Identification of a potent and selective 5-HT 1B receptor antagonist

…, HR Marshall, ST Flynn, RJ King, M Thompson…

Index: Wyman, Paul A.; Marshall, Howard R.; Flynn, Sean T.; King, Ron J.; Thompson, Mervyn; Smith, Paul W.; Hadley, Michael S.; Price, Gary W.; Scott, Claire M.; Dawson, Lee A. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 21 p. 4708 - 4712

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Citation Number: 5

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.