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  • Title: Binding to alpha-adrenergic receptors: differential pharmacological potencies and binding affinities of benzodioxanes.
    Author: Kapur H, Rouot B, Snyder SH.
    Journal: Eur J Pharmacol; 1979 Aug 15; 57(4):317-28. PubMed ID: 226379.
    Abstract:
    We have compared the influence of a series of benzodioxane alpha-adrenergic antagonists on 3H-WB-4101 and 3H-clonidine binding to alpha-receptor sites in the brain and peripheral tissues with their pharmacological properties. The drug specificity of 3H-WB-4101 binding is quite similar in central and peripheral tissues. Pharmacological potencies of benzodioxanes at postsynaptic alpha-receptors in the rat vas deferens correlate with potencies at 3H-WB-4101 but not at 3H-clonidine binding sites. These findings suggest pharmacological effects of these drugs are mediated by "alpha-1 postsynaptic receptors" labeled by 3H-WB-4101. For several benzodioxanes absolute pharmacological potencies at postsynaptic alpha-receptors of the rat vas deferens are substantially less than their potencies at 3H-WB-4101 sites. The potencies of benzodioxane analogues at 3H-clinidine binding sites are similar to their pharmacological potencies at presynaptic autoreceptors in the rat vas deferens.
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