40273-45-8Relevant articles and documents
Adrenoceptor and Tetrabenazine Antagonism Activities of Some Pyridinyltetrahydropyridines
Saari, Walfred S.,Halczenko, Wasyl,Huff, Joel R.,Guare, James P.,Hunt, Cecilia A.,et al.
, p. 1182 - 1185 (1984)
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 α2-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 clonidine and methoxamine in the rat isolated, field-stimulated vas deferens.In addition, this compound, and the corresponding desfluoro derivative, blocked tetrabenazine-induced ptosis in the mouse.