Skip to main content
SpringerLink
Log in

Sarafotoxins and Their Relationship to the Endothelin Family of Peptides

  • Chapter
Book cover Endothelin and Its Inhibitors

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 152))

Abstract

The sarafotoxins (SRTXs), a family of peptides isolated from the venom of the snake Atractaspis engaddensis, show striking structural similarities to the endothelins (ETs) produced by endothelial cells. Four isoforms of SRTXs have been identified: SRTX-a, SRTX-b, SRTX-c, and SRTX-e. SRTX-d, which was previously assumed to exist, has not been found (Bdolah et al. 1989b). SRTXe differs from the proposed SRTX-d in having a Gly instead of an Asp in position 18 (Ducancel et al. 1993). These peptides have powerful cardiotoxic effects and cause contraction of smooth muscles. They all contain 21 amino acids and two disulfide bridges, between Cys1-Cys15 and Cys3-Cys11. There is a very high degree of sequence similarity, not only within each family (ETs, 71–95%; SRTXs, 81–95%), but also between families (52–67%) (Kochva et al. 1993). The ETs are produced in minute quantities in mammals (measurable in picomoles per gram of tissue), whereas the SRTXs are produced in large amounts in the venom of the snake (0.1 mmol/g). The SRTXs and ETs may be divided into two groups on the basis of their toxicity. The most lethal are ET1 and SRTX-b; ET-3 is less toxic, and SRTX-c and SRTX-e cause death only at very high doses, if at all. For example, in ICR mice, the LD50 for SRTX-b and ET-1 is 15 μg/kg body weight (Bdolah et al. 1989a). ET-1 and SRTX-b were found to cause severe disturbances in heart function at the level of the A-V conduction system and the coronary vessels, ultimately leading to cartiac arrest.

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

Access this chapter

Log in via an institution
Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
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

  • Andersen NH, Chen C, Marschner TM, Krystek SR, Bassolino DA (1992) Conformational isomerism of endothelin in acidic aqueous media: a quantitative NOESY analysis. Biochemistry 31:1280–1295

    Article  PubMed  CAS  Google Scholar 

  • Angelova K, Puett D, Narayan P (1997) Identification of endothelin receptor subtypes in sheep choroid plexus. Endocrine 7:287–293

    Article  PubMed  CAS  Google Scholar 

  • Arinami T, Ishikawa M, Inoue A, Yanagisawa M, Masaki T, Yoshida MC, Hamaguchi H (1991) Chromosomal assignments of the human endothelin family genes: the endothelin-1 gene (EDN1) to 6p23-p24, the endothelin-2 gene (EDN2) to lp34, and the endothelin-3 gene (EDN3) to 20q13.2-q13.3. Àm J Hum Genet 48:990–996

    PubMed  CAS  Google Scholar 

  • Atkins AR, Ralston GB, Smith R. (1994) Conformational stability of the endothelin/sarafotoxin family of peptides. Int J Peptide Protein Res 44:372–377

    Article  CAS  Google Scholar 

  • Atkins AR, Martin RC, Smith R (1995) 1H NMR studies of sarafotoxin SRTb, a nonselective endothelin receptor agonist, and IRL 1620, an ETB receptor-specific agonist. Biochemistry 34:2026–2033

    Article  PubMed  CAS  Google Scholar 

  • Bdolah A, Wollberg Z, Ambar I, Kloog Y, Sokolovsky M, Kochva E (1989a) Disturbances in the cardiovascular system caused by endothelin and sarafotoxin. Biochem Pharmacol 38:3145–3146

    Article  PubMed  CAS  Google Scholar 

  • Bdolah A, Wollberg Z, Fleminger G, Kochva E (1989b) SRTX-d, a new native peptide of the endothelin/sarafotoxin family. FEBS Lett 256:1–3

    Article  PubMed  CAS  Google Scholar 

  • Bdolah A, Wollberg Z, Kochva E (1991) Snake Toxins. In: Harvey L (ed) Pergamon, New York, pp 415–424

    Google Scholar 

  • Bdolah A, Kochva E, Ovadia M, Kinamon S, Wollberg Z (1997) Resistance of the Egyptian mongoose to sarafotoxins. Toxicon 35:1251–1261

    Article  PubMed  CAS  Google Scholar 

  • Becker A, Dowdle EB, Hechler U, Kauser K, Donner P, Schleuning WD (1993) Bibrotoxin, a novel member of the endothelin/sarafotoxin peptide family, from the venom of the burrowing asp Atractaspis bibroni. FEBS Lett 315:100–103

    Article  PubMed  CAS  Google Scholar 

  • Bell KM, Prise VE, Chaplin DJ, Tozer GM (1995) Effect of endothelin-1 and sarafotoxin S6c on blood flow in a rat tumor. J Cardiovasc Pharmacol 26:S222–S225

    PubMed  CAS  Google Scholar 

  • Bloch KD, Friedrich SP, Lee M-E, Eddy RL, Shows TB, Quertermous T (1989) Structural organization and chromosomal assignment of the gene encoding endothelin. J Biol Chem 264:10851–10857

    PubMed  CAS  Google Scholar 

  • Bodelsson G, Stjernquist M (1993) Characterization of endothelin receptors and localization of 125I-endothelin-1 binding sites in human umbilical artery. Eur J Pharmacol 249:299–305

    Article  PubMed  CAS  Google Scholar 

  • Bogoni G, Rizzo A, Calo G, Campobasso C, D’Orleans-Juste P, Regoli D (1996) Characterization of endothelin receptors in the human umbilical artery and vein. Br J Pharmacol 119:1600–1604

    Article  PubMed  CAS  Google Scholar 

  • Breuiller-Fouche M, Heluy V, Fournier T, Dallot E, Vacher-Lavenu MC, Ferre F (1998) Role of endothelin-1 in regulating proliferation of cultured human uterine smooth muscle cells. Mol Hum Reprod 4:33–39

    Article  PubMed  CAS  Google Scholar 

  • Calogero AE, Burrello N, Ossino AM (1998) Endothelin (ET)-1 and ET-3 inhibit estrogen and cAMP production by rat granulosa cells in vitro. J Endocrinol 157:209–215

    Article  PubMed  CAS  Google Scholar 

  • Clozel M, Gray GA, Breu V, Loffler B-M, Osterwalder K (1992) The endothelin ETB receptor mediates both vasodilation and vasoconstriction in vivo. Biochem Biophys Res Commun 186:867–873

    Article  PubMed  CAS  Google Scholar 

  • Cristol J-P, Warner T D,Thiemermaan C, Vane JR (1993) Mediation via different receptors of the vasoconstrictor effects of endothelins and sarafotoxins in the systemic circulation and renal vasculature of the anaesthetized rat. Br J Pharmacol 108:776–779

    Article  PubMed  CAS  Google Scholar 

  • Davenport AP, Morton AJ, Brown MJ. (1991) Localization of endothelin-1 (ET-1), ET-2, and ET-3, mouse VIC, and sarafotoxin S6b binding sites in mammalian heart and kidney. J Cardiovasc Pharmacol 17:S152–S155

    Article  PubMed  CAS  Google Scholar 

  • DeNucci G, Thomas R, D’Orleans-Juste P, Antunes E, Walder C, Warner TD, Vane JK (1988) Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium-derived relaxing factor. Proc Natl Acad Sci USA 85:9797–9800

    Article  CAS  Google Scholar 

  • Devadason PS, Henry PJ (1997) Comparison of the contractile effects and binding kinetics of endothelin-1 and sarafotoxin S6b in rat isolated renal artery. Br J Pharmacol 121:253–263

    Article  PubMed  CAS  Google Scholar 

  • Doherty AM, Cody WL, Leitz NL, Depue PL, Taylor MD, Rapundalo ST, Hingorani GP, Major TC, Panek RL, Taylor DG (1991) Structure-activity studies of the C-terminal region of the endothelins and sarafotoxins. J Cardiovasc Pharmacol 17:S59–S61

    Article  PubMed  CAS  Google Scholar 

  • Docherty C, MacLean MR (1998a) Development of endothelin receptors in perinatal rabbit pulmonary resistance arteries. Br J Pharmacol 124:1165–1174

    Article  PubMed  CAS  Google Scholar 

  • Docherty C, MacLean MR (1998b) EndothelinB receptors in rabbit pulmonary resistance arteries: effect of left ventricular dysfunction. J Pharmacol Exp Ther 284:895–903

    PubMed  CAS  Google Scholar 

  • Doi Y, Ozaka T, Katsuki M, Fukushige H, Toyama E, Kanazawa Y, Arashidani K, Fujimoto S (1995) Histamine release from Weibel-Palade bodies of toad aortas induced by endothelin-1 and sarafotoxin-S6b. Anat Rec 242:374–382

    Article  PubMed  CAS  Google Scholar 

  • Douglas SA, Hiley CR (1991) Endothelium-dependent mesenteric vasorelexant effects and systemic actions of endothelin(16–21) and other endothelin-related peptides in the rat. Br J Pharmacol 104:311–320

    Article  PubMed  CAS  Google Scholar 

  • Douglas SA, Beck GR Jr, Elliot JD, Ohlstein EH (1995) Pharmacologic evidence for the presence of three functional endothelin receptor subtypes in the rabbit lateral saphenous vein. Br J Pharmacol 114:1529–1540

    Article  PubMed  CAS  Google Scholar 

  • Ducancel F, Matre U, Dupont C, Lajeunesse E, Wollberg Z, Bdolah A, Kochva E, Boulain JC, Menez A (1993) Cloning and sequence analysis of cDNAs encoding precursors of sarafotoxins. Evidence for an unusual rosary-type organization. J Biol Chem 268:3052–3055

    PubMed  CAS  Google Scholar 

  • Eglezos A, Cucchi P, Patacchini R, Quartara L, Maggi CA, Mizrahi J (1993) Differential effects of BQ-123 against endothelin-1 and endothelin-3 on the rat vas deferens: evidence for an atypical endothelin receptor. Br J Pharmacol 109:736–738

    Article  PubMed  CAS  Google Scholar 

  • Elferink JGR, de Koster BM (1996) Modulation of human neutrophil chemotaxis by the endothelin-B receptor agonist sarafotoxin S6c.Chemico-Biol Int 101:165–174

    Article  CAS  Google Scholar 

  • Faro R, Grassikassisse DM, Donato JL, Boin I, Opgenorth TJ, Withrington PG, Zatz R, Antunes E, Denucci G (1995) Role of endothelin ET(A) and ET(B) receptors in the arterial vasculature of the isolated canine liver. J Cardiovasc Pharmacol 26:S204–S207

    PubMed  CAS  Google Scholar 

  • Galron R, Bdolah A, Kochva E, Wollberg Z, Kloog Y, Sokolovsky M (1991) Kinetic and cross-linking studies indicate different receptors for endothelins and sarafotoxins in the ileum and cerebellum. FEBS Lett 283:11–14

    Article  PubMed  CAS  Google Scholar 

  • Gardiner SM, Compton AM, Kemp PA, Bennett T (1990) Cardiac output effects of endothelin-1, -2 and -3 and sarafotoxin S6b in conscious rats. J Auton Nerv Syst 30:143–147

    Article  PubMed  CAS  Google Scholar 

  • Gater PR, Wasserman MA, Renzetti LM (1996) Effects of Ro 47–0203 on endothelin1 and sarafotoxin S6c-induced contractions of human bronchus and guinea-pig trachea. Eur J Pharmacol 304:123–128

    Article  PubMed  CAS  Google Scholar 

  • Gellai M, De Wolf R, Pullen M, Nambi P (1994) Distribution and functional role of renal ET receptor subtypes in normotensive and hypertensive rata. Kidney Int 46:1287–1294

    Article  PubMed  CAS  Google Scholar 

  • Gellai M, Fletcher T, Pullen M, Nambi P (1996) Evidence for the existence of endothelin-B receptor subtypes and their physiological roles in the rat. Am J Physiol 271:R254–R261

    PubMed  CAS  Google Scholar 

  • Gulati A, Rebello S (1992) Characteristics of endothelin receptors in the central nervous system of spontaneously hypertensive rats. Neuropharmacology 31: 243–250

    Article  PubMed  CAS  Google Scholar 

  • Han SP, Knuepfer MM, Trapani AJ, Fok KF, Westfall TC (1990) Cardiac and vascular actions of sarafotoxin S6b and endothelin-1. Life Sci 46:767–775

    Article  PubMed  CAS  Google Scholar 

  • Harrison VJ, Randriantsoa A, Schoeffter P (1992) Heterogeneity of endothelinsarafotoxin receptors mediating contraction of pig coronary artery. Br J Pharmac 105:511–513

    Article  CAS  Google Scholar 

  • Hay DWP (1992) Pharmacological evidence for distinct endothelin receptors in guinea-pig bronchus and aorta. Br J Pharmacol 106:759–761

    Article  PubMed  CAS  Google Scholar 

  • Hay DWP, Luttmann MA (1997) Nonpeptide endothelin receptor antagonists. IX. Characterization of endothelin receptors in guinea-pig bronchus with SB 209670 and other endothelin receptor antagonists. J Pharmacol Exp Ther 280:959–965

    PubMed  CAS  Google Scholar 

  • Hay DWP, Luttmann MA, Beck G, Ohlstein EH (1996) Comparison of endothelinB (ETB) receptors in rabbit isolated pulmonary artery and bronchus. Br J Pharmacol 118:1209–1217

    Article  PubMed  CAS  Google Scholar 

  • Inoue A, Yanagisawa M, Kimura S, Kasuya Y, Miyauchi T, Goto K, Masaki T (1989) The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc Natl Acad Sci USA. 86: 2863–2867

    Article  PubMed  CAS  Google Scholar 

  • Ishikawa H, Haruno I, Harada Y, Yoshitomi T, Ishikawa S, Katori M (1996) Pharmacological characterization of endothelin receptors in the rabbit iris sphincter muscle: suggestion for the presence of atypical receptors. Curr Eye Res 15:73–78

    Article  PubMed  CAS  Google Scholar 

  • Iwasaki T, Notoya M, Hayasaki-Kajiwara Y, Shimamura T, Naya N, Ninomiya M, Nakajima M (1999) Endothelium-independent vascular relaxation mediating ETB receptor in rabbit mesenteric arteries. Am J Physiol 276:H383–390

    PubMed  CAS  Google Scholar 

  • Johns CR, Hiley CR (1990) Heterogeneity of [125I]sarafotoxin S6b binding in rat tissues. Eur J Pharmacol 183:1746

    Article  Google Scholar 

  • Kitazumi K, Shiba T, Nishiki K, Furukawa Y, Takasaki C, Tasaka K. (1990) Structure-activity relationship in vasoconstrictor effects of sarafotoxins and endothelin-1. FEBS Lett 260:269–272

    Article  PubMed  CAS  Google Scholar 

  • Kloog Y, Ambar I, Sokolovsky M, Kochva E, Bdolah A, Wollberg Z (1988) Sarafotoxin, a novel vasoconstrictor peptide: phosphoinositide hydrolysis in rat heart and brain. Science 242:268–270

    Article  PubMed  CAS  Google Scholar 

  • Kochva E, Bdolah A, Wollberg Z. (1993) Sarafotoxins and endothelins: evolution, structure and function. Toxicon 31:541–568

    Article  PubMed  CAS  Google Scholar 

  • Koshi T, Suzuki C, Arai K, Mizoguchi T, Torii T, Hirata M, Ohkuchi M, Okabe T (1991) Syntheses and biological activities of endothelin-1 analogs. Chem Pharm Bull 39:3061–3063

    Article  PubMed  CAS  Google Scholar 

  • Kumar A, Shahani BT, Gulati A (1996) Modification of systemic and regional circulatory effects of intracerebroventricular administration of endothelin-1 (ET-1) by propranolol in anesthetized rats. Gen Pharmacol 27:1025–1033

    Article  PubMed  CAS  Google Scholar 

  • Kumar A, Morrison S, Gulati A (1997) Effect of ETA receptor antagonists on cardiovascular responses induced by centrally administered sarafotoxin 6b: role of sympathetic nervous system. Peptides 18:855–864.

    Article  PubMed  CAS  Google Scholar 

  • Lamthanh H, Bdolah A, Creminon C, Grassi J, Menez A, Wollberg Z, Kochva E (1994) Biological activities of [Thr2]sarafotoxin-b, a synthetic analogue of sarafotoxin-b. Toxicon 32:1105–1114

    Article  PubMed  CAS  Google Scholar 

  • Landan G, Bdolah A, Wollberg Z, Kochva E, Graur D (1991a) Evolution of the sarafotoxin/endothelin superfamily of proteins. Toxicon 29:237–244

    Article  PubMed  CAS  Google Scholar 

  • Landan G, Bdolah A, Wollberg Z, Kochva E, Graur D (1991b) The evolutionary history of the sarafotoxin/endothelin/endothelin-like superfamily J Cardiovasc Pharmacol 17:S517–S519

    Article  PubMed  CAS  Google Scholar 

  • Laursen M, Bodelsson G, Stjernquist M (1998) Atypical receptors mediate the response to endothelin-1 and sarafotoxin S6b in the human umbilical artery. Eur J Pharmacol 362:167–172

    Article  PubMed  CAS  Google Scholar 

  • Lecoin L, Sakurai T, Ngo M-T, Abe Y, Yanagisawa M, Le Douarin NM (1998) Cloning and characterization of a novel endothelin receptor subtype in the avian class. Proc Natl Acad Sci USA 95:3024–3029

    Article  PubMed  CAS  Google Scholar 

  • Leis HJ, Zach D, Huber E, Windischhofer W (1998) Prostaglandin endoperoxide synthase-2 contributes to the endothelin/sarafotoxin-induced prostaglandin E2 synthesis in mouse osteoblastic cells (MC3T3-E1): evidence for a protein tyrosine kinase-signaling pathway and involvement of protein kinase C. Endocrinology 139:1268–1277

    Article  PubMed  CAS  Google Scholar 

  • Lin WW, Chen YM, Lee SY, Nishio H, Kimura T, Sakakibara S, Lee CY (1990) Cardiovascular effects of two disulfide analogues of sarafotoxin S6b. Toxicon 28:911–923

    Article  PubMed  CAS  Google Scholar 

  • Luciano LG, D’Orleans-Juste P, Calixto JB, Rae GA (1998) Endothelin-1 selectively potentiates the purinergic component of sympathetic neurotransmission in rat seminal vesicle. J Cardiovasc Pharmacol 31:S515–S517

    Article  PubMed  CAS  Google Scholar 

  • MacLean MR, Mackenzie JF, Docherty CC (1998) Heterogeneity of endothelin-B receptors in rabbit pulmonary resistance arteries. J Cardiovasc Pharmacol 31:S115–S118

    Article  PubMed  Google Scholar 

  • Maguire JJ, Kuc RE, Rous BA, Davenport AP (1996) Failure of BQ123, a more potent antagonist of sarafotoxin 6b than of endothelin-1, to distinguish between these agonists in binding experiments. Br J Pharmacol 118:335–342

    Article  PubMed  CAS  Google Scholar 

  • Matsuda H, Kawaguchi A, Uematsu M, Ohmori F, Nagata S, Miyatake K (1996) Endothelins contract guinea-pig pulmonary artery and enhance its adrenergic response via ETA receptors. Clin Exp Pharmacol Physiol 23:379–385

    Article  PubMed  CAS  Google Scholar 

  • McCulloch KM, Docherty C, MacLean MR (1998) Endothelin receptors mediating contraction of rat and human pulmonary resistance arteries: effect of chronic hypoxia in the rat. Br J Pharmacol 123:1621–1630

    Article  PubMed  CAS  Google Scholar 

  • Miasiro N, Karaki H, Paiva (1998) Distinct endothelin-B receptors mediate the effects of sarafotoxin S6c and IRL1620 in the ileum. J Cardiovasc Pharmacol 31:S175–S178

    Article  PubMed  CAS  Google Scholar 

  • Miller V, Michener SR (1995) Modulation of contractions to and receptors for endothelins in canine veins. Am J Physiol 268:H345–H350

    PubMed  CAS  Google Scholar 

  • Mills, RG, Ralston, GB, King GF (1994) The solution structure of sarafotoxin-c. J Biol Chem 269:23413–23419

    PubMed  CAS  Google Scholar 

  • Mondon F, Maka F, Sabry S, Ferre F (1995) Endothelin-induced phosphoinositide hydrolysis in the muscular layer of stem villi vessels of human term placenta. Eur J Endocrinol 133:606–612

    Article  PubMed  CAS  Google Scholar 

  • Moreland S, McMullen D, Abboa-Offei B, Seymour A (1994) Evidence for a differential location of vasoconstrictor endothelin receptors in the vasculature. Br J Pharmacol 112:704–708

    Article  PubMed  CAS  Google Scholar 

  • Mutafova-Yambolieva VN, Westfall DP (1998) Inhibitory and facilitatory presynaptic effects of endothelin on sympathetic cotransmission in the rat isolated tail artery. Br J Pharmacol 123:136–142

    Article  PubMed  CAS  Google Scholar 

  • Nambi P, Wu H-L, Pullen M, Aiyar N, Bryan D, Elliott J (1992) Identification of endothelin receptor subtypes in rat kidney cortex using subtype-selective ligands. Mol Pharmacol 42:336–339

    PubMed  CAS  Google Scholar 

  • Nambi P, Pullen M, Kumar C (1994) Identification of a novel endothelin receptor in Xenopus laevis liver. Neuropeptides 26:181–185

    Article  PubMed  CAS  Google Scholar 

  • Nambi P, Pullen M, Brooks DP, Gellai M (1995) Identification of ETB receptor subtypes using linear and truncated analogs of ET. Neuropeptides 29:331–336

    Article  PubMed  CAS  Google Scholar 

  • Nishiyama M, Takahara Y, Masaki T, Nakajima N, Kimura S (1995) Pharmacological heterogeneity of both endothelin ETA- and ETB-receptors in the human saphenous vein. Jpn J Pharmacol 69:391–398

    Article  PubMed  CAS  Google Scholar 

  • Nosaka C, Ishikawa H, Haruno I, Yoshitomi T, Kase H, Ishikawa S, Harada Y (1998) Radioligand binding characteristics of the endothelin receptor in the rabbit iris. Jpn J Pharmacol 76:289–296

    Article  PubMed  CAS  Google Scholar 

  • Opgenorth TH, Wu-Wong JR, Shiosaki K (1992) Endothelin-converting enzymes. FASEB J 6:2653–2659

    PubMed  CAS  Google Scholar 

  • Panek RL, Major TC, Hingorani GP, Doherty AMA, Taylor DG (1992) Endothelin and structurally related analogs distinguish between endothelin receptor subtypes. Biochem Biophys Res Commun 183:566–571

    Article  PubMed  CAS  Google Scholar 

  • Pate MA, Chester AH, Brown TJ, Roach AG, Yacoub MH (1998) Atypical antagonism observed with BQ-123 in human saphenous vein. J Cardiovasc Pharmacol 31:S172–S174

    Article  PubMed  CAS  Google Scholar 

  • Poulat P, De Champlain J, D’Orleans-Juste P, Couture R (1996) Receptor and mechanism that mediate endothelin- and big endothelin-1-induced phosphoinositide hydrolysis in the rat spinal cord. Eur J Pharmacol 315:327–334

    Article  PubMed  CAS  Google Scholar 

  • Rasmussen TE, Jougasaki M, Supaporn T, Hallett JW Jr, Brooks DP, Burnett JC Jr (1998) Cardiovascular actions of ET-B activation in vivo and modulation by receptor antagonism. Am J Physiol 274:R131-R138

    PubMed  CAS  Google Scholar 

  • Rebello S, Roy S, Saxena PR, Gulati A (1995) Systemic hemodynamic and regional circulatory effects of centrally administered endothelin-1 are mediated though ETA receptors. Brain Res 676:141–150

    Article  PubMed  CAS  Google Scholar 

  • Rose PM, Krystek SR Jr, Patel PS, Liu ECK, Lynch JS, Lach DA, Fisher SM, Webb ML (1995) Aspartate mutation distinguishes ETA but not ETB receptor subtype-selective ligand binding while abolishing phospholipase C activation in both receptors. FEBS Lett 361:243–249

    Article  PubMed  CAS  Google Scholar 

  • Russell FD, Davenport AP (1996) Characterization of the binding of endothelin ETB selective ligands in human and rat heart. Br J Pharmacol 119:631–636

    Article  PubMed  CAS  Google Scholar 

  • Servitja JM, Masgrau R, Sarri E, Picatoste F (1998) Involvement of ET(A) and ET(B) receptors in the activation of phospholipase D by endothelins in cultured rat cortical astrocytes. Br J Pharmacol 124:1728–1734

    Article  PubMed  CAS  Google Scholar 

  • Shannon TR, Hale CC (1994) Identification of a 65 kDa endothelin receptor in bovine cardiac sarcolemmal vesicles. Eur J Pharmacol 267:233–238

    Article  PubMed  CAS  Google Scholar 

  • Shraga-Levine Z, Galron R, Sokolovsky M (1994) Cyclic GMP formation in rat cerebellar slices is stimulated by endothelins via nitric oxide formation and by sarafotoxins via formation of carbon monoxide. Biochemistry 33:14656–14659

    Article  PubMed  CAS  Google Scholar 

  • Shraga-Levine Z, Sokolovsky M (1996) cGMP formation in rat atrial slices is ligand and endothelin receptor subtype specific. Circ Res 78:424–430

    Article  PubMed  CAS  Google Scholar 

  • Shraga-Levine Z, Sokolovsky M (2000) Functional Coupling of G Proteins to Endothelin Receptors Is Ligand and Receptor Subtype Specific. Cellular and Molecular Neurobiology 20:305–317

    Article  PubMed  CAS  Google Scholar 

  • Sokolovsky M (1995) Endothelin receptor subtypes and their role in transmembrane signaling mechanisms. Pharmacol Ther 68:435–471

    Article  PubMed  CAS  Google Scholar 

  • Sokolovsky M, Galron R, Kloog Y, Bdolah A, Indig FE, Blumberg S, Fleminger G (1990) Endothelins are more sensitive than sarafotoxins to neutral endopeptidase: possible physiological significance. Proc Natl Acad Sci USA 87:4702–4706

    Article  CAS  Google Scholar 

  • Sokolovsky M, Shraga-Levine Z, Galron R (1994) Ligand-specific stimulation/inhibition of cAMP formation by a novel endothelin receptor subtype. Biochemistry 33:11417–11419

    Article  PubMed  CAS  Google Scholar 

  • Sudhir K, Ko E, Zellner C, Wong HE, Hutchison SJ, Chou TM, Chatterjee K (1997) Physiological concentrations of estradiol attenuate endothelin 1- induced coronary vasoconstriction in vivo. Circulation 96:3626–3632

    Article  PubMed  CAS  Google Scholar 

  • Sudjarwo SA, Hori M, Tanaka M, Matsuda T, Okada T, Karaki H (1994) Subtypes of endothelin ETA and ETB receptors mediating venous smooth muscle contraction. Biochem Biophys Res Commun 200:627–633

    Article  PubMed  CAS  Google Scholar 

  • Takasaki C, Aimoto S, Kitazumi K, Tasaka K, Shiba T, Nishiki K, Furukawa Y, Takayanagi R, Ohnaka K, Nawata H (1991) Structure-activity relationships of sarafotoxins: chemical syntheses of chimera peptides of sarafotoxins S6b and S6c. Eur J Pharmacol 198:165–169

    Article  PubMed  CAS  Google Scholar 

  • Tamaoki H, Kyogoku Y, Nakajima K, Sakakibara S, Hayashi M, Kobayashi Y (1992) Conformational study of endothelins and sarafotoxins with the cystine-stabilized helical motif by means of CD spectra. Biopolymers 32:353–357

    Article  PubMed  CAS  Google Scholar 

  • Tanaka T, Ogawa T, Matsuda Y. (1995) Species differences in the binding characteristics of RES-701–1: a potent endothelin ETB receptor-selective antagonist. Biochem Biophys Res Commun 209:712–716

    Article  PubMed  CAS  Google Scholar 

  • Uchida K, Yuzuki R, Kamikawa Y (1998) The role of receptor-operated Ca2+ influx in endothelin-induced contraction of the muscularis mucosae. J Cardiovasc Pharmacol 31:S504–S506

    Article  PubMed  CAS  Google Scholar 

  • Warner TD, Allcock GK, Corder R, Vane JR (1993a) Use of the endothelin antagonists BQ-123 and PD 142893 to reveal three endothelin receptors mediating smooth muscle contraction and the release of EDRF. Br J Pharmacol 110:777–782

    Article  PubMed  CAS  Google Scholar 

  • Warner TD, Allcock GK, Mickley EJ, Corder R, Vane JR (1993b) Comparative studies with the endothelin receptor antagonists BQ-123 and PD 142893 indicate at least three endothelin receptors J Cardiovasc Pharmacol 22:S117–S120

    Article  PubMed  CAS  Google Scholar 

  • White DG, Garrat H, Mundin JW, Sumner MJ, Vallance PJ, Watts IS (1994) Human saphenous vein contains both endothelin ETA and ETB contractile receptors. Eur J Pharmacol 257:307–310

    Article  PubMed  CAS  Google Scholar 

  • Williams DL, Jones KL, Pettibone DJ, Lis EV, Clinschmidt BV (1991) Sarafotoxin S6c: an agonist which distinguishes between endothelin receptor subtypes. Biochem Biophys Res Commun 175:556–661

    Article  PubMed  CAS  Google Scholar 

  • Yoneyama T, Hori M, Tanaka T, Matsuda Y, Karaki H (1995) Endothelin ETA and ETB receptors facilitating parasympathetic neurotransmission in the rabbit trachea. J Pharmacol Exp Therap 275:1084–1089

    CAS  Google Scholar 

  • Zuccarello M, Boccaletti R, Rapoport RM (1998a) Endothelin ETB receptor-mediated constriction in the rabbit basilar artery. Eur J Pharmacol 350:R7-R9

    Article  PubMed  CAS  Google Scholar 

  • Zuccarello M, Boccaletti R, Rapoport RM (1998b) Endothelin ETB receptormediated relaxation of rabbit basilar artery. Eur J Pharmacol 357:67–71

    Article  PubMed  CAS  Google Scholar 

Download references

Authors
  1. M. Sokolovsky
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Z. Shraga-Levine
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. Department of Cardiac, Vascular and Inflammation Research, The William Harvey Research Institute St. Barthomew’s and the Royal London School of Medicine and Dentistry, Charterhouse Square, London, EC1M 6BQ, UK

    Timothy D. Warner Ph.D

Rights and permissions

Reprints and permissions

Copyright information

© 2001 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Sokolovsky, M., Shraga-Levine, Z. (2001). Sarafotoxins and Their Relationship to the Endothelin Family of Peptides. In: Warner, T.D. (eds) Endothelin and Its Inhibitors. Handbook of Experimental Pharmacology, vol 152. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-56899-2_2

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-56899-2_2

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-63237-2

  • Online ISBN: 978-3-642-56899-2

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation