title: Identification of a potent and selective 5-HT1B receptor antagonist.
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.
authors.affiliation: Psychiatry CEDD, New Frontiers Science Park, GlaxoSmithKline, Third Avenue, Harlow, Essex CM19 5AW, UK. paul.wyman@gsk.com
authors.forename: Paul A
authors.initials: PA
authors.lastname: Wyman
authors.forename: Howard R
authors.initials: HR
authors.lastname: Marshall
authors.forename: Sean T
authors.initials: ST
authors.lastname: Flynn
authors.forename: Ron J
authors.initials: RJ
authors.lastname: King
authors.forename: Mervyn
authors.initials: M
authors.lastname: Thompson
authors.forename: Paul W
authors.initials: PW
authors.lastname: Smith
authors.forename: Michael S
authors.initials: MS
authors.lastname: Hadley
authors.forename: Gary W
authors.initials: GW
authors.lastname: Price
authors.forename: Claire M
authors.initials: CM
authors.lastname: Scott
authors.forename: Lee A
authors.initials: LA
authors.lastname: Dawson
mesh_terms: D000818:Animals; D006801:Humans; D008024:Ligands; D008862:Microsomes, Liver; D051381:Rats; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D058829:Serotonin 5-HT1 Receptor Antagonists; D012702:Serotonin Antagonists