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 Chem Lett. 2000 Sep 4;10(17):1991-4. doi: 10.1016/s0960-894x(00)00400-5.
G S Welmaker  1 ,  J A Nelson ,  J E Sabalski ,  A L Sabb ,  J R Potoski ,  D Graziano ,  M Kagan ,  J Coupet ,  J Dunlop ,  H Mazandarani ,  S Rosenzweig-Lipson ,  S Sukoff ,  Y Zhang
Affiliations
  • 1. Medicinal Chemistry, Chemical Sciences, Wyeth-Ayerst Research, Princeton, NJ 08543, USA. [email protected]
PMID: 10987434 DOI: 10.1016/s0960-894x(00)00400-5
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.).

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