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Some studies of the action of betahistine at H1 and H2 receptors for histamine

  • Histamine and Kinins
  • Proceedings of the Symposium ‘The Mast Cell Revisited’ November 8, 1984 New York, USA
  • Published:
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Abstract

Betahistine produced a concentration-dependent contraction of the guinea-pig ileum and was about 27 times less active than histamine in this respect. Betahistine induced desensitization of contractile responses to histamine in the guinea-pig ileum. The H1 histamine receptor antagonist mepyramine was a competitive antagonist of the action of betahistine on the guinea-pig ileum.

Betahistine caused relaxation of the rat uterus contracted by acetylcholine, and this action of betahistine was blocked by the H2 receptor antagonist cimetidine. Betahistine had a concentration-dependent positive chronotropic action on isolated guinea-pig atria, and in this respect was tenfold less potent than histamine. The action of betahistine on the atria was blocked by the H2 receptor antagonist YM11170. Betahistine caused a concentration-related contraction of the isolated lung parenchymal strip of the guinea-pig, and YM11170 potentiated this effect.

Betahistine failed to release histamine from rat peritoneal mast cells at concentrations up to 100 μM and it did not prevent histamine release induced by either substance P or anti-IgE.

Betahistine produced a dose-related flare and wheal reaction when injected intradermally into human skin.

It is concluded that betahistine has agonist activity at both H1 and H2 receptors for histamine.

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Authors and Affiliations

  1. Department of Pharmacology, University College London, Gower Street, WC1E 6BT, London

    P. R. Gater, S. E. Webber, G. P. H. Gui, N. A. Hayes & J. C. Foreman

  2. Department of Neuropharmacology, Glaxo Group Research Limited, SG12 0DJ, Ware, Hertfordshire

    C. C. Jordan

  3. Duphar Laboratories Limited, Gaters Hill, SO3 3JD, West End, Southampton

    J. J. Ashford

Authors
  1. P. R. Gater
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  2. S. E. Webber
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  3. G. P. H. Gui
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  4. C. C. Jordan
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  5. N. A. Hayes
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  6. J. J. Ashford
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  7. J. C. Foreman
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Gater, P.R., Webber, S.E., Gui, G.P.H. et al. Some studies of the action of betahistine at H1 and H2 receptors for histamine. Agents and Actions 18, 342–350 (1986). https://doi.org/10.1007/BF01964995

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  • DOI: https://doi.org/10.1007/BF01964995

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