Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines

…, W Halczenko, JR Huff, JP Guare Jr…

Index: Saari, Walfred S.; Halczenko, Wasyl; Huff, Joel R.; Guare, James P.; Hunt, Cecilia A.; et al. Journal of Medicinal Chemistry, 1984 , vol. 27, # 9 p. 1182 - 1185

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Citation Number: 8

Abstract

A series of pyridinyltetrahydropyridine derivatives was synthesized and evaluated as adrenoceptor and tetrabenazine antagonists. 4-(3-Fluoro-2-pyridinyl)-1, 2, 5, 6- tetrahydropyridine proved to be the most potent and selective cyp-adrenoceptor antagonist of the series as measured in vitro by displacement of [3H] clonidine and [3H] prazosin from membrane binding sites of calf cerebral cortex and by antagonism of the effects of ...