CHARACTERISTICS OF HISTAMINE H1-RECEPTORS IN PERIPHERAL-TISSUES LABELED WITH [MEPYRAMINE-H-3

  • 1 January 1979
    • journal article
    • research article
    • Vol. 209  (3) , 437-442
Abstract
Specific binding of [3H]mepyramine to membranes of various peripheral tissues of different species [rat, rabbit, guinea-pig, mice and a Cynomolgus monkey] was demonstrated. Drug specificity indicates an association with histamine H1-receptors. Of all the tissues examined brain contains the highest numbers of binding sites, while sustantial levels of specific [3H]mepyramine binding are also demonstrable in some species in heart, lung, adrenal and ileum. Negligible specific [3H]mepyramine bnding is observed in the liver, stomach and uterus of several species. The lesser bronchoconstricting response of the rat than of other species to histamine is paralleled by a lower number of [3H]mepyramine binding sites in rat lung than in other species. Similar numbers of [3H]mepyramine binding sites occur in ileal membranes of rat, guinea pig and rabbit, although contractile effects of histamine vary in these species. In the guinea-pig ileum, [3H]mepyramine binding is most concentrated in the longitudinal muscle itself where histamine exerts its predominant contractile effects. In the bovine adrenal gland, [3H]mepyramine binding is more abundant and has higher affinity for drugs in the medulla than in the cortex.

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