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

Authors
Welmaker, GS Nelson, JA Sabalski, JE Sabb, AL Potoski, JR Graziano, D Kagan, M Coupet, J Dunlop, J Mazandarani, H Rosenzweig-Lipson, S Sukoff, S Zhang, YX
Citation
Gs. Welmaker et al., 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, BIOORG MED, 10(17), 2000, pp. 1991-1994
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
17
Year of publication
2000
Pages
1991 - 1994
Database
ISI
SICI code
0960-894X(20000904)10:17<1991:SA5(AO>2.0.ZU;2-0
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 exhibi t 5-HT2C agonist binding and Functional activity. Compound 21R inhibited fo od intake over 2 h in fasted, male Sprague-Dawley rats with ED50 values of 2 mg/kg (ip) and 10 mg/kg (po). (C) 2000 Elsevier Science Ltd. All rights r eserved.