PMID: 108389Jun 1, 1979

Characteristics of histamine H1-receptors in peripheral tissues labeled with [3H]mepyramine

The Journal of Pharmacology and Experimental Therapeutics
R S ChangS H Snyder

Abstract

Specific binding of [3H]mepyramine to membranes of various peripheral tissues of different species has been demonstrated. Drug specificity indicates an association with histamine H1-receptors. Of all the tissues examined brain contains the highest numbers of binding sites, while substantial levels of specific [3H]mepyramine binding are also demonstrable in some species in heart, lung, adrenal and ileum. Negligible specific [3H]mepyramine binding 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. However, similar numbers or [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 quinea-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.

Related Concepts

Adrenal Glands
Aminopyridines
Anthropoidea
Ascending Aorta Structure
Cavia porcellus
Ileum
Lung
Macaca fascicularis
Smooth Muscle
Myocardium

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