title: Development of a presynaptic 5-HT1A antagonist.
abstract: A new 5-HT(1A) silent antagonist 14 (5-HT(1A) IC(50)=2.2 nM) antagonizes the effects of agonists on reciprocal forepaw treading behavior, on neuronal firing in the rat dorsal raphé, and on 5-HT(1A) release in the raphé and hippocampus. While 14 alone was inactive in the social interaction paradigm, it completely reversed the social interaction activity of the serotonergic compounds (buspirone, 1, and 2).
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. mattsonr@bms.com
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Mattson
authors.forename: John D
authors.initials: JD
authors.lastname: Catt
authors.forename: Charles P
authors.initials: CP
authors.lastname: Sloan
authors.forename: Qi
authors.initials: Q
authors.lastname: Gao
authors.forename: Richard B
authors.initials: RB
authors.lastname: Carter
authors.forename: Anthony
authors.initials: A
authors.lastname: Gentile
authors.forename: Cathy D
authors.initials: CD
authors.lastname: Mahle
authors.forename: F Fatima
authors.initials: FF
authors.lastname: Matos
authors.forename: Rachel
authors.initials: R
authors.lastname: McGovern
authors.forename: Cam P
authors.initials: CP
authors.lastname: VanderMaelen
authors.forename: Frank D
authors.initials: FD
authors.lastname: Yocca
mesh_terms: D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000494:pharmacology; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001923:Brain Chemistry / Q000187:drug effects; D002065:Buspirone / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004569:Electroencephalography / Q000187:drug effects; D007398:Interpersonal Relations; D008297:Male; D017551:Microdialysis; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D017661:Receptors, Presynaptic / Q000187:drug effects*; D011985:Receptors, Serotonin / Q000187:drug effects*; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists / Q000138:chemical synthesis*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D014151:Anti-Anxiety Agents; D017661:Receptors, Presynaptic; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D002065:Buspirone