title: Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.
abstract: A series of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines was shown to exhibit 5-HT2C agonist binding and functional activity. Compound 21R inhibited food intake over 2 h in fasted, male Sprague Dawley rats with ED50 values of 2 mg/kg (i.p.) and 10 mg/kg (p.o.).
authors.affiliation: Medicinal Chemistry, Chemical Sciences, Wyeth-Ayerst Research, Princeton, NJ 08543, USA. welmakg@war.wyeth.com
authors.forename: G S
authors.initials: GS
authors.lastname: Welmaker
authors.forename: J A
authors.initials: JA
authors.lastname: Nelson
authors.forename: J E
authors.initials: JE
authors.lastname: Sabalski
authors.forename: A L
authors.initials: AL
authors.lastname: Sabb
authors.forename: J R
authors.initials: JR
authors.lastname: Potoski
authors.forename: D
authors.initials: D
authors.lastname: Graziano
authors.forename: M
authors.initials: M
authors.lastname: Kagan
authors.forename: J
authors.initials: J
authors.lastname: Coupet
authors.forename: J
authors.initials: J
authors.lastname: Dunlop
authors.forename: H
authors.initials: H
authors.lastname: Mazandarani
authors.forename: S
authors.initials: S
authors.lastname: Rosenzweig-Lipson
authors.forename: S
authors.initials: S
authors.lastname: Sukoff
authors.forename: Y
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000818:Animals; D001067:Appetite Depressants / Q000138:chemical synthesis* / Q000494:pharmacology; D004435:Eating / Q000187:drug effects; D008297:Male; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin / Q000187:drug effects*; D017366:Serotonin Receptor Agonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001067:Appetite Depressants; D011719:Pyrazines; D011810:Quinoxalines; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists