Abstract
Antihistamines that powerfully and selectively inhibit certain effects of histamine have been known for over 25 years. The effects of histamine that they inhibit are contractile actions on the smooth muscle of the gut, uterus and bronchioles and capillary permeability responses. Some other effects of histamine are highly resistant to these antihistamines and they include stimulation of gastric secretion, relaxation of rat uterus and positive inotropic effects on isolated atria (Loew, 1947; Ashford et al., 1949; Dutta, 1949; Trendelenberg, 1960). Indeed, it has been demonstrated that gastric secretion induced by histamine is enhanced rather than diminished by antihistamines, including mepyramine (Wood, 1948) and triprolidine (Green, 1953), perhaps in consequence of histamine release (Chap. 34, Sect. CIL). Compounds that selectively inhibit histamine-induced gastric secretion and other effects of histamine resistant to the earlier antihistamines were first reported only in 1972 by Black and colleagues. They are referred to as antagonists at H2 receptors, in distinction from the earlier antihistamines whose inhibitory effects at low concentrations characterised a histamine receptor for which Ash and Schild in 1966 had suggested the symbol H1. The distinction between H1 and H2 receptors is already well characterised by studies both of selective agonists (Ash and Schild, 1966; Black et al., 1972) and antagonists (Black et al., 1972, 1973, 1975).
This is a preview of subscription content, log in via an institution.
Buying options
Tax calculation will be finalised at checkout
Purchases are for personal use only
Learn about institutional subscriptionsPreview
Unable to display preview. Download preview PDF.
References
Adamson, D.W., Barrett, P.A., Billinghurst, J.W., Green, A.F., Jones, T.S.G.: Geometrical isomers in a series of antihistamines. Nature (Lond.) 168, 204–205 (1951)
Aitken, M.M., Sanford, J.: Modification of acute systemic anaphylaxis in cattle by drugs and by vagotomy. J. comp. Path. 82, 247–256 (1972 a)
Aitken, M.M., Sanford, J.: Effects of histamine, 5-hydroxytryptamine and bradykinin on cattle and their modification by antagonists and by vagotomy. J. comp. Path. 82, 257–266 (1972 b)
Alberty, J., Takkunen, R.: Der Anteil von Histamin an der anaphylaktischen und der durch einen chemischen Histaminfreisetzer hervorgerufenen vasculären Hautreaktion. Int. Arch. Allergy 10, 285–304(1957)
Ankier, S.L, Neat, M.L.: Some studies on acute inflammation induced by dextran in the mouse. Int. Arch. Allergy 42, 264–277 (1972)
Ankier, S.L, West, G.B.: Inhibition of the anaphylactoid reaction in rats. Brit. J. Pharmacol. 33, 304–311(1968)
Armitage, P., Herxheimer, H., Rosa, L.: Protective action of antihistamines in the anaphylactic microshock of the guinea pig. Brit. J. Pharmacol. 7, 625–632 (1952)
Ash, A.S.F., Schild, H.O.: Receptors mediating some actions of histamine. Brit. J. Pharmacol. 27, 427–439 (1966)
Ashford, C.A., Heller, H., Smart, G.A.: The action of histamine on hydrochloric acid and pepsin secretion in man. Brit. J. Pharmacol. 4, 153–161 (1949)
Augstein, J., Farmer, J.B., Lee, T.B., Sheard, P., Tattersall, M. L.: Selective inhibitor of slow-reacting substance of anaphylaxis. Nature (New Biol.) 245, 215–217 (1973)
Austen, K.F., Humphrey, J.H.: In vitro studies of the mechanism of anaphylaxis. In: Dixon, F. J., Humphrey, J.H. (Eds.): Advances in Immunology, Vol. 3, pp. 1–96. New York-London: Academic Press 1963
Aviado, D.M., Sadavongvivad, C.: Pharmacological significance of biogenic amines in the lungs: histamine. Brit. J. Pharmacol. 38, 366–373 (1970)
Bain, W.A.: Discussion on antihistamine drugs. Proc. roy. Soc. Med. 42, 615–625 (1949)
Bain, W.A.: The evaluation of drugs in man, with special reference to antihistamines. Analyst. 76, 573–579(1951)
Baumgarten, A., Wilhelm, D.L.: Vascular permeability responses in hypersensitivity: I. The tuberculin reaction. Pathology 1, 301–315 (1969)
Beach, V.L., Steinetz, B.G.: Quantative measurement of Evans blue space in tissue of the rat; influence of 5-hydroxytryptamine antagonists and phenelzine on experimental inflammation. J. Pharmacol, exp. Ther. 131, 400–406 (1961)
Becker, E.L., Mota, L, Wong, D.: Inhibition by antihistamines of the vascular permeability increase induced by bradykinin. Brit. J. Pharmacol. 34, 330–336 (1968)
Bein, H.J.: The pharmacology of rauwolfia. Pharmacol. Rev. 8, 435–483 (1956)
Beretta, C., Ferrini, R., Glässer, A.H.: 1-Methyl-8-β-carbobenzyloxy-aminomethyl 10 α-ergoline, a potent and long-lasting 5-hydroxytryptamine antagonist. Nature (Lond.) 207, 421–422 (1965)
Bernauer, W., Hahn, F., Giertz, H.: Comparison of the antilethal, broncholytic and antiemphyse-matous activities of mepyramine in anaphylactic, histamine, and anaphylatoxin shock of guinea pigs. Arch. int. Pharmacodyn. 178, 137–151 (1969)
Berry, P.A., Collier, H.O.J.: Bronchoconstrictor action and antagonism of a slow reacting substance from anaphylaxis of guinea pig isolated lung. Brit. J. Pharmacol. 23, 201–216 (1964)
Bhattacharya, B.K., Lewis, G.P.: The effects of reserpine and compound 48/80 on the release of amines from the mast cells of rats. Brit. J. Pharmacol. 11, 411–416 (1956)
Black, J.W., Duncan, W.A.M., Durant, G.J., Ganellin, C.R., Parsons, E.M.: Definition and antagonism of histamine H2-receptors. Nature (Lond.) 236, 385–390 (1972)
Black, J.W., Duncan, W.A.M., Emmett, J.C., Ganellin, C.R., Hesselbo, T, Parsons, M.E., Wyllie, J.H.: Metiamide-an orally active histamine H2 receptor antagonist. Agents Actions 3, 133–137 (1973)
Black, J.W., Owen, D.A.A., Parsons, M.E.: An analysis of the depressor responses to histamine in the cat and dog: involvement of both H1 and H2-receptors. Brit. J. Pharmacol. 54, 319–324 (1975)
Brimblecombe, R.W., Duncan, W.A.M., Durant, G.J., Emmett, J.C., Ganellin, C.R., Parsons, M.E.: Cimetidine. Nonthiourea histamine H2-receptor antagonist. J. int. med. Res. 3, 86–92 (1975)
Brittain, R.T., D’Arcy, P.F., Hunt, J.H.: Resolution of chlorpheniramine and the pharmacological properties of its isomers. Nature (Lond.) 183, 734–735 (1959)
Brocklehurst, W.E.: Occurrence of an unidentified substance during anaphylactic shock in cavy lung. J. Physiol. (Lond.) 120, 16 P (1953)
Brocklehurst, W.E.: The release of histamine and formation of a slow-reacting substance (SRS-A) during anaphylactic shock. J. Physiol. (Lond.) 151, 416–435 (1960)
Brocklehurst, W.E.: Pharmacologically active substances in hypersensitivity reactions. In: Cruickshank, R., Weir, D.M. (Eds.): Modern Trends in Immunology, Vol. 2, pp. 235–249. London: Butterworth 1967
Brocklehurst, W.E., Humphrey, J H., Perry, W.L.M.: The role of histamine in cutaneous antigen-antibody reactions in the rat. J. Physiol. (Lond.) 129, 205–225 (1955)
Brocklehurst, W.E., Humphrey, J.H., Perry, W.L.M.: Cutaneous antigen-antibody reactions in the rat. J. Physiol. (Lond.) 150, 489–500 (1960)
Brown, P.C., Consden, R., Glynn, L.E.: Observations on the shrink temperature of collagen and its variations with age and disease. Ann. rheum. Dis. 17, 196–208 (1958)
Bushby, S.R.M., Green, A.F.: The release of histamine by polymyxin B and polymyxin E. Brit. J. Pharmacol. 10, 215–219 (1955)
Cameron, J.: Anaphylactic shock in mice. Brit. J. exp. Path. 37, 470–476 (1956)
Carr, J.: The effect of anti-inflammatory drugs on increased vascular permeability induced by chemical mediators. J. Path. 108, 1–14 (1972).
Casey, F.B., Tokuda, S.: A comparative study of the mechanisms of passive cutaneous anaphylaxis induced by mouse IgG, rabbit IgG, and rabbit F (ab′)2 antibodies. Int. Arch. Allergy 44, 737–744(1973)
Casy, A.F., Ison, R.R.: Stereochemical influences upon antihistaminic activity. Further studies of isomeric 4-amino-1, 2-diarylbutenes. J. Pharm. (Lond.) 22, 270–278 (1970)
Church, M. K.: Response of rat lung to humoral mediators of anaphylaxis and its modification by drugs and sensitization. Brit. J. Pharmacol. 55, 423–430 (1975)
Church, M.K., Collier, H.O.J., James, G.W.L.: The inhibition by dexamethasone and disodium cromoglycate of anaphylactic bronchoconstriction in the rat. Brit. J. Pharmacol. 46, 56–65 (1972)
Church, M.K., Miller, P.: Simple models of anaphylaxis and of histamine and 5-hydroxytryptamine induced inflammation using the mouse pinna. Brit. J. Pharmacol. 55, 315P (1975)
Collier, H.O.J.: Role of kallikrein-kinin system in lung diseases. In: Proc. No. 27 of the Fogerty International Center. Washington, D.C.: U.S. Government Printing Office 1976. In press
Collier, H.O.J., Holgate, J.A., Schachter, M., Shorley, P.G.: The bronchoconstrictor action of bradykinin in the guinea pig. Brit. J. Pharmacol. 15, 290–297 (1960)
Collier, H.O.J., James, G.W.L.: Humoral factors affecting pulmonary inflation during acute anaphylaxis in the guinea pig in vivo. Brit. J. Pharmacol. 30, 283–301 (1967)
Collier, H.O.J., James, G.W.L., Piper, P.J.: Antagonism of fenamates and like-acting drugs of bronchoconstriction induced by bradykinin or antigen in the guinea pig. Brit. J. Pharmacol. 34, 76–87 (1968)
Collier, H.O.J., Shorley, P.G.: Analgesic antipyretic drugs as antagonists of bradykinin. Brit. J. Pharmacol. 15, 601–610 (1960)
Collier, H.O.J., Shorley, P.G.: Antagonism by mefenamic and flufenamic acids of the broncho-constrictor action of kinins in the guinea pig. Brit. J. Pharmacol. 20, 345–351 (1963)
Collier, H.O. J., Sweatman, W.J.F.: Antagonism by fenamates of prostaglandin F2α and of slow reacting substance on human bronchiole muscle. Nature (Lond.) 219, 864–865 (1968)
Copp, F.C., Green, A.F., Hodson, H.F., Randall, A.W., Sim, M.F.: New peripheral antagonists of 5-hydroxytryptamine. Nature (Lond.) 214, 200–201 (1967)
Craig, J.P., Wilhelm, D.L.: Cutaneous anaphylaxis in the guinea pig and its relative insusceptibility to an antihistamine. J. Immunol. 90, 43–51 (1963)
Craps, L., Inderbitzin, Th.: Anaphylactoid and anaphylactic cutaneous exoserosis in the rat. Int. Arch. Allergy 18, 268–285 (1961)
Day, M., Vane, J.R.: An analysis of the direct and indirect actions of drugs on the isolated guinea pig ileum. Brit. J. Pharmacol. 20, 150–170 (1963)
Di Rosa, M., Giroud J.P., Willoughby, D.A.: Studies of the mediators of the acute inflammatory response induced in rats in different sites by carrageenan and turpentine. J. Path. 104, 15–29 (1971)
Di Rosa, M, Willoughby, D.A.: Screens for antiinflammatory drugs. J. Pharm. (Lond.) 23, 297–298(1971)
Doepfner, W., Cerletti, A.: Comparison of lysergic acid derivatives and antihistamines as inhibitors of the oedema provoked in the rat’s paw by serotonin. Int. Arch. Allergy 12, 89–97 (1958)
Doherty, N.S., Robinson, B.V.: The inflammatory response to carrageenan. J. Pharm. (Lond.) 27, 701–703 (1975)
Durant, G.J., Ganellin, C.R., Parsons, M.E.: Chemical differentiation of histamine H1 and H2-receptor agonists. J. med. Chem. 18, 905–909 (1975)
Dutta, N.K.: Some pharmacological properties common to antihistamine compounds. Brit. J. Pharmacol. 4, 281–289 (1949)
Eakins, K.E.S., Karim, S.M.M., Miller, J.D.: Antagonism of some smooth muscle actions of prostaglandins by polyphloretin phosphate. Brit. J. Pharmacol. 39, 556–563 (1970)
Eakins, K.E., SannerJ.H.: Prostaglandin antagonists. In: Karim, S.M.M. (Ed.): The Prostaglandins. Progress in Research, pp. 263–292. Oxford: Medical & Technical Publishing Co. Ltd. 1972
El-Ackad, T.M., Meyer, M. J., Sturkie, P.D.: Inotropic and chronotropic actions of histamine on the avian heart. Fed. Proc. 33, Abst. 2110 (1974)
Ensor, C.R., Russell, D., Chen, G.: A comparative study on some aspects of the pharmacology of diphenhydramine (Benadryl) and chemically related compounds. J. Pharmacol, exp. Ther. 112, 318–325(1954)
Erspamer, V. (Ed.): 5-Hydroxytryptamine and Related Indolealkylamines. Handbook of Experimental Pharmacology, Vol. XIX. Berlin-Heidelberg-New York: Springer 1966
Eyre, P.: Histamine release from calf lung in vitro by specific antigen and by compound 48/80. Arch. int. Pharmacodyn. 192, 347–352 (1971a)
Eyre, P.: Pharmacology of bovine pulmonary vein anaphylaxis in vitro. Brit. J. Pharmacol. 43, 302–311 (1971b)
Eyre, P., Lewis, A.J., Wells, P.W.: Acute systemic anaphylaxis in the calf. Brit. J. Pharmacol. 47, 504–516 (1973)
Eyre, P., Wells, P.W.: Histamine H2-receptors modulate systemic anaphylaxis: a dual cardiovascular action of histamine in calves. Brit. J. Pharmacol. 49, 364–367 (1973)
Fanchamps, A., Doepfner, W., Weidmann, H., Cerletti, A.: Pharmakologische Charakterisierung von Deseril, einem Serotonin-Antagonisten. Schweiz, med. Wschr. 90, 1040–1046 (1960)
Farmer, J.B., Richards, I.M., Sheard, P., Woods, A.M.: Mediators of passive lung anaphylaxis in the rat. Brit. J. Pharmacol. 55, 57–64 (1975)
Fastier, F. N.: Structure activity relationships of amidine derivatives. Pharmacol. Rev. 14, 37–90 (1962)
Feinberg, S.M., Malkiel, S., Feinberg, A.R.: The Antihistamines. Their Clinical Application. Chicago-Illinois: Yearbook Publications Inc. 1950
Feldberg, W., Miles, A.A.: Regional variations of increased permeability of skin capillaries induced by histamine liberator and their relation to the histamine content of the skin. J. Physiol. (Lond.) 120, 205–213 (1953)
Feldberg, W., Smith, A.N.: Release of histamine by tryptamine and 5-hydroxytryptamine. Brit. J. Pharmacol. 8, 406–411 (1953)
Ferreira, S.H., Moncada, S., Vane, J. R.: Indomethacin and aspirin abolish prostaglandin release from the spleen. Nature (New Biol.) 231, 237–239 (1971)
Fink, M.A., Rothlauf, M.V.: In vitro anaphylaxis in the sensitised mouse uterus. Proc. Soc. exp. Biol. (N.Y.) 90, 477–480 (1955)
Flower, R., Grygleski, R., Herbaczynska-Cedro, K., Vane, J.R.: Effects of anti-inflammatory drugs on prostaglandin biosynthesis. Nature (New Biol.) 238, 104–106 (1972)
Flower, R. J., Harvey, E. A., Moncada, S., Nijkamp, F., Vane, J. R.: Some properties of rabbit aorta contracting substance-releasing factor (RCS-RF). Brit. J. Pharmacol. 461P–462P (1976)
Flynn, S.B., Owen, D.A.A.: Histamine receptors in peripheral vascular beds in the cat. Brit. J. Pharmacol. 55, 181–188 (1975)
Fourneau, E., Bovet, D.: The “sympatholytic” action of a new derivative of dioxane. Arch. int. Pharmacodyn. 46, 178–191 (1933)
Fowle, A.S.E., Hughes, D.T.D., Knight, G.J.: The evaluation of histamine antagonists in man. Europ. J. clin. Pharmacol. 3, 215–220 (1971)
Gaddum J.M., Picarelli, Z.P.: Two kinds of tryptamine receptor. Brit. J. Pharmacol. 12, 323–328 (1957)
Ganellin, C.R., Port, G.N. J., Richards, W.G.: Conformation of histamine derivatives. II. Molecular orbital calculations of preferred conformations in relation to dual receptor activity. J. med. Chem. 16, 616–620 (1973)
Ganley, O.H.: Protective effect of cyproheptadine, a new antihistamine antiserotonin compound on lethal burns in the mouse. Arch. int. Pharmacodyn. 138, 125–132 (1962)
Garattini, S., Valzelli, L.: Serotonin. Amsterdam: Elsevier 1965
Garcia-Arocha, H.: Liberation of 5-hydroxytryptamine and histamine in the anaphylactic reaction of the rat. Canad. J. Biochem. 39, 403–416 (1961)
Gelfand, M.D., West, G.B.: Experimental studies with the butanolamide and propanolamide of 1-methyl-lysergic acid. Int. Arch. Allergy. 18, 286–291 (1961)
Goose, J., Blair, A.M.J.N.: Passive cutaneous anaphylaxis in the rat, induced with two homolo- gous reagin-like antibodies and its specific inhibition with disodium cromoglycate. Immunology 16, 749–760 (1969)
Gramajo, R., Cervio, N.: The use in rheumatology of a synthetic antiserotonin: methysergide. Pren. méd. argent. 52, 2900–2902 (1965)
Green, A.F.: The antagonism of histamine and the anaphylactic response by phenylpyridylallylamines. Brit. J. Pharmacol. 8, 171–176 (1953)
Green, A.F.: Antihypertensive drugs. In: Garattini, S., Shaw, P. A. (Eds.): Advances in Pharmacology, Vol. 1, pp. 161–225. New York: Academic Press Inc. 1962
Greig, M.E., Griffin, R.L.: Antagonism of slow reacting substance in anaphylaxis (SRS-A) and other spasmogens on the guinea pig tracheal chain by hydratropic acids and their effects on anaphylaxis. J. med. Chem. 18, 112–116 (1975)
Gyermek, L.: Drugs which antagonize 5-hydroxytryptamine and related indolealkylamines. In: Erspamer, V. (Ed.): Handbook of Experimental Pharmacology, Vol. 19, pp. 471–528.Berlin-Heidelberg-New York: Springer 1966
Gyermek, L., Nador, K.: The pharmacology of tropane compounds in relation to their steric structure. J. Pharm. (Lond.) 9, 209–229 (1957)
Haddox, C.H., Saslaw, M.S.: Urinary 5-methoxytryptamine in patients with rheumatic fever. J. clin. Invest. 42, 435–441 (1963)
Halbert, S.P., Bircher, R., Dahle, E.: Studies on the mechanism of the lethal toxic action of streptolysin “O” and the protection by certain antiserotonin drugs. J. Lab. clin. Med. 61, 437–452 (1963)
Halpern, B.N.: Synthetic antihistamine substances. Arch. int. Pharmacodyn. 68, 339–408 (1942)
Halpern, B.N., Dumas, J., Reber, H.: Rôle favorisant d’un antihistaminique de synthese dans la généralisation de l’infection locale. C.R. Soc. Biol. (Paris) 143, 1563–1565 (1949)
Halpern, B.N., Liacopoulos, P., Liacopoulos-Briot, M.: Recherches sur les substances exogenes et endogenes agissant sur la permeabilite capillaire et leur antagonists. Arch. int. Pharmacodyn. 119, 56–101(1959)
Halpern, B.N., Neveu, T., Spector, S.: On the nature of the chemical mediators involved in anaphylactic reactions in mice. Brit. J. Pharmacol. 20, 389–398 (1963)
Ham, N.S.: Solution conformation of antihistamines. J. pharm. Sci. 60, 1764–1765 (1971)
Hanna, P.E., Ahmed, A.E.: Conformationally restricted analogues of histamine Hl receptor antagonists, trans and cis-1, 5-Diphenyl-3-dimethylaminopyrrolidine. J. med. Chem. 16, 963–968 (1973)
Harms, A.F., Nauta, W.T.: The effects of alkyl substitution in drugs. 1. Substituted dimethyl-aminoethyl benzhydryl ethers. J. med. Chem. 2, 57–77 (1960)
Henson, P.M., Cochrane, C. G.: Immunological induction of increased vascular permeability. I.A rabbit passive cutaneous anaphylactic reaction requiring complement, platelets, and neutrophils. J. exp. Med. 129, 153–165 (1969)
Herxheimer, H.: The 5-hydroxytryptamine shock in the guinea-pig. J. Physiol. (Lond.) 128, 435–445 (1955)
Herxheimer, H., Stresemann, E.: The effect of some new antihistamines on the anaphylactic microshock of the guinea pig. Brit. J. Pharmacol. 21, 414–418 (1963)
Higginbotham, R.D.: Influence of adrenalectomy and Cortisol on resistance of mice to histamine, serotonin, anaphylactic, and endotoxin shocks. J. Allergy 33, 35–44 (1962)
Highton, T.C., Garrett, M.H.: Some effects of serotonin and related compounds on human collagen. Lancet 1963, 1, 1234–1237
Ison, R.R., Casy, A.F.: Structural influences upon antihistamine activity; 3-amino-L-aryl-L-(2-pyridyl)propenes and related compounds. J. Pharm. (Lond.) 23, 848–856 (1971)
Ison, R.R., Franks, F.M., Soh, K.S.: The binding of conformationally restricted antihistamines to histamine receptors. J. Pharm. (Lond.) 25, 887–894 (1973)
James, M.N.G., Williams, G.J.B.: Structural studies of histamine H1 effector molecules: the crystal structure of the antihistaminic drug (+)-chlorpheniramine maleate; [(+)-S-(p-chlorophenyl)-L-(2-pyridyl)-3-N, N-dimethylamine maleate]. Canad. J. Chem. 52, 1872–1879 (1974)
Jones, D.G., Kay, A.B.: Inhibition of eosinophil Chemotaxis by the antagonist of slow reacting substance of anaphylaxis-compound FPL 55712. J. Pharm. (Lond.) 26, 917–918 (1974)
Julou, L., Ducrot, R., Bardone, M.C., Detaille, J.Y., Feo, C., Guyonnet, J.C., Loiseau, G., Pasquet, J.: Etude des propriétés pharmacologiques de la diméthylsulfamido-3 (diméthylamino-2 propyl)-10 phénothiazine (8, 599 R.P.). Arch. int. Pharmacodyn. 159, 70–86 (1966)
Kalz, F., Fekete, Z.: Studies on capillary permeability using Coomassie blue as indicator. J. invest. Derm. 36, 37–46 (1961)
Kellaway, C.H., Trethewie, E.R.: The liberation of a slow-reacting smooth muscle-stimulating substance in anaphylaxis. Quart. J. exp. Physiol. 30, 121–145 (1940)
Kier, L.B.: Molecular orbital calculations of the preferred conformations of histamine and a theory on its dual activity. J. med. Chem. 11, 441–445 (1968 a)
Kier, L.B.: Preferred conformation of serotonin and a postulate on the nature of its receptor from molecular orbital calculations. J. pharm. Sci. 57, 1188–1191 (1968b)
Kraft, E., Zimmerman, B.G.: Influence of histamine H1 and H2-receptor blockers on sympathetic vasodilator and vasoconstrictor responses in canine paw. Brit. J. Pharmacol. 53, 51–58 (1975)
Kutter, E., Hansen, C.: Steric parameters in drug design. Monoamine oxidase inhibitors and antihistamines. J. med. Chem. 12, 647–652 (1969)
Levi, R., Lee, C.-H.: Characterization of cardiac histamine receptors by means of selective H1 and H2-agonists and antagonists. Fed. Proc. 33, Abst. 2109 (1974)
Lindquist, K.J.: A unique class of rabbit immuno-globulins eliciting passive cutaneous anaphylaxis in homologous skin. Immunochemistry 5, 525–542 (1968)
Loew, E.R.: Pharmacology of antihistamine compounds. Physiol. Rev. 27, 542–573 (1947)
Logan, G., Wilhelm, D.L.: Vascular permeability changes in inflammation. I. The role of endogenous permeability factors in ultraviolet injury. Brit. J. exp. Path. 47, 300–314 (1966)
Maling, H.M., Webster, M.E., Williams, M.A., Wilford, S., Anderson, W.: Inflammation induced by histamine, serotonin, bradykinin and compound 48/80 in the rat: antagonists and the mechanism of action. J. Pharmacol, exp. Ther. 191, 300–310 (1974)
Margolin, S., Tislow, R.: Experimental and clinical efficacy of trimeton and chlor-trimeton maleate. Ann. Allergy 8, 515–518 (1950)
Mathé, A.A., Strandberg, K.: Antagonism of slow reacting substance by polyphloretin phosphate on isolated human bronchi. Acta physiol. scand. 82, 460–465 (1971)
Mathe, A.A., Strandberg, K., Fredholm, B.: Antagonism of prostaglandin F2α induced bronchoconstriction and blood pressure changes by polyphloretin phosphate in the guinea-pig and cat. J. Pharm. (Lond.) 24, 378–382 (1972)
Mawson, C., Whittington, H.: Evaluation of the peripheral and central antagonistic activities against 5-hydroxytryptamine of some new agents. Brit. J. Pharmacol. 39, 223 P (1970)
McQueen, D.S.: The effects of prostaglandin E2, prostaglandin F2α and polyphloretin phosphate on respiration and blood pressure in anaesthetized guinea pigs. Life Sci. 12, 163–172 (1973)
Miles, A.A., Wilhelm, D.L.: The activation of endogenous substances inducing pathological in-creases of capillary permeability. Part I. A survey of endogenous permeability factors. In: The Biochemical Response to Injury, pp. 51–83. Oxford: Blackwell 1960
Mota, I.: Mast cells and anaphylaxis. Ann. N.Y. Acad. Sci. 103, 264–277 (1963)
Mota, I.: The mechanism of anaphylaxis. I. Production and biological properties of mast cell sensitizing antibody. Immunology 7, 681–699 (1964)
Movat, H.Z., Di Lorenzo, N.L., Taichman, N.S., Berger, S., Stein, H.: Suppression by antihistamine of passive cutaneous anaphylaxis produced with anaphylactic antibody in the guinea pig. J. Immunol. 98, 230–235 (1967)
Murray, M., Smith, W.D., Waddell, A.H., Jarrett, W.F.H.: Nippostrongylus brasiliensis: histamine and 5-hydroxytryptamine inhibition and worm expulsion. Exp. Parasit. 30, 58–63 (1971)
Nauta, W.T., Bultsma, T., Rekker, R.F., Timmerman, H.: Structure-activity relations in a series of compounds related to diphenhydramine. Med. Chem. Spec. Contrib. Int. Symp. 3rd., 1972, p. 125 (Pub. 1973). Ed. Pratesi, P. London: Butterworth 1973
Northover, B.J., Subramanian, G.: A study of possible mediators of inflammatory reactions in the mouse foot. Brit. J. Pharmacol. 18, 346–355 (1962)
Orange, R.P., Murphy, R.C., Austen, K.F.: Inactivation of slow reacting substance of anaphylaxis (SRS-A) by arylsulfatases. J. Immunol. 113, 316–322 (1974)
Orange, R.P., Murphy, R.C., Karnovsky, M.L., Austen, K.F.: The physicochemical characteristics and purification of slow-reacting substance of anaphylaxis. J. Immunol. 110, 760–770 (1973)
Orange, R.P., Stechschulte, D.J., Austen, K.F.: Immunochemical and biologic properties of rat IgE. II. Capacity to mediate the immunologic release of histamine and slow reacting substance of anaphylaxis (SRS-A). J. Immunol. 105, 1087–1095 (1970)
Orange, R.P., Valentine, M.D., Austen, K.F.: Antigen-induced release of slow reacting substance of anaphylaxis (SRS-Arat) in rats prepared with homologous antibody. J. exp. Med. 127, 767–782(1968)
Orr, T.S.C., Gwilliam, J., Cox, J.S.G.: Studies on passive cutaneous anaphylaxis in the rat with disodium cromoglycate. Immunology 19, 469–479 (1970)
Orr, T.S.C., Gwilliam, J., Cox, J.S.G.: Studies on passive cutaneous anaphylaxis in the rat with disodium cromoglycate. II. A comparison of the rat anti-DNP 7 Sy2 and rat reagin induced cutaneous reactions. Immunology 21, 405–417 (1971)
Ovary, Z.: Immediate reactions in the skin of experimental animals provoked by antibody-antigen interaction. In: Kallos, P. (Ed.): Progr. Allergy, Vol. 5, pp. 459–508. Basel-New York: S. Karger 1958
Ovary, Z., Bier, O.G.: Quantitative studies on passive cutaneous anaphylaxis in the guinea pig and its relationship to the Arthus phenomenon. J. Immunol. 71, 6–11 (1953)
Palmer, M.A., Piper, P.J., Vane, J.R.: Release of rabbit aorta contracting substance (RCS) and prostaglandins induced by chemical or mechanical stimulation of guinea-pig lungs. Brit. J. Pharmacol. 49, 226–242 (1973)
Parratt, J.R., West, G.B.: Release of 5-hydroxytryptamine and histamine from tissues of the rat. J. Physiol. (Lond.) 137, 179–192 (1957 a)
Parratt, J.R., West, G.B.: 5-Hydroxytryptamine and the anaphylactoid reaction in the rat. J. Physiol. (Lond.) 139, 27–41 (1957 b)
Parratt, J.R., West, G.B.: Inhibition by various substances of oedema formation in the hind-paw of the rat induced by 5-hydroxytryptamine, histamine, dextran, egg white and compound 48/80. Brit. J. Pharmacol. 13, 65–70 (1958)
Paton, W.D.M.: Compound 48/80: a potent histamine liberator. Brit. J. Pharmacol. 6, 499–508 (1951)
Paton, W.D.M.: The release of histamine. In: Kallos, P. (Ed.): Progr. Allergy, Vol. 5, pp. 79–148. Basel-New York: S. Karger 1958
Peck, A.W., Fowle, A.S.E., Bye, C.: A comparison of triprolidine and clemastine on histamine antagonism and performance tests in man: implications for the mechanism of drug induced drowsiness. Europ. J. clin. Pharmacol. 8, 455–463 (1975)
Perini, A., Mota, I.: Heterogeneity of guinea-pig homocytotropic antibodies. Immunology 22, 915–923 (1972)
Petri, G., Cspiak, J., Kovacs, A., Bentzik, M.: Data on the pathology of pyogenic inflammation. I. The role of histamine in pyogenic inflammation and the effect of antihistaminics on its course. Acta med. Acad. Sci. hung 3, 347–368 (1952)
Phair, J.P., Eisenfeld, A.J., Levine, R.J., Kantor, F.S.: Effects of pharmacological inhibition of histamine synthesis upon immunological reactions in guinea-pigs. Immunology 18, 611–619 (1970)
Piper, P.J., Vane, J.R.: Release of additional factors in anaphylaxis and its antagonism by antiin-flammatory drugs. Nature (Lond.) 223, 29–35 (1969)
Pletscher, A., Shore, P.A., Brodie, B.B.: Serotonin release as a possible mechanism of reserpine action. Science 122, 374–375 (1955)
Pletscher, A., Shore, P.A., Brodie, B.B.: Serotonin as a mediator of reserpine action in brain. J. Pharmacol, exp. Ther. 116, 84–89 (1956)
Radwan, A.C., West, G.B.: Alterations in histidine decarboxylase activity during anaphylactic shock in the rat. Brit. J. Pharmacol. 30, 392–399 (1967)
Rekker, R.F., Nauta, W.T., Bultsma, T., Waringa, C.G.: Integrated QSAR of Hreceptor antagonists. Europ. J. med. Chem. 10, 557–562 (1975)
Reuse, J.J.: Antihistamine drugs and histamine release, especially in anaphylaxis. In: Wolstenholme, G.E.W., O’Connor, C.M. (Eds.): Histamine. Ciba Foundation Symposium 1955, pp. 150–154. London: Churchill 1956
Rieveschl, G.R.: Dialkylaminoalkyl benzhydryl ethers. U.S. Patent 2, 421, 714 (1947)
Rochae Silva, M.: Chemical mediators of the acute inflammatory reaction. Ann. N.Y. Acad. Sci. 116, 899–911(1964)
Rochae Silva, M. Ed.: Handbook of Experimental Pharmacology. Histamine and Antihistaminics. Part 1. Histamine. Its chemistry, metabolism, and physiological and pharmacological actions, Vol. XVIII. Berlin-Heidelberg-New York: Springer 1966
Rochae Silva, M. (Eds.): Handbook of Experimental Pharmacology, Part 2. Histaminen and Antihistaminics, Vol. XVIII. Berlin-Heidelberg-New York: Springer 1977
Rowley, D.A., Benditt, E. P.: 5-Hydroxytryptamine and histamine as mediators of the vascular injury produced by agents which damage mast cells in rats. J. exp. Med. 103, 399–411 (1956)
Sanyal, R.K., West, G.B.: Anaphylactic shock in the albino rat. J. Physiol. (Lond.) 142, 571–584 (1958 a)
Sanyal, R.K., West, G.B.: The relationship of histamine and 5-hydroxytryptamine to anaphylactic shock in different species. J. Physiol. (Lond.) 144, 525–531 (1958 b)
Schachter, M.: Histamine and Antihistamines, Vol. I. International Encyclopedia of Pharmacology and Therapeutics, Section 74. Oxford-New York-Toronto-Sydney-Braunschweig: Pergamon Press 1973
Scherbel, A.L., Harrison, J.W.: Exaggerated reactivity to serotonin in patients with rheumatoid arthritis and related diseases. Circulation 18, 777 (1958)
Scherbel, A.L., McKittrick, R.L., Hawk, W. A.: Lesions in rats caused by serotonin and histamine before and after amine oxidase inactivation and serotonin inhibition. J. clin. Invest. 39, 1025–1026 (1960)
Scherbel, A.L., Schmid, E.A.: Effect of serotonin inhibitors on connective tissue disease. Cleveland Clin. Quart. 29, 1–15 (1962)
Schneider, J.A.: Pharmacology of Rauwolfia. In: Rauwolfia. Pharmacology of Rauwolfia, pp. 109–143. Boston, Mass.: Little, Brown 1957
Sevitt, S.: Early and delayed oedema and increase in capillary permeability after burns of the skin. J. Path. Bact. 75, 27–37 (1958)
Sevitt, S., Bull, J.P., Cruickshank, C.N.D., Jackson, D.M., Lowbury, E.J.L.: Failure of an antihistamine drug to influence the course of experimental human burns. Brit. med. J. 1952II, 57–62
Sicuteri, R, Michelacci, S., Franchi, G.: Antagonism between an antiserotonin-the butanolamide of 1-methyl-lysergic-acid-and the effects of a histamine-liberating substance 48/80 B.W. in man. Int. Arch. Allergy 15, 291–299 (1959)
Shafi’ee, A., Hite, G.: The absolute configurations of the pheniramines, methyl phenidates, and pipradols. J. med. Chem. 12, 266–270 (1969)
Smith, J.B., Willis, A.L.: Aspirin selectively inhibits prostaglandin production in human platelets. Nature (New Biol.) 231, 235–237 (1971)
Sparrow, E.M., Wilhelm, D.L.: Species differences in susceptibility to capillary permeability factors: histamine, 5-hydroxytryptamine, and compound 48/80. J. Physiol. (Lond.) 137, 51–65 (1957)
Spector, W.G., Willoughby, D.A.: Histamine and 5-hydroxytryptamine in acute experimental pleurisy. J. Path. Bact. 74, 57–65 (1957)
Spector, W.G., Willoughby, D.A.: Experimental suppression of the early inflammatory phenomena of turpentine pleurisy in rats. Nature (Lond.) 181, 708–709 (1958)
Spector, W.G., Willoughby, D.A.: Experimental suppression of the acute inflammatory changes of thermal injury. J. Path. Bact. 78, 121–132 (1959a)
Spector, W.G., Willoughby, D.A.: The demonstration of the role of mediators in turpentine pleurisy in rats by experimental suppression of the inflammatory changes. J. Path. Bact. 77, 1–17 (1959 b)
Spector, W.G., Willoughby, D.A.: The inflammatory response. Bact. Rev. 27, 117–154 (1963)
Stacey, R.S.: Clinical aspects of cerebral and extracerebral 5-hydroxytryptamine. In: Handbook of Experimental Pharmacology. 5-Hydroxytryptamine and related indolealkylamines. Berlin-Heidelberg-New York: Springer-Verlag 1965, Vol. XIX
Starr, M.S., West, G.B.: Bradykinin and oedema formation in heated paws of rats. Brit. J. Pharmacol. 31, 178–187 (1967)
Stechschulte, D.J., Austen, K.F.: Anaphylaxis. In: Zweifach, B.W., Grant, L., McCluskey, R.T. (Eds.): The Inflammatory Process, 2nd Ed., Vol. III, Ch. 5. New York-London: Academic Press 1974
Stechschulte, D.J., Austen, K.F., Bloch, K.J.: Antibodies involved in antigen-induced release of slow reacting substance of anaphylaxis (SRS-A) in the guinea pig and rat. J. exp. Med. 125, 127–147 (1967)
Stewart, P.B., Bliss, J.Q.: The permeability-increasing factor in diluted human plasma. Brit. J. exp. Path. 38, 462–466 (1957)
Stone, C.A., Wenger, H.C., Ludden, C.T., Stavorski, J.M., Ross, C.A.: Antiserotonin-antihistaminic properties of cyproheptadine. J. Pharmacol, exp. Ther. 131, 73–84 (1961)
Strandberg, K., Uvnas, B.: Purification and properties of the slow reacting substance formed in the cat paw perfused with compound 48/80. Acta physiol. scand. 82, 358–374 (1971)
Stringer, H.C.W., Highton, T.C.: The shrinkage temperature of skin collagen. Aust. J. Derm. 5, 230–234(1960)
Takagi, K., Tukao, T.: Effects of some drugs on capillary permeability in the anaphylaxis of the mouse. Jap. J. Pharmacol. 21, 455–465 (1971)
Tokuda, S., Weiser, R.S.: Studies on the role of serotonin and mast cells in anaphylaxis of the mouse produced with soluble antigen-antibody complexes. J. Immunol. 86, 292–301 (1961)
Toldy, L., Vargha, L., Toth, L, Borsy, J.: Promethazine 1. Acta chim. Acad. Sci. hung. 19, 273–275 (1959)
Trendelenberg, U.: The action of histamine and 5-hydroxytryptamine on isolated mammalian atria. J. Pharmacol, exp. Ther. 130, 450–460 (1960)
Uda, T.: The mode of inhibitory actions of guaiazulene and some other antiinflammatory agents on the anaphylactoid edemas. Nippon Yakurigaku Zasshi 56, 1151–1163 (1960)
Van Arman, C.G., Begany, A.J., Miller, L.M., Pless, H.H.: Some details of the inflammations caused by yeast and carrageenin. J. Pharmacol, exp. Ther. 150, 328–334 (1965)
Vane, J.R.: Inhibition of prostaglandin synthesis as a mechanism for aspirinlike drugs. Nature (New Biol.) 231, 232–235 (1971)
Vane, J.R., Ferreira, S.H.: Interactions between bradykinin and prostaglandins. Life Sci. 16, 804–805 (1975)
Vane, J.R., Ferreira, S.H.: Interactions between bradykinin and prostaglandins. In: Proc. No. 27 of the Fogerty International Center. Washington, D.C.: U.S. Government Printing Office 1976. In press
Vaz, N.M., Prouvost-Danon, A.: Behaviour of mouse mast cells during anaphylaxis in vitro. In: Kallos, P., Waksman, B.H. (Eds.): Progr. Allergy, Vol. XIII, pp. 111–173. Basel-New York: S. Karger 1969
Villaneuva, R., Hinds, L., Katz, R.L., Eakins, KE.: The effect of polyphloretin phosphate on some smooth muscle actions of prostaglandins in the cat. J. Pharmacol, exp. Ther. 180, 78–85 (1972)
Vinegar, R., Schreiber, W., Hugo, R.: Biphasic development of carrageenin edema in rats. J. Pharmacol, exp. Ther. 166, 96–103 (1969)
Vinegar, R., Truax, J.F., Selph, J.L.: Some quantitative temporal characteristics of carrageenin-induced pleurisy in the rat. Proc. Soc. exp. Biol. (N.Y.) 143, 711–714 (1973)
Vogel, G., Marek, M.L.: Über die Hemmung verschiedener Rattenpfoten-Ödeme durch Serotonin-Antagonisten. Arzneimittel-Forsch. 11, 1051–1054 (1961)
Warner, R.R.P.: Current status and implications of serotonin in clinical medicine. In: Dock, W., Snapper, I. (Eds.): Advances in Internal Medicine, Vol. XIII, pp. 241–282. Chicago: New Book Medical Publ. Inc. 1967
Weeks, R.E., Gunnar, R.M.: Effect of tripelennamine hydrochloride on acute inflammation. Arch. Path. (Chicago) 48, 178–182 (1949)
Weis, J.: Investigations on some experimental inflammations in mouse paws. Med. exp. (Basel) 8, 1–11(1963)
Wells, P.W., Eyre, P.: The pharmacology of passive cutaneous anaphylaxis in the calf. Canad. J. Physiol. Pharmacol. 50, 255–262 (1972)
West, G.B.: 5-Hydroxytryptamine, tissue mast cells and skin oedema. Int. Arch. Allergy 10, 257–275 (1957)
Wilhelm, D.L.: The mediation of increased vascular permeability in inflammation. Pharmacol. Rev. 14, 251–280(1962)
Wilhelm, D.L.: Chemical mediators. In: Zweifach, B.W., Grant, L., McCluskey, R.T. (Eds.): The Inflammatory Process, 2nd Ed., Vol. II, pp. 251–301. New York-London: Academic Press 1973
Wilhelm, D.L., Mason, B.: Rationale of antihistaminic therapy in thermal injury. An experimental evaluation in the guinea pig. Brit. med. J. 1958II, 1141–1143
Wilhelm, D.L., Mason, B.: Vascular permeability changes in inflammation: the role of endogenous permeability factors in mild thermal injury. Brit. J. exp. Path. 41, 487–506 (1960)
Willis, A.L.: Parallel assay of prostaglandin-like activity in rat inflammatory exudate by means of cascade superfusion. J. Pharm. (Lond.) 21, 126–128 (1969 a)
Willis, A.L.: Release of histamine, kinin, and prostaglandins during carrageenin-induced inflammation in the rat. In: Mantegazza, P., Horton, E.W. (Eds.): Prostaglandins, Peptides, and Amines, pp. 31–38. London-New York: Academic Press 1969b
Willoughby, D.A.: Pharmacological suppression of increased capillary permeability following irradiation of the intestine of rats. Nature (Lond.) 184, 1156 (1959)
Willoughby, D.A.: Pharmacological aspects of the vascular permeability changes in the rat’s intestine following abdominal radiation. Brit. J. Radiol. 33, 515–519 (1960)
Willoughby, D.A.: Mediation of increased vascular permeability of inflammation. In: Zweifach, B.W., Grant, L., McCluskey, R.T. (Eds.): The Inflammatory Process, 2nd Ed., Vol. II, pp. 303–331. New York-London: Academic Press 1973
Winter, C.A., Risley, E.A., Nuss, G.W.: Carrageenin-induced edema in hind paw of the rat as an assay for antiinflammatory drugs. Proc. Soc. exp. Biol. (N.Y.) 111, 544–547 (1962)
Winter, C.A., Risley, E.A., Nuss, G.W.: Antiinflammatory and antipyretic activities of indome-thacin, l-(p-chlorobenzyl)-5-methoxy-2-methylindole-3-acetic acid. J. Pharmacol, exp. Ther. 141, 369–376 (1963)
Witiak, D.T.: Antiallergenic agents. In: Burger, A. (Ed.): Medicinal Chemistry, Vol. 2, 3rd Ed., Ch. 65, pp. 1643–1668. New York: Wiley 1970
Wood, D.R.: The effect on gastric secretion of different rates of histamine infusion and of “Neoantergan”. Brit. J. Pharmacol. 3, 231–236 (1948)
Woolley, D.W., Shaw, E.: Differentiation between receptors for serotonin and tryptamine by means of the exquisite specificity of antimetabolites. J. Pharmacol, exp. Ther. 121, 13–17 (1957)
Wyllie, J.H., Hesselbo, T., Black, J.W.: Effects in man of histamine H2-receptor blockade by burimamide. Lancet 1972II, (7787), 1117–1120
Zileli, T., Chapman, L., Wolff, H.G.: Antiinflammatory action of UML-491 (1-methyl-D-lysergic acid butanolamide dimaleate) demonstrated by the granuloma pouch technique in rats. Arch. int. Pharmacodyn. 136, 463–464 (1962)
Zvaifler, N.J., Bauer, H., Robinson, J.O.: IgE immunoglobulin in the rabbit. In: Austen, K.F., Becker, E.L. (Eds.): Biochemistry of the Acute Allergic Reactions, Vol. 2, pp. 33–44. Oxford: Blackwell 1971
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1979 Springer-Verlag Berlin Heidelberg
About this chapter
Cite this chapter
Green, A.F., Garland, L.G., Hodson, H.F. (1979). Antagonists of Histamine, 5-Hydroxytryptamine and SRS-A. In: Vane, J.R., Ferreira, S.H. (eds) Anti-Inflammatory Drugs. Handbook of Experimental Pharmacology, vol 50 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-66891-3_15
Download citation
DOI: https://doi.org/10.1007/978-3-642-66891-3_15
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-642-66893-7
Online ISBN: 978-3-642-66891-3
eBook Packages: Springer Book Archive