Structure—Activity Relationships for alpha-1 Adrenergic Receptor Agonists and Antagonists

Résumé fourni par la source

Ahlquist (1948) proposed that adrenergic receptors could be classified into two separate subtypes, designated as alpha and beta and invoked this hypothesis to explain the varying effects of sympathomimetic amines. Subsequently, it became apparent that these classifications were inadequate because of the demonstration by Furchgott (1967) and Lands et al. (1967) that the class of beta-adrenergic receptors consisted of at least two independent subtypes (beta-1 and beta-2), which could be identified and shown to mediate different pharmacologic responses. Recently, the alpha-adrenergic receptor was also shown to represent a nonhomogeneous population (Langer, 1973, 1974; Starke, 1972; Starke et al., 1975; Borowski et al., 1977), in that agonists and antagonists have been developed that demonstrate preferential activity at either a prejunctional alpha-adrenergic receptor located on the sympathetic nerve varicosity, or a postjunctional alpha-adrenergic receptor located on a particular effector organ and mediating its response. It was originally proposed that the terms alpha-1 and alpha-2 be used to designate the postjunctional and prejunctional alpha-adrenergic receptors, respectively (Langer, 1974). These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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