Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
J Med Chem
; 27(9): 1182-5, 1984 Sep.
Article
en En
| MEDLINE
| ID: mdl-6088770
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 alpha 2-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.
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Banco de datos:
MEDLINE
Asunto principal:
Piridinas
/
Tetrabenazina
/
Receptores Adrenérgicos alfa
Límite:
Animals
Idioma:
En
Año:
1984
Tipo del documento:
Article