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.
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.).
Welmaker
G S
GS
Medicinal Chemistry, Chemical Sciences, Wyeth-Ayerst Research, Princeton, NJ 08543, USA. welmakg@war.wyeth.com
Nelson
J A
JA
Sabalski
J E
JE
Sabb
A L
AL
Potoski
J R
JR
Graziano
D
D
Kagan
M
M
Coupet
J
J
Dunlop
J
J
Mazandarani
H
H
Rosenzweig-Lipson
S
S
Sukoff
S
S
Zhang
Y
Y
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
D001067:Appetite Depressants; D011719:Pyrazines; D011810:Quinoxalines; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists