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ID: ALA1143456

Journal: Bioorg Med Chem Lett

Title: Identification of a potent and selective 5-HT1B receptor antagonist.

Authors: Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA.

Abstract: An SAR study around the mixed 5-HT1ABD receptor antagonist SB-272183 found that introduction of cis-2,6-dimethyl substitution onto the piperazine ring was a key structural change, which imparted a combination of both excellent selectivity over the 5-HT1A and 5-HT1D receptors and low intrinsic activity. This led to the identification of the selective 5-HT1B receptor antagonist SB-616234.

CiteXplore: 16153839

DOI: 10.1016/j.bmcl.2005.07.085