Abstract [ 3 H]Mepyramine binds with high affinity to membranes from brain of human, rat, guinea‐pig, rabbit and mouse with drug specificity indicating an association with histamine H 1 receptors. Considerable species differences occur in the affinity of [ 3 H]mepyramine, with guinea‐pig and human having 34 times greater affinity than rat, mouse or rabbit. The greater affinity of [ 3 H]mepyramine in guinea‐pig than in rat is attributable both to faster association and slower dissociation rates in guinea‐pig. Species differences in affinity for H 1 receptor sites occur for some antihistamines but not for others. Some tricyclic antidepressant and neuroleptic drugs are extremely potent inhibitors of [ 3 H]mepyramine binding, exceeding in potency any H 1 antihistamines examined. The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [ 3 H]mepyramine binding. The regional distribution of specific [ 3 H]mepyramine binding differs considerably in the various species examined.
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Chang et al. (1979) studied this question.
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