Synthesis, in vitro [3H] prazosin displacement, and in vivo activity of 3-aryl-4, 5, 6, 7-tetrahydropyrazolo [4, 3-c] pyridines, a new class of antihypertensive agents

G Winters, A Sala, D Barone…

Index: Winters, Giorgio; Sala, Alberto; Barone, Domenico; Baldoli, Emiliana Journal of Medicinal Chemistry, 1985 , vol. 28, # 7 p. 934 - 940

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Citation Number: 21

Abstract

The a-adrenoceptor antagonists prazosin, corynanthine, and WB 4101 lower blood pressure mainly by blocking postsynaptic a,-adrenoceptors on the vascular effector Prazosin, which may also have central a-blocking activity; is the only one used in antihypertensive therapy, but its use is restricted by a serious side effect, namely," the first-dose phenomenonn, a severe initial hypotension associated with syncope."'During a program of synthesis of new ...