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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.

Welmaker, G S; Nelson, J A; Sabalski, J E; Sabb, A L; Potoski, J R; Graziano, D; Kagan, M; Coupet, J; Dunlop, J; Mazandarani, H; Rosenzweig-Lipson, S; Sukoff, S; Zhang, Y.

Bioorg Med Chem Lett ; 10(17): 1991-4, 2000 Sep 04.

Article in English | MEDLINE | ID: mdl-10987434

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.).

Subject(s)

Appetite Depressants/chemical synthesis , Pyrazines/chemical synthesis , Quinoxalines/chemical synthesis , Receptors, Serotonin/drug effects , Serotonin Receptor Agonists/chemical synthesis , Animals , Appetite Depressants/pharmacology , Eating/drug effects , Male , Pyrazines/pharmacology , Quinoxalines/pharmacology , Rats , Rats, Sprague-Dawley , Receptor, Serotonin, 5-HT2C , Serotonin Receptor Agonists/pharmacology , Structure-Activity Relationship

ABSTRACT

Subject(s)

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