Adrenoceptor and Tetrabenazine Antagonism Activities of Some Pyridinyltetrahydropyridines

Article abstract of DOI:10.1021/jm00375a017

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.