Abstract
An extended series of structurally different histamine H 1 receptor antagonists was investigated for binding at central and peripheral histamine H 1 receptors in vitro. Antagonist affinities were measured by displacements of [ 3H]mepyramine from both guinea-pig cerebellum and lung membrane suspensions. Single [ 3H]mepyramine binding sites with identical affinity for [ 3H]mepyramine were found in both tissues; however, the H 1 receptor density was 6-fold lower in lungs than in cerebellum. None of the antagonists tested showed substantial preference for either of the receptors. It is concluded from the displacement data that there is no difference between the antagonist binding sites of cerebellum and lung H 1 receptors.
Published Version
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