Evidence for and against heterogeneity of alpha 1-adrenoceptors

Recent experimental evidence has suggested that the alpha 1 adrenoceptor may need to be further subdivided. It can no longer be stated categorically that alpha 1-adrenoceptors are present only at postjunctional sites, in view of several reports of alpha 1-mediated modulation of adrenergic and cholinergic neurotransmission. Furthermore, comparison of the pharmacologic characteristics of the alpha 1-adrenoceptor in different species and/or tissues can show clear differences in sensitivity to selective agonists and antagonists, and differences in the degree of dependence on extracellular calcium. However, in other cases, alpha 1-adrenoceptors at diverse sites have been found to have identical characteristics. Furthermore, the subcategories identified by the various selective agents do not fall into the same discrete groups, in contrast to division of alpha-adrenoceptors into alpha 1 and alpha 2-adrenoceptors. Therefore, at this time it seems premature to subdivide the alpha 1-adrenoceptor further.