Synthesis of 1??Methyl??5??(pyrazol??3??and??5??yl??and 1, 2, 4??triazol??3??and 5??yl)??1, 2, 3, 6??tetrahydropyridine Derivatives and Their Evaluation as Muscarinic Receptor …

…, C Mustazza, A Borioni, F Gatta, K Tayebati…

Index: Del Giudice, Maria Rosaria; Mustazza, Carlo; Borioni, Anna; Gatta, Franco; Tayebati, Khosrow; Amenta, Francesco; Tucci, Paolo; Pieretti, Stefano Archiv der Pharmazie, 2003 , vol. 336, # 3 p. 143 - 154

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Citation Number: 6

Abstract

Abstract A series of 1-methyl-5-(pyrazol-3-and-5-yl-and 1, 2, 4-triazol-3-and 5-yl)-1, 2, 3, 6- tetrahydropyridine derivatives structurally related to arecoline were synthesized and evaluated on M 1, M 2, and M 3 muscarinic receptors using [3 H] pirenzepine and [3 H] NMS as ligands. The binding affinity depended on the position and size of the substituents. The most interesting compounds were further evaluated in functional studies on isolated ...