Author/Authors :
Paul A. Wyman، نويسنده , , Howard R. Marshall، نويسنده , , Sean T. Flynn، نويسنده , , Ron J. King، نويسنده , , Mervyn Thompson، نويسنده , , Paul W. Smith، نويسنده , , Michael S. Hadley، نويسنده , , Gary W. Price، نويسنده , , Claire M. Scott، نويسنده , , Lee A. Dawson، نويسنده ,
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.
