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Biological Activity:
Potent and highly selective CB1 antagonist (Ki= 7.8 and 7943 nM for CB1 and peripheral cannabinoid CB2, respectively); more potent (100-fold) S-(-)-enantiomer in comparison with opposite R(+)-SLV319 (Axon 1714) .
References:
JH Lange etal. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J. Med.l Chem. 2004, 47(3), 627–643. [online]
JH Lange and CG Kruse. Recent advances in CB1 cannabinoid receptor antagonists. Curr. Opin. Drug Discov. Devel. 2004, 7(4), 498-506. [online]
AB Need et al. The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats. Psychopharmacol. 2006, 184(1), 26–35. [online]
Chemical Name: (S)-(-)-3-(4-chlorophenyl)-N'-(4-chlorophenylsulfonyl)-N-methyl-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamide
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