Antagonists of Histamine, 5-Hydroxytryptamine and SRS-A

  • A. F. Green
  • L. G. Garland
  • H. F. Hodson
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 50 / 2)


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).


Capillary Permeability Antigen Challenge Disodium Cromoglycate Passive Cutaneous Anaphylaxis Systemic Anaphylaxis 
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  • A. F. Green
  • L. G. Garland
  • H. F. Hodson

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