist of platelet activating factor (PAF), on washed rabbit platelets. Thromb Res 41:211–222

    Article  PubMed  CAS  Google Scholar 

  • Dahlback M, Bergstrand H, Sorenby L (1984) Bronchial anaphylaxis in actively sensitized Sprague Dawley rats: studies of mediators involved. Acta Pharmacol Tox 55:6–17

    Article  CAS  Google Scholar 

  • Danko G, Sherwood JE, Grissom B, Kreutner W, Chapman RW (1988) Effect of the PAF antagonists, CV-3988 and L-652,731 on the pulmonary and hematological responses to guinea pig anaphylaxis. Pharmacol Res Commun 20:785–798

    Article  PubMed  CAS  Google Scholar 

  • Davidson SK, Summers JB, Albert DH, Holms JH, Heyman HR, Magocc TJ, Conway RG, Rhein DA, Carter GW (1995) N-(Acyloxyalkyl) pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist. J Med Chem 37:4423–4429

    Article  Google Scholar 

  • Demopoulus CA, Pinckard RN, Hanahan DJ (1979) Platelet activating factor. Evidence for 1-O-alkyl 2-acetyl sn-glyceryl 3-phosphorylcholine as the active component (a new class of lipid chemical mediators). J Boil Chem 254:9355–9358

    Google Scholar 

  • Denizot Y, Trimoreau F, Dupuis F, Verger C, Praloran V (1995) PAF and haematopoiesis: III. Presence and metabolism of platelet activating factor in human bone marrow. Biochim Biophys Acta 1265:55–60

    Article  PubMed  Google Scholar 

  • Denjean A, Arnoux B, Benveniste J, Lockhart A, Masse R (1981) Bronchoconstriction induced by intratracheal administration of platelet activating factor (PAF-acether) in baboons. Agents Actions 11:567–568

    Article  PubMed  CAS  Google Scholar 

  • Denjean A, Arnoux B, Masse R, Lockart A, Benveniste J (1983) Acute effects of intratracheal administrtion of platelet activating factor in baboons. J Appl Physiol 55:799–804

    PubMed  CAS  Google Scholar 

  • Desquand S, Touvay C, Randon J, Lagente V, Vilain B, Parini M, Etienne A, Lefort J, Braquet P, Vargaftig BB (1986) Interference of BN 52021 (Ginkgolide B) with bronchopulmonary effects of PAF-acether in the guinea pig. Eur J Pharmacol 127:83–95

    Article  PubMed  CAS  Google Scholar 

  • Desquand S, Lefort J, Dumarey C, Vargaftig BB (1990) The booster injection of antigen during active sensitization of guinea pig modifies the anti-anaphylactic activity of the PAF antagonist WEB 2086. Br J Pharmacol 100:217–222

    PubMed  CAS  Google Scholar 

  • Doebber T, Wu M (1988) Platelet activating factor induced cellular and pathophysiological responses in the cardiovascular system. Drug Dev Res 12:151–161

    Article  CAS  Google Scholar 

  • Doebber TW, Wu MS, Robbins JC, Choy BM, Chang MN, Shen TY (1985) Platelet activating factor (PAF) involvement in endotoxin-induced hypotension in rats. Studies with PAF receptor dadsurenone. Biochem Biophys Res Commun 127:799–808

    Article  PubMed  CAS  Google Scholar 

  • Doebber TW, Wu MS, Biftu T (1986) Platelet activating factor (PAF) mediation of rat anaphylactic responses to soluble immune complexes. Studies with a PAF receptor antagonist L-752,731. J Immunol 136:4659–4668

    PubMed  CAS  Google Scholar 

  • Emanuelli G, Montrucchio G, Gaia E, Dughera L, Corvetti G, Gubetta L (1989) Experimental acute pancreatitis induced by platelet activating factor in rabbits. Am J Pathol 134:315–325

    PubMed  CAS  Google Scholar 

  • Evans TW, Chung KF, Rogers DF, Barnes PJ (1987) Effect of platelet activating factor on airway permeability: possible mechanisms. J Appl Physiol 63:479–484

    PubMed  CAS  Google Scholar 

  • Evans T, Dent G, Rogers D, Aursudkij B, Chung KF, Barnes P (1988) Effect of a Paf antagonist, WEB 2086, on airway microvascular leakage in the guinea pig and platelet aggregation in man. Br J Pharmacol 94:164–168

    PubMed  CAS  Google Scholar 

  • Fernandez-Gallardo S, Ortega M, Priego J, Casa F, Sunkel C, Sanchez Crespo M (1990) Pharmacological actions of PCA 4248, a new platelet activating factor receptor antagonist: in vivo studies. J Pharmacol Exp Ther 255:34–39

    PubMed  CAS  Google Scholar 

  • Fitzgerald MF, Moneada S, Parente L (1986) The anaphylactic release of platelet activating factor from perfused guinea pig lungs. Br J Pharmacol 88:149–153

    PubMed  CAS  Google Scholar 

  • Freitag A, Watson RM, Mastros G, Eastwood C, O’Byrne PM (1991) Effects of treatment with the oral platelet activating factor antagonist (WEB 2086) on allergen induced asthmatic responses in human subjects. Am Rev Respir Dis 143:A156

    Google Scholar 

  • Garito ML, Prihoda TJ, McMannus LM (1995) Salivary PAF levels correlate with severity of periodontal inflammation. J Dent Res 74:1048–1056

    Article  PubMed  CAS  Google Scholar 

  • Grandel K, Farr R, Wanderer A, Eisenstadt T, Wasserman S (1985) Association of platelet activating factor with primary acquired cold urticaria. N Engl J Med 313:405–409

    Article  PubMed  CAS  Google Scholar 

  • Grue-Sorensen G, Nielsen I, Neilsen C (1988) Derivatives of 2-methylene propane 1,3-diol as a new class of antagonists of platelet activating factor. J Med Chem 31:1174–1178

    Article  PubMed  CAS  Google Scholar 

  • Hadvary P, Baumgartner HR (1985) Interference of PAF antagonists with platelet aggregation and the formation of platelet thrombi. Prostaglandins 30:694–702

    Article  Google Scholar 

  • Hakansson L, Venge P (1990) Inhibition of neutrophil and eosinophil chemotactic responses to PAF by the PAF antagonists WEB 2086, L-652–731, and SRI 63–441. J Leukoc Biol 47:449–456

    PubMed  CAS  Google Scholar 

  • Halonen M, Palmer J, Lohman I, McManus L, Pinckard RN (1980) Respiratory and circulatory alterations induced by acetyl glyceryl ether phosphorylcholine, a mediator of IgE anaphylaxis in the rabbit. Am Rev Respir Dis 122:915–924

    PubMed  CAS  Google Scholar 

  • Hanahan DJ, Demopoulos CA, Liehr J, Pinckard RN (1980) Identification of a platelet activating factor isolated from rabbit basophils as acetylglyceryl ether phosphorylcholine. J Biol Chem 255:5514–5516

    PubMed  CAS  Google Scholar 

  • Handley DA (1987) New developments for clinical applications for PAF antagonists. J Clin Exp Med 143:415–418

    Google Scholar 

  • Handley DA (1988) Development and therapeutic indications of PAF receptor antagonists. Drugs Future 13:137–152

    Google Scholar 

  • Handley DA (1989a) Quantitation of in vitro and in vivo biological effects of platelet activating factor. In: Chang JY, Lewis AJ (eds) Pharmacological methods in the control of inflammation. Liss, New York, pp 23–49

    Google Scholar 

  • Handley DA (1989b) The development and application of colloidal gold as a microscopic probe. In: Hayat MA (ed) Colloidal gold: principles, methods and applications. Academic, San Diego, vol 1, pp 1–12

    Google Scholar 

  • Handley D (1990a) Preclinical and clinical pharmacology of platelet activating factor receptor antagonists. Med Res Rev 10:351–370

    Article  PubMed  CAS  Google Scholar 

  • Handley DA (1990b) Platelet activating factor as a mediator of endotoxin mediated diseases. In: Handley DA, Saunders R, Houlihan W, Tomesch J (eds) Platelet activating factor in immune complex and endotoxin mediated diseases. Dekker, New York, pp 451–495

    Google Scholar 

  • Handley DA, Cerasoli F (1994) PAF antagonists as asthma therapeutics. In: Page CP, Metzger WJ (eds) Drugs and the lung. Raven, New York, pp 467–505

    Google Scholar 

  • Handley DA, Saunders RN (1986) Platelet activating factor and inflammation in atherosclerosis: targets for drug development. Drug Dev Res 7:361–375

    Article  CAS  Google Scholar 

  • Handley DA, Lee M, Saunders RN (1983) Extravasation and aortic changes accompaning acute and subacute intraperitoneal administration of PAF. In: Benveniste J, Arnout B (eds) Platelet activating factor. Elsivier, Amsterdam, pp 243–251

    Google Scholar 

  • Handley DA, Van Valen RG, Melden MK, Saunders RN (1984) Evaluation of dose and route effects of platelet activating factor-induced extravasation in the guinea pig. Thromb Haemost 52:34–36

    PubMed  CAS  Google Scholar 

  • Handley DA, Lee ML, Saunders RN (1985) Evidence for a direct effect on vascular permeability of platelet activating factor induced hemoconcentration in the guinea pig. Thromb Haemost 54:756–759

    PubMed  CAS  Google Scholar 

  • Handley DA, Farley C, Deacon RW, Saunders RN (1986a) Evidence for distinct systemic extravasation effects of platelet activating factor, leukotrienes B4, C4, D4 and histamine in the guinea pig. Prostaglandins Leukot Med 21:269–277

    Article  PubMed  CAS  Google Scholar 

  • Handley DA, Tomesch JC, Saunders RN (1986b) Inhibition of PAF induced responses in the rat, guinea pig, dog and primate by the receptor antagonist SRI 63–441. Thromb Haemost 56:40–44

    PubMed  CAS  Google Scholar 

  • Handley DA, Van Valen RG, Melden MK, Flury S, Lee ML, Saunders RN (1986c) Inhibition and reversal of endotoxin-, aggregated IgG- and PAF-induced hypotension in the rat by SRI 63–072, a PAF receptor antagonist. Immunopharmacology 12:11–17

    Article  PubMed  CAS  Google Scholar 

  • Handley DA, Van Valen RG, Saunders RN (1986d) Vascular responses of platelet-activating factor in the cebus apella primate and inhibitory profiles of PAF antagonists SRI 63–072 and SRI 63–119. Immunopharmacology 11:175–182

    Article  PubMed  CAS  Google Scholar 

  • Handley DA, Anderson RC, Saunders RN (1987a) Inhibition by SRI 63–072 and SRI 63–119 of PAF acether and immune complex effects in the guinea pig. Eur J Pharmacol 141:409–416

    Article  PubMed  CAS  Google Scholar 

  • Handley DA, Van Valen RG, Tomesch JC, Melden MK, Jaffe JA, Ballard F, Saunders RN (1987b) Biological properties of the receptor antagonist SRI 63–441 in the PAF and endotoxin models of hypotension in the rat and dog. Immunopharmacology 13:125–132

    Article  PubMed  CAS  Google Scholar 

  • Handley DA, Van Valen RG, Winslow CM, Tomesch JC, Saunders RN (1987c) In vitro and in vivo pharmacological effects of the PAF receptor antagonist SRI 63–675. Thromb Haemost 57:187–190

    PubMed  CAS  Google Scholar 

  • Handley D, Van Valen RG, Lee ML, Saunders RN (1987d) Cebus appela primate responses to platelet activating factor and inhibition of platelet activating factor antagonist SRI 63–072. In: Winslow CM, Lee ML (eds) New horizons in platelet activating factor research. Wiley, New York, pp 335–341

    Google Scholar 

  • Handley DA, Van Valen RG, Melden MK, Houlihan WJ, Saunders RN (1988) Biological effects of the orally active PAD receptor antagonist SDZ 64–412. J Pharmacol Exp Ther 247:617–628

    PubMed  CAS  Google Scholar 

  • Handley DA, Houlihan W, Tomesch J, Farley C, Deacon R, Koletar J, Prashed M, Hughes J, Jaeggi C (1989) Chemistry and pharmacology of PAF antagonists. In: Sammuelsson B, Wong P, Sun F (eds) Evaluation of changes at potential metabolism sites on activity and duration of activity. Adv Prostaglandin Thromboxane Leukot Res 19:367–370

    Google Scholar 

  • Handley DA, Lee M, Farley C, Deacon R, Melden M, Van Valen RG, Winslow CM, Saunders R (1990) Biological characterization of cyclimmonium PAF antagonists. In: Handley DA, Houlihan W, Saunders R, Tomesch J (eds) Platelet activating factor in endotoxin and immune complex mediated diseases. Dekker, New York, pp 157–175

    Google Scholar 

  • Handley DA, DeLeo J, Havill AM (1992) Induction by aerosol allergen of sustained and nonspecific IgE-mediated airway hyperreactivity in the guinea pig. Agents Actions 37:201–203

    Article  PubMed  CAS  Google Scholar 

  • Havill AM, Van Valen RG, Handley DA (1990) Prevention of non-specific airway hyperreactivity after allergen challenge in guinea pigs by the PAF receptor antagonist SDZ 64–412. Br J Pharmacol 99:396–400

    PubMed  CAS  Google Scholar 

  • Hayashi M, Kimura J, Yamaki K, Suwabe Y, Dozen M, Imai Y, Oh-ishi S (1987a) Detection of platelet activating factor in exudates of rats with phorbol myristate acetate induced pleurisy. Thromb Res 48:299–310

    Article  PubMed  CAS  Google Scholar 

  • Hayashi M, Kimura J, Oh-ishi S, Tsushima S, Nomura H (1987b) Characterization of the activity of a platelet activating factor antagonist, CV-3988. Jpn J Pharmacol 44:127–134

    Article  PubMed  CAS  Google Scholar 

  • Hellewell PG (1990) The contribution of platelet activating factor to immune complex mediated inflammation. In: Handley DA, Saunders R, Houlihan W, Tomesch J (eds) Platelet activating factor in immune complex and endotoxin mediated diseases. Dekker, New York, pp 367–386

    Google Scholar 

  • Herbert JM, Lespy L, Maffrand JP (1991) Protective effect of SR 27417, a novel PAF antagonist, on lethal anaphylactic and endotoxin-induced shock in mice. Eur J Pharmacol 205:271–276

    Article  PubMed  CAS  Google Scholar 

  • Heuer HO (1991a) Inhibition of active anaphylaxis in mice and guinea pigs by the new hetrazepinoic PAF antagonist bepafant (WEB 2170). Eur J Pharmacol 199:157–163

    Article  PubMed  CAS  Google Scholar 

  • Heuer HO (1991b) WEB 2347: pharmacology of a new very potent and long acting hetrazepinic PAF antagonist and its action in repeatedly sensitized guinea pigs. J Lipid Mediat 4:39–44

    PubMed  CAS  Google Scholar 

  • Houlihan WJ, Lee ML, Nemecek GM, Handley DA, Winslow CM, Jaeggi C (1987) Antitumor activity of SRI 62–834, a cyclic ether analogue of ET-18-OCH3. Lipids 22:884–890

    Article  PubMed  CAS  Google Scholar 

  • Houlihan WJ, Cheon SH, Handley DA, Larson DA (1991) Synthesis and pharmacology of a novel class of long-lasting PAF antagonists. J Lipid Mediat 3:91–99

    PubMed  CAS  Google Scholar 

  • Houlihan WJ, Lee ML, Munder P, Handley DA, Jaeggi SC, Winslow C (1994) Antitumor activity of a piperidine phospholipid. Drug Res 44:1348–1388

    Google Scholar 

  • Houlihan WJ, Munder P, Handley DA, Cheon SH, Parillo VA (1995a) Antitumor activity of 5-aryl-2,3 dihydroimidazo [2,1-a] isoquinolines. J Med Chem 38:234–240

    Article  PubMed  CAS  Google Scholar 

  • Houlihan WJ, Munder P, Handley DA, Nemecek GA (1995b) 5-(4′-piperidinomethyl phenyl) 2,3-dihydroimidazo [2,1-a] isoquinoline (SDZ 62–434). A novel antitumor agent. Drug Res 22:1143–1155

    Google Scholar 

  • Hsueh W, Gonzalez-Crussi F, Arroyave J (1987) Platelet activating factor: an endogenous mediator of bowel necrosis endotoxemia. FASEB J 1:403–406

    PubMed  CAS  Google Scholar 

  • Hwang MN, Chang ML, Garcia QQ, Huang L, King VF (1987) L-652–469, a dual antagonist of platelet activating factor and dihydropyridines from Tussilago farfara. Eur J Pharmacol 141:269–278

    Article  PubMed  CAS  Google Scholar 

  • Hwang SB (1987) Specific receptor sites for platelet activating factor on rat liver plasma membranes. Arch Biochem Biophys 257:339–344

    Article  PubMed  CAS  Google Scholar 

  • Hwang SB, Lam M (1986) Species difference in the specific receptor of platelet activating factor. Biochem Pharmacol 35:4511–4518

    Article  PubMed  CAS  Google Scholar 

  • Hwang S, Lam M, Biftu T, Beattie T, Shen T (1985) Trans 2,5 bis-(3,4,5-trimethoxyphenyl) tetrahydrofuran. J Biol Chem 260:15639–15645

    PubMed  CAS  Google Scholar 

  • Hwang SB, Lam MH, Li CL, Shen TY (1986) Release of platelet activating factor and its involvement in the first phase of carrageenin-induced rat foot edema. Eur J Pharmacol 120:33–41

    Article  PubMed  CAS  Google Scholar 

  • Hwang SB, Lam M, Alberts A, Bugianesi R, Chabala J, Ponpipom M (1988) Biochemical and pharmacological characterization of L-659,989: an extremely potent, selctive and competitive receptor antagonist to platelet activating factor. J Pharmacol Exp Ther 246:534–541

    PubMed  CAS  Google Scholar 

  • Ide S, Kawahara K, Takahashi T, Sasaki N, Shingu H, Nagayasu T, Yamamoto S, Tagawa T, Tomita M (1995) Donor administration of PAF antagonist (TCV-309) enhances lung preservation. Transplant Proc 27:570–573

    PubMed  CAS  Google Scholar 

  • Inarrea P, Gomez-Cambronero J, Nieto M, Sanchez Crespo M (1984) Characteristics of the binding of platelet activating factor to platelets to different animal species. Eur J Pharmacol 105:309–315

    Article  PubMed  CAS  Google Scholar 

  • Inarrea P, Gomez-Cambronero J, Pascual J, del Carmen Ponte M, Hernando L, Sanchez-Crespo M (1985) Synthesis of PAF acether and blood volume changes in Gram negative sepsis. Immunopharmacology 9:45–52

    Article  PubMed  CAS  Google Scholar 

  • Ishida K, Thompson R, Beattie LL, Wiggs B, Schellenberg RR (1990) Inhibition of antigen-induced airway hyperresponsiveness, but not acute hypoxia nor airway eosinophilia, by an antagonist of platelet-activating factor. J Immunol 144:3907–3911

    PubMed  CAS  Google Scholar 

  • Ito S, Camussi G, Tetta C, Milgrom F, Andres G (1984) Hyperacute renal allograft rejection in the rabbit. Lab Invest 51:148–161

    PubMed  CAS  Google Scholar 

  • Jackson C, Schumacher W, Kunkel S, Driscoll E, Lucchesi B (1986) Platelet activating factor and the release of a platelet-derived coronary artery vasodilator substance in the canine. Circ Res 58:218–229

    PubMed  CAS  Google Scholar 

  • Jancar S, Abdo E, Sampietre M, Kwasniewski FH, Coelho AMM, Bonizzia A, Machado MCC (1995) Effect of PAF antagonists on cerulein-induced pancreatitis. J Lipid Mediat Cell Signal 11:41–49

    Article  PubMed  CAS  Google Scholar 

  • Joly F, Bessou G, Benveniste J, Ninio E (1987) Ketotifen inhibits Paf-acether biosynthesis and b-hexosaminidase release in mouse mast cells stimulate with antigen. Eur J Pharmacol 144:133–139

    Article  PubMed  CAS  Google Scholar 

  • Komuro Y, Imanishi N, Uchida M, Morooka S (1991) Biological effect of orally active platelet activating factor receptor antagonist SM-10661. Mol Pharmacol 38:378–384

    Google Scholar 

  • Kornecki E, Ehrlich Y, Lenox R (1984) Platelet activaing factor induced aggregation of human platelets specifically inhibited by triazolobenzodiazepines. Science 226:1954–1957

    Article  Google Scholar 

  • Kroegel C, Yakawa T, Westwick J, Barnes PJ (1989) Evidence for two distinct platelet activating factor receptors on eosinophils: dissociation between PAF-induced in-tracellular calcium mobilization and Superoxide anion generation in eosinophils. Biochem Biophys Res Commun 162:511–521

    Article  PubMed  CAS  Google Scholar 

  • Lagente V, Desquand S, Hadvary P, Cirino M, Lellouch-Tubiana A, Vargaftig BB (1988) Interference of Paf antagonist Ro 19–3704 with Paf and antigen-induced bronchoconstriction in the guinea pig. Br J Pharmacol 94:27–36

    PubMed  CAS  Google Scholar 

  • Lee T, Lenihan D, Malone B, Roddy L, Wasserman S (1984) Increased biosynthesis of platelet activating factor in activated human eosinophils. J Biol Chem 259:5526–5530

    PubMed  CAS  Google Scholar 

  • Lefort J, Sedivy P, Desquand S, Randon J, Coeffier E, Floch A, Benveniste J, Vargaftig BB (1988) Pharmacological profile of 48740 R.P., a PAF acether antagonist. Eur J Pharmacol 150:257–268

    Article  PubMed  CAS  Google Scholar 

  • Lellouch-Tubiana A, Lefort J, Simon MT, Pfister A, Vargaftig BB (1988) Eosinophil recruitment into guinea pig lungs after PAF-acether and allergen administration. Am Rev Respir Dis 137:948–954

    PubMed  CAS  Google Scholar 

  • Lepran I, Lefer AM (1985) Ischemia aggravating effects of platelet activating factor in acute myocardial ischemia. Basic Res Cardiol 80:135–141

    Article  PubMed  CAS  Google Scholar 

  • Lewis AJ, Dervinis A, Chang J (1984) The effects of antiallergic and bronchodilator drugs on platelet activating factor (PAF-acether) bronchospasm and platelet aggregation. Agents Actions 15:636–642

    Article  PubMed  CAS  Google Scholar 

  • Lohman IC, Halonen M (1990) Effects of the PAF antagonist WEB 2086 on PAF-induced physiological alterations and on IgE anaphylaxis in the rabbit. Am Rev Respir Dis 142:390–397

    PubMed  CAS  Google Scholar 

  • Luo G, Albert DH, Rhein DA, Conway RG, Sheppard GS, Summers JB, Carter GW (1993) A-79981: a novel PAF antagonist blocks endotoxin induced small intestinal damage in conscious rats. J Immunol 150:211A

    Google Scholar 

  • Ma Y, Dunham E (1988) Antagonism of the vasodilator effects of a platelet activating factor precursor in anesthetized spontaneously hypertensive rats. Eur J Pharmacol 145:153–162

    Article  PubMed  CAS  Google Scholar 

  • Makowka L, Miller C, Chapchap P, Podestra P, Pan C, Pressely D, Mazzaferro V, Esquivel C, Todo S, Banner B, Jaffe R, Saunders R, Starzel TE (1987) Prolongation of pig-to-dog renal xenograft survival by modification of the inflammatory mediator response. Annu Surg 206:482–495

    Article  CAS  Google Scholar 

  • Makowka L, Chapman F, Cramer D, Qian S, Sun H, Starzel TE (1990) Platelet activating factor and hyperacute rejection. Transplantation 50:359–365

    CAS  Google Scholar 

  • Malavasi F, Tetta C, Funaro A (1986) Fc receptor triggering induced expression of surface activation antigens and release of platelet activating factor in large granulocytes. Proc Natl Acad Sci USA 83:2443–2447

    Article  PubMed  CAS  Google Scholar 

  • Marquis O, Robaut C, Cavero I (1988) [3H] 52770 RP, a platelet activating factor receptor antagonist, and tritiated platelet activating factor label a common specific binding site in human polymorphoncuclear leukocytes. J Pharmacol Exp Ther 244:709–715

    PubMed  CAS  Google Scholar 

  • McFadden RG, Bishop MA, Caveney AN, Fraher LJ (1995) Effect of platelet activating factor (PAF) on the migration of human lymphocytes. Thorax 50:265–269

    Article  PubMed  CAS  Google Scholar 

  • Mclntyre T, Zimmerman G, Prescott S (1986) Leukotrienes C4 and D4 stimulate human endothelial cells to synthesize platelet activating factor and bind neutrophils. Proc Natl Acad Sci USA 83:2204–2208

    Article  Google Scholar 

  • Meade CJ, Heuer H, Kempe R (1991) Biochemcial pharmacology of platelet activating factor (and PAF antagonists) in relation to clinical and experimental throm-bocytopenia. Biochem Pharmacol 41:657–668

    Article  PubMed  CAS  Google Scholar 

  • Merlos M, Gomez LA, Giral M, Vericat ML, Rafanell JG, Forn J (1991) Effects of PAF antagonists in mouse ear oedema induced by serveral inflammatory agents. Br J Pharmacol 104:990–994

    PubMed  CAS  Google Scholar 

  • Minor T, Yamaguchi T, Isselhard W (1995) Treatment of preservation/reperfusion injury by platelet activating factor antagonism in the rat liver graft. Transplant Proc 27:522–523

    PubMed  CAS  Google Scholar 

  • Misawa M, Takata T (1988) Effects of platelet activating factor on rat airways. Jpn J Pharmacol 48:7–13

    Article  PubMed  CAS  Google Scholar 

  • Miyamoto T, Ohno H, Yano T, Okada T, Hamanaka N, Kawasaki A (1985) Ono-6240: a new potent antagonist of platelet activating factor. In: Hayaishi O, Yamamoto S (eds) Adv Prostaglandin Thromboxane Leukot Res 15:719–720

    Google Scholar 

  • Mojarad M, Hamasaki Y, Said IS (1983) Platelet activating factor increases pulmonary microvascular permeability and induced pulmonary edema. Bull Eur Physiopath Respir 19:253–256

    CAS  Google Scholar 

  • Mondot S, Cavero I (1988) Cardiovascular profile of 59227 RP, a novel potent and specific PAF receptor antagonist. Prostaglandin 35:827

    Article  Google Scholar 

  • Montrucchio G, Alloatti G, Mariano F, De Paulis R, Comino A, Emanuelli G, Camussi G (1990) Role of platelet activating factor in the reperfusion injury of rabbit ischemie heart. Am J Pathol 137:71–81

    PubMed  CAS  Google Scholar 

  • Myers A, Ramey E, Ramwell P (1983) Glucocorticoid protectin against PAF-acether toxicity in mice. Br J Pharmacol 79:595–598

    PubMed  CAS  Google Scholar 

  • Nagaoka J, Harada K, Kimura A, Kobayashi S, Murakami M, Yoshimura K, Yamada K, Asano O, Katayama K, Yamatsu S (1991) Inhibitory effects of the novel platelet activating factor receptor antagonist, l-ethyl-2-[N-(2-methoxy) benzoyl-N-[(2R) 2-methoxy 3-(4-octadecylcarbamoyloxy) piperidinocarbonyl oxypropyloxy] carbonyl] aminomethyl pyridinium chloride, in several experimentally induced shock models. Drug Res 41:719–724

    CAS  Google Scholar 

  • Namm DH, Tadepalli AS, High JA (1982) Species specificity of the platelet response to 1-O-alkyl-2-acetyl sn glycero-3-phosphocholine. Thromb Res 25:341–350

    Article  PubMed  CAS  Google Scholar 

  • Nathan N, Denizot Y (1995) PAF and human cardiovascular disorders. J Lipid Mediat Cell Signall 11:103–104

    Article  CAS  Google Scholar 

  • Natsume Y, Inanishi N, Koike H, Morooka S (1994) Effect of the platelet activating factor antagonist (+)-cis-3,5-dimethyl-2-(3-pyridyl) thiazolidin-4-one hydrochlo-ride on endotoxin-induced hypotension and hematological parameters in rats. Drug Res 44:1208–1213

    CAS  Google Scholar 

  • Neuwirth R, Singhal P, Satriano J, Braquet P, Schlondorff D (1987) Effect of platelet activating factor antagonists on cultured rat mesangial cells. J Pharmacol Exp Ther 242:409–414

    Google Scholar 

  • Nguyen P, Petitfrere E, Potron G (1995) Mechanisms of the platelet aggregation induced by activated neutrophils and inhibitory effect of specific PAF receptor antagonist. Thromb Res 78:33–42

    Article  PubMed  CAS  Google Scholar 

  • Nunez D, Chignard M, Korth R, Le Couedic J, Norel X, Spinnewyn B, Braquet P, Benveniste J (1986) Specific inhibition of PAF-acether induced platelet activation by BN 52021 and comparison with the PAF acether inhibitors kadsurenone and CV-3988. Eur J Pharmacol 123:197–205

    Article  PubMed  CAS  Google Scholar 

  • O’Donnell SR, Erjefalt I, Persson GA (1990) Early and late tracheobronchial plasma exudation by platelet activating factor administered to the airway mucosal surface in guinea pigs: effects of WEB 2086 and enprofylline. J Pharmacol Exp Ther 254:65–70

    PubMed  Google Scholar 

  • Okamoto M, Yoshida K, Nishikawa N (1986a) FR-900452, a specific antagonist of platelet activating factor (PAF) produced by Streptomyces phaeofaciens. J Antibiot (Tokyo) 39:198–204

    CAS  Google Scholar 

  • Okamoto M, Yoshida K, Nishikawa M, Kohsaka M, Aoki H (1986b) Platelet activating factor (PAF) involvement in endotoxin induced thrombocytopenia in rabbits: studies with FR-900452, a specific inhibitor of PAF. Thromb Res 42:661–671

    Article  PubMed  CAS  Google Scholar 

  • Olson NC (1992) SRI 63–675: a platelet activating factor receptor antagonist. Cardiovasc Drug Rev 10:54–70

    Article  CAS  Google Scholar 

  • Ortega MP, Cillero F, Narvaiza J, Maroto ML, Smith CA, Redpath K, Priego JC (1992) Effectiveness, tolerance and plasma levels of PCA-4248, a new PAF antagonist, after administration in human healthy volunteers. In: 4th International Congress on PAF and Related Lipid Mediators, Paris, Abstr c4.2

    Google Scholar 

  • Page CP, Morley J (1986) Evidence favouring PAF rather than leukotrienes in the pathogesesis of asthma. Pharmacol Res Commun 18:217–237

    Article  PubMed  CAS  Google Scholar 

  • Paris D, Cottin M, Demonchaux P, Augert G, Dupassieux P, Lenoir P, Peck M, Jasserand D (1995) Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo [3,2,1-ij] quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic applications in asthma. J Med Chem 38:669–685

    Article  PubMed  CAS  Google Scholar 

  • Patterson R, Harris KE (1983) The activity of aerosolized and intracuteneous synthetic platelet activating factor (AGEPC) in rhesus monkeys with IgE mediated airway responses and normal monkeys. J Lab Clin Med 102:933–938

    PubMed  CAS  Google Scholar 

  • Patterson R, Bernstein PR, Harris KE, Krell PD (1984) Airway responses to sequential challenges with platelet actiavting factor and leukotriene D4 in rhesus monkey. J Lab Clin Med 104:340–345

    PubMed  CAS  Google Scholar 

  • Patterson R, Harris KE, Lee ML, Houlihan WJ (1986) Inhibition of rhesus monkey airway and cutaneous responses to platelet activating factor (PAF) (AGEPC) with the anti-PAF agent SRI 63–072. Int Arch Allergy Appl Immunal 81:265–272

    Article  CAS  Google Scholar 

  • Patterson R, Harris KE, Handley DA, Saunders RN (1987) Evaluation of the effect of a platelet activating factor (PAF) receptor antagoniston platelet activating factor and ascaris antigen-induced airway respones in rhesus monkeys. J Lab Clin Med 110:606–611

    PubMed  CAS  Google Scholar 

  • Patterson R, Harris KE, Bernstein PR, Krell RD, Handley DA, Saunders RN (1989) Effects of combined receptor antagonists of leukotriene D4 (LTD4) and platelet activating factor (PAF) on rhesus airway responses to LTD4, PAF and antigen. Int Arch Allergy Appl Immunol 88:462–470

    Article  PubMed  CAS  Google Scholar 

  • Perico N, Delaini F, Tagliaferri M, Abbate M, Cucchi M, Bertani T, Remuzzi G (1988) Effect of platelet activating factor and its specific receptor antagonist on glomerular permeability to proteins in isolated perfused rat kidney. Lab Invest 58:163–171

    PubMed  CAS  Google Scholar 

  • Pettipher ER, Higgs GA, Henderson B (1987) PAF-acether in chronic arthritis. Agents Actions 21:98–103

    Article  PubMed  CAS  Google Scholar 

  • Pinckard R, Ludwig JC, McManus L (1988) Platelet activating factors. In: Gallin JI, Goldstein I, Snyderman R (eds) Inflammation: basic principles and clinical correlates. Raven, New York, pp 1–46

    Google Scholar 

  • Pinckard RN, Woodard DS, Showell HJ, Conklyn MJ, Novak MJ, McManus LM (1994) Structural and (patho)physiological diversity of PAF. Clin Rev Allergy 12:329–359

    PubMed  CAS  Google Scholar 

  • Pinquier JL, Sedivy P, Bruno R, Bompart E, Grégoire J, Strauch G, Gaillot J, Clucas A (1991) Inhibitin of ex vivo PAF-induced platelet aggregation by the PAF antagonist RP 48740: relationship to plasma concentrations in healthy volunteers. Eur J Clin Pharmacol 41:141–145

    Article  PubMed  CAS  Google Scholar 

  • Ponipom M, Bugianesi R, Brokker S, Yue B, Hwang S, Shen T (1987) Structure-activity relationships of kadsurenone analogues. J Med Chem 30:136–142

    Article  Google Scholar 

  • Pons R, Rossi AG, Norman KE, Williams TJ, Nourshargh S (1993) Role of platelet activating factor (PAF) in platelet accumulation in rabbit skin: effect of the novel long-acting PAF antagonist UK-74,505. Br J Pharmacol 109:234–242

    PubMed  CAS  Google Scholar 

  • Pretolani M, Lefort J, Malanchere E, Vargaftig BB (1987) Interference by the novel PAF-acether antagonist WEB 2086 with the bronchopulmonary responses to PAF-acether and to active and passive anaphylactic shock in guinea pigs. Eur J Pharmacol 140:311–321

    Article  PubMed  CAS  Google Scholar 

  • Rabinovici R, Yue T, Farhat M, Smith EF, Esser KM, Slivjak M, Feuerstein G (1990) Platelet activating factor (PAF) and tumor necrosis factor-a (TNFa) interactions in endotoxemic shock: studies with BN 50739, a novel PAF antagonist. J Pharmacol Exp Ther 255:256–263

    PubMed  CAS  Google Scholar 

  • Rayamajhi P, Bruchhausen Fv (1989) Inhibition in vitro of PAF biosynthesis from lyso-PAF by antirheumatic gold salts and gold compounds. Arch Pharmacol 340:R84 Renooij W, Snyder F (1981) Biosynthesis of 1-alkyl 2-acetyl sn-glycero-3-phosphocholine (platelet activating factor and a hypotensive lipid) by cholinephosphotransferase in various rat tissues. Biochim Biophys Acta 663:545–556

    Google Scholar 

  • Robaut C, Durand G, James C, Lave D, Sedivy P, Floch A, Mondot S, Pacot D, Cavero I, Le Fur G (1987) PAF binding sites. Characterization by [3H] 52770, a pyrrolo [1,2c] thiazole derivative, in rabbit platelets. Biochem Pharmacol 36:3221–3229

    Article  PubMed  CAS  Google Scholar 

  • Robaut C, Mondot S, Floch A, Tahraoue L, Cavero I (1988) Pharmacological profile of a novel, potent and specific PAF receptor antagonist the 59227 RP. Prostaglandins 35:838

    Article  Google Scholar 

  • Robertson DA, Genovese A, Levi R (1987) Negative inotropic effect of platelet activating factor on human myocardium: a pharmacological study. J Pharmacol Exp Ther 243:834–839

    PubMed  CAS  Google Scholar 

  • Robertson DA, Wang DY, Lee CO, Levi R (1988) Negative inotropic effect of platelet activating factor: association with a decrease in intracellular sodium activity. J Pharmacol Exp Ther 245:124–128

    PubMed  CAS  Google Scholar 

  • Rosam A, Wallace J, Whittle B (1986) Potent ulcerogenic actions of platelet activating factor on the stomach. Nature 319:54–56

    Article  PubMed  CAS  Google Scholar 

  • Rylander R, Beijer L (1987) Inhalation of endotoxin stimulates alevolar macrophage production of platelet activating factor. Am Rev Respir Dis 135:83–86

    PubMed  CAS  Google Scholar 

  • Sakuma Y, Muramoto K, Harada K, Katayama S, Tsunoda H, Katayama K (1991) Inhibitory effects of a novel PAF antagonist E6123 on anaphylactic responses in passively and actively sensitized guinea pigs and passively sensitized mice. Prostaglandins 42:541–555

    Article  PubMed  CAS  Google Scholar 

  • Saito M, Fujimura M, Ogawa H, Matsuda T (1995) Role of thromboxane A2 and platelet-activating factor in allegic bronchoconstriction in guinea pig airway in vivo. J Lipid Mediat Cell Signal 11:1–12

    Article  PubMed  CAS  Google Scholar 

  • Sanjar S, Aoki S, Boubekeur K, Chapman I, Smith D, Kings M, Morley J (1990a) Eosinophil accumulation in pulmonary airways of guinea pigs induced by exposure to an aerosol of platelet activating factor: effect of anti-asthma drugs. Br J Pharmacol 99:267–272

    PubMed  CAS  Google Scholar 

  • Sanjar S, Aoki S, Kristersson A, Smith D, Morley J (1990b) Antigen challenge induces pulmonary eosinophil accumulation and airway hyperreactivity in sensitized guinea pigs: the effect of anti-asthma drugs. Br J Pharmacol 99:679–686

    PubMed  CAS  Google Scholar 

  • Satoh K, Imaizumi T, Kawamura Y, Yoshida H, Takamatsu S, Mizono S, Shoji B, Takamatsu M (1988) Activity of platelet-activating factor (PAF) acetylhydrolase in plasma from patients with ischemic cerebrovascular disease. Prostaglandins 35:685–698

    Article  PubMed  CAS  Google Scholar 

  • Saunders RN, Handley DA (1987) Platelet activating factor antagonists. Annu Rev Pharmacol Toxicol 27:237–255

    Article  PubMed  CAS  Google Scholar 

  • Saunders R, Handley DA (1990) PAF and immunopathological responses. In: Handley DA, Saunders R, Houlihan W, Tomesch J (eds) Platelet activating factor in immune complex and endotoxin mediated diseases. Dekker, New York, pp 223–246

    Google Scholar 

  • Schleimer RP, MacGlashan DW, Peters S, Pinckard N, Adkinson N, Lichtenstein LW (1986) Characterization of inflammatory mediator release from purified human lung mast cells. Am Rev Respir Dis 133:614–617

    PubMed  CAS  Google Scholar 

  • Seth P, Kumari R, Dikshit M, Srimal RC (1994) Effect of platelet activating factor antagonists in different models of thrombosis. Thromb Res 76:503–512

    Article  PubMed  CAS  Google Scholar 

  • Shen TY, Hwang S, Chang M, Doebber T, Lam M, Wu M, Wang X, Han G, Li R (1985) Characterizartion of a platelet activating factor receptor antagonist isolated from haifenteng (Piper futokadsura): specific inhibition if in vitro and in vivo platelet activating factor induced effects. Proc Natl Acad Sci USA 82:672–676

    Article  PubMed  CAS  Google Scholar 

  • Sheppard GS, Pireh D, Carrera GM, Bures MG, Heyman HR, Steinman DH, Davidson H et al. (1994) 3-(2-(3-pyridinyl) thiazolid-4-oyl)-indoles, a novel series of PAF antagonists. J Med Chem 37:2011–2032

    Article  PubMed  CAS  Google Scholar 

  • Sisson JH, Prescott SM, Mclntyre TM, Zimmerman GA (1987) Production of platelet activating factor by stimulated polymorphonculear leukocytes. J Immunol 138:3918–3926

    PubMed  CAS  Google Scholar 

  • Smallbone B, Taylor NE, McDonald JW (1987) Effects of L652,731, a platelet activating factor (PAF) receptor antagonist, on PAF- and complement-induced pulmonary hypertension in sheep. J Pharmacol Exp Ther 242:1035–1040

    PubMed  CAS  Google Scholar 

  • Snyder F (1995) Platelet-activating factor and its analogs: metabolic pathways and related intracellular processes. Biochim Biophys Acta 1254:231–249

    PubMed  Google Scholar 

  • Stahl GL, Terashita ZI, Lefer AM (1986) Role of platelet activating factor on propagation of cardiac damage during myocardial ischemia. J Pharmacol Exp Ther 244:898–904

    Google Scholar 

  • Stahl GL, Terachita Z, Lefer AM (1988) Role of platelet activating factor in propagation of cardiac damage during myocardial ischemia. J Pharmacol Exp Ther 244:898–904

    PubMed  CAS  Google Scholar 

  • Steil AA, Rodriguez MDCG, Alonso A, Sanchez Crespo M, Bosca L (1995) Platelet-activating factor: the effector of protein-rich plasma extravasation and nitric-oxide synthase induction in rat immune complex peritonitis. Br J Pharmacol 114:895–901

    PubMed  CAS  Google Scholar 

  • Stenzel H, Hummer B, Hahn H (1987) Effect of the PAF antagonist SRI 63–441 on the allergic response in wake dogs with natural asthma. Agents Actions 21:253–260

    Article  CAS  Google Scholar 

  • Stewart A, Dusting G (1988) Characterization of receptor for platelet activating factor on platelets, polymorphonuclear leukocytes and macrophages. Br J Pharmacol 94:1225–1233

    PubMed  CAS  Google Scholar 

  • Stockmans F, Arnout J, Depre M, DeSchepper P, Argehrn JC, Vermylen J (1991) TCV-309, a novel PAF antagonist, inhibits PAF induced human platelet aggregation ex vivo. Thromb Haemost 65: 1108–1117

    Google Scholar 

  • Summers JB, Albert DH (1995) Platelet activating factor antagonists. Adv Pharmacol 32:67–168

    Article  PubMed  CAS  Google Scholar 

  • Takada Y, Boudjema K, Jaeck D, Chenard MP, Wolf P, Cliqualbre J, Yamaoka Y (1995) Platelet activating factor antagonist has a protective effect on preservation/reperfusion injury of the graft in pig liver transplant. Transplant Proc 27:747–748

    PubMed  CAS  Google Scholar 

  • Takatani M, Yoshioka Y, Tasaka A, Terashita ZI, Imura Y, Nishikawa K, Tsuhima S (1989) Platelet activating factors antagonists: synthesis and structure activity studies of a novel PAF antagonist modified in the phosphorylcholine moiety. J Med Chem 32:56–64

    Article  PubMed  CAS  Google Scholar 

  • Takehara S, Mikashima H, Muramoto Y, Terasawa M, Setoguchi M, Tahara T (1990) Pharmacological actions of Y-24180, a new specific antagonist of platelet activating factor (PAF): II. Interactions with PAF and benzodiazepine receptors. Prostaglandins 40:571–583

    Article  PubMed  CAS  Google Scholar 

  • Tanabe Y, Yamamoto H, Murakami M, Yanagi K, Kubota Y, Okumura H, Sanemitsu Y, Suzukamo G (1995) Synthetic study of the highly potent and selective anti-platelet activating factor thiazolidin-4-one agents and related compounds. J Chem Soc Perkin Trans 1:935–947

    Article  Google Scholar 

  • Terasawa M, Mikashima H, Tahara T, Maruyama Y (1987) Antagonistic activity of etizolam on platelet activating factor in vivo experiments. Jpn J Pharmacol 44:381–386

    Article  PubMed  CAS  Google Scholar 

  • Terasawa M, Aratani H, Setoguchi M, Tahara M (1990) Pharmacological actions of Y-24180: I. A potent specific antagonist of platelet activating factor. Prostaglandins 40:553–569

    Article  PubMed  CAS  Google Scholar 

  • Terashita ZI, Tsushima S, Yoshioka Y, Nomura H, Inada Y, Nishikawa K (1983) CV-3988-a specific antagonist of platelet activating factor (PAF). Life Sci 32:1975–1982

    Article  PubMed  CAS  Google Scholar 

  • Terashita Z, Imura Y, Nishikawa K (1985) Inhibition by CV-3988 of the binding of [3H]-platelet activating factor (PAF) to the platelet. Biochem Pharmacol 34:1491–1499

    Article  PubMed  CAS  Google Scholar 

  • Terashita Z, Imura Y, Takatani M, Tsushima S, Nishikawa K (1987) CV-6209: a highly potent platelet activating factor antagonist in vitro and in vivo. J Pharmacol Exp Ther 242:263–268

    PubMed  CAS  Google Scholar 

  • Terashita Z, Kawamura M, Takatani M, Tsushima S, Imura Y, Nishikawa K (1992) Benefitial effects of TCV-309, a novel potent and selective platelet activating factor antagonist in endotoxin and anaphylacitic shock in rodents. J Pharmacol Exp Ther 260:748–755

    PubMed  CAS  Google Scholar 

  • Tetta C, Camussi G, Bussolino F, Herrick-Davis K, Baglioni C (1991) Inhibition of the synthesis of platelet activating factor by antiinflammatory peptides (antiflammins) without methionine. J Pharmacol Exp Ther 257:616–620

    PubMed  CAS  Google Scholar 

  • Tomioka K, Garrido R, Ahmed A, Stevenson JS, Abraham WM (1989) YM 461, PAF antagonist, blocks antigen-induced late airway responses and airway hyperresponsiveness in allergic sheep. Eur J Pharmacol 170:209–215

    Article  PubMed  CAS  Google Scholar 

  • Tramposch KM, Chilton FH, Stanley PL, Franson RC, Havens MB, Nettleton DO, Davern LB, Sarling IM, Bonney RJ (1993) Inhibitor of phospholipase A2 blocks eicosanoid and platelet activating factor biosynthesis and has topical anti-inflammatory activity. J Pharmacol Exp Ther 271:852–859

    Google Scholar 

  • Ueno A, Ishida H, Oh-ishi S (1995) Comparative study of endotoxin-induced hypotension in kininogen-deficient rats with that in normal rats. Br J Pharmacol 114:1250–1256

    PubMed  CAS  Google Scholar 

  • Ukena D, Krogel C, Yukawa T, Sybrecht G, Barnes PJ (1989) PAF-receptors on eosinophils: identification with a novel ligand, [3H] WEB 2086. Biochem Pharmacol 38:1702–1705

    Article  PubMed  CAS  Google Scholar 

  • Underwood SL, Lewis SA, Raeburn D (1992) RP 59227, a novel PAF receptor antagonist: effects in guinea pig models of airway hyperreactivity. Eur J Pharmacol 210:97–102

    Article  PubMed  CAS  Google Scholar 

  • Vargaftig BB, Lefort J, Chicnard M, Benveniste J (1980) Platelet activating factor induced platelet-dependent bronchoconstriction unrelated to the formation of Prostaglandin derivatives. Eur J Pharmacol 65:185–192

    Article  PubMed  CAS  Google Scholar 

  • Vargaftig BB, Lefort J, Rotilio D (1983) Route-dependent interactions between PAF-acether and guinea pig bronchopulmonary smooth muscle: relevance of cyclooxygenase mechanisms. In: Benveniste J, Arnoux A (eds) Platelet activating factor. INSERM Symposium. Elsevier, Amsterdam, pp 307–313

    Google Scholar 

  • Wallace JL, Steel G, Whittle B, Lagente V, Vargaftig BB (1987) Evidence for platelet activating factor as a mediator of endotoxin induced gastrointestinal damage in the rat. Gastroenterology 93:765–773

    PubMed  CAS  Google Scholar 

  • Wang J, Kester M, Dunn M (1988) The effects of endotoxin on platelet activating factor synthesis in cultured rat glomerular mesangial cells. Biochim Biophys Acta 969:217–224

    Article  PubMed  CAS  Google Scholar 

  • Whately R, Zimmerman G, Mclntyre T, Prescott S (1988) Endothelium from diverse vascular sources synthesizes platelet activating factor. Arteriosclerosis 8:321–331

    Article  Google Scholar 

  • Whittaker M (1993) PAF receptor antagonists: recent advances. Curr Opin Ther Pat 3:1569–1573

    Article  Google Scholar 

  • Whittaker M, Beauchamp CL, Bowles SA, Cakett KS, Christodoulou MS, Galloway WA, Longstaff DS, McGuinness GP, Miller A, Timiiis DJ, Wood LM (1992) BB-823, a PAF receptor antagonist with picomolar activity. Pharmacol Comm 1:251–257

    CAS  Google Scholar 

  • Whittle B, Boughton-Smith N, Hutcheson I, Esplugues JV, Wallace JL (1987) Increased intestinal formation of Paf in endotoxin induced damage in the rat. Br J Pharmacol 92:3–4

    PubMed  CAS  Google Scholar 

  • Wilkens JH, Wilkens H, Uffmann J, Bovers J, Fabel H, Frolich JC (1990) Effects of the PAF antagonist (BN 52063) on bronchoconstriction and platelet activation during exercise induced asthma. Br J Clin Pharmacol 29:85–91

    PubMed  CAS  Google Scholar 

  • Wilkens H, Wilkens JH, Bosse S (1991) Effects of an inhaled PAF antaongist (WEB 2086) on allergen-induced early and late asthmatic responses and increased bronchial responsiveness to methacholine. Am Rev Respir Dis 143:A812

    Google Scholar 

  • Winslow C, Anderson R, D’Aries F, Frisch G, DeLillo A, Lee M, Saunders RN (1987) Toward understanding the mechanism of action of platelet activating factor antagonists. In: Winslow CM, Lee ML (eds) New horizons in platelet activating factor research. Wiley, New York, pp 153–168

    Google Scholar 

  • Yamazaki R, Sugatani J, Fujii I, Kuroyangi M, Umehara K, Ueno A, Suzuki Y, Miwa M (1994) Development of a novel method for determination of acetyl-coA: 1-alkyl-sn- glycero-3-phosphocholine acetyltransferase activity and its application to screening for acetyltransferase inhibitors. Biochem Pharmacol 47:995–1006

    Article  PubMed  CAS  Google Scholar 

  • Yin M, Kurvers HAJM, Buurman WA, Tangelder GJ, Booster MH, Daemen JHC, Kondracki S, Kootstra G (1995) Beneficial effect of platelet-activating factor antagonist TCV-309 on renal ischemia-reperfusion injury. Transplant Proc 27:774–776

    PubMed  CAS  Google Scholar 

  • Zanglis A, Lianos EA (1987) Platelet activating factor biosynthesis and degradation in the rat glomeruli. J Lab Clin Med 110:330–337

    PubMed  CAS  Google Scholar 

  • Zehr KJ, Poston RS, Lee PC, Uthoff K, Kumar P, Cho PW, Gillinov AM, Redmond JM, Wilkenstein JA, Herskowitc A, Cameron DE (1995) Platelet activating factor inhibition reduces lung injury after cardiopulmonary bypass. Ann Thorac Surg 59:328–335

    Article  PubMed  CAS  Google Scholar 

  • Zhou W, Chao W, Levine BA, Olsen MS (1990) Evidence for platelet activating factor as a late phase mediator of chronic pancreatitis in the rat. Am J Pathol 137:1501–1508

    PubMed  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1997 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Handley, D. (1997). Biosynthetic Inhibitors and Receptor Antagonists to Platelet Activating Factor. In: von Bruchhausen, F., Walter, U. (eds) Platelets and Their Factors. Handbook of Experimental Pharmacology, vol 126. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-60639-7_24

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-60639-7_24

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-64488-7

  • Online ISBN: 978-3-642-60639-7

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics