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  • Title: Identification of a potent and selective 5-HT1B receptor antagonist.
    Author: Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA.
    Journal: Bioorg Med Chem Lett; 2005 Nov 01; 15(21):4708-12. PubMed ID: 16153839.
    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.
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