Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.

JH, Lange; HK, Coolen; Stuivenberg HH, van; JA, Dijksman; AH, Herremans; E, Ronken; HG, Keizer; K, Tipker; AC, McCreary; W, Veerman; HC, Wals; B, Stork; PC, Verveer; Hartog AP, den; Jong NM, de; TJ, Adolfs; J, Hoogendoorn; CG, Kruse

doi:10.1021/jm031019q

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Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.

Shared by NobleBlocks on Jan 1, 2004 • 12:00 AM UTC

Authors:

Lange JH

Coolen HK

van Stuivenberg HH

Abstract

A series of novel 3,4-diarylpyrazolines was synthesized and evaluated in cannabinoid (hCB(1) and hCB(2)) receptor assays. The 3,4-diarylpyrazolines elicited potent in vitro CB(1) antagonistic activities and in general exhibited high CB(1) vs CB(2) receptor subtype selectivities. Some key representat...

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