Relevant Features of the Pharmacology of Prazosin

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Abstract
An account is given of the work performed in this laboratory to demonstrate that prazosin differs from the classical α-adrenoceptor antagonists in that it possesses a high degree of selectivity for α1-adrenoceptors as opposed to α2-adrenoceptors. This selectivity ensures the preservation of local feedback control of the release of noradrenergic transmitter by α2-adrenoceptors. It is considered to be largely responsible for the therapeutic success of prazosin and its relative absence of effects such as tolerance, tachycardia, diarrhoea, and renin release that severely limited the clinical application of the classical α-adrenoceptor antagonists. Mention is made of the potential use of prazosin as a research tool, especially as a radioligand in binding experiments, for the identification of α-adrenoceptors in different tissues and for the direct demonstration of changes in α1-adrenoceptor type and number in specific disease states.

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