Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor

…, G Marchese, JM Mussinu, P Saba, S Tambaro…

Index: Ruiu, Stefania; Pinna, Gerard A.; Marchese, Giorgio; Mussinu, Jean-Mario; Saba, Pierluigi; Tambaro, Simone; Casti, Paola; Vargiu, Romina; Pani, Luca Journal of Pharmacology and Experimental Therapeutics, 2003 , vol. 306, # 1 p. 363 - 370

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Citation Number: 99

Abstract

Abstract The compound N-piperidinyl-[8-chloro-1-(2, 4-dichlorophenyl)-1, 4, 5, 6- tetrahydrobenzo [6, 7] cyclohepta [1, 2-c] pyrazole-3-carboxamide](NESS 0327) was synthesized and evaluated for binding affinity toward cannabinoid CB 1 and CB 2 receptor. NESS 0327 exhibited a stronger selectivity for CB 1 receptor compared with N-piperidinyl-5- (4-chlorophenyl)-1-(2, 4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR ...