Synthesis and muscarinic activities of 3-(pyrazolyl)-1, 2, 5, 6-tetrahydropyridine derivatives

R Plate, MJM Plaum, T de Boer, JS Andrews…

Index: Plate, Ralf; Plaum, Marc J. M.; De Boer, Thijs; Andrews, John S.; Rae, Duncan R.; Gibson, Sam Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 2 p. 227 - 237

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Citation Number: 28

Abstract

A series of 3-(pyrazolyl)-1, 2, 5, 6-tetrahydropyridine derivatives (B) was synthesized and tested for muscarinic activity in receptor binding assays using [3H]-oxotremorine-M (3H-OXO- M) and [3H]-pirenzepine (3H-PZ) as ligands. Potential muscarinic agonistic or antagonistic properties of the compounds were determined using binding studies measuring their potencies to inhibit the binding of 3H-OXO-M and 3H-PZ. Preferential inhibition of 3H-OXO ...

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