Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines

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 displa...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1984-09, Vol.27 (9), p.1182-1185
Main Authors: Saari, Walfred S, Halczenko, Wasyl, Huff, Joel R, Guare, James P, Hunt, Cecilia A, Randall, William C, Lotti, Victor J, Yarbrough, George G
Format: Article
Language:English
Subjects:
Animals
Blepharoptosis - drug therapy
Cerebral Cortex - metabolism
Chemistry
Clonidine - antagonists & inhibitors
Exact sciences and technology
Heterocyclic compounds
Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings
Male
Methoxamine - antagonists & inhibitors
Mice
Organic chemistry
Preparations and properties
Pyridines - chemical synthesis
Pyridines - pharmacology
Rats
Receptors, Adrenergic, alpha - metabolism
Structure-Activity Relationship
Tetrabenazine - antagonists & inhibitors
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00375a017