Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists. Article

Röver, S, Adams, DR, Bénardeau, A et al. (2005). Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists. . BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 15(15), 3604-3608. 10.1016/j.bmcl.2005.05.074

cited authors

  • Röver, S; Adams, DR; Bénardeau, A; Bentley, JM; Bickerdike, MJ; Bourson, A; Cliffe, IA; Coassolo, P; Davidson, JEP; Dourish, CT; Hebeisen, P; Kennett, GA; Knight, AR; Malcolm, CS; Mattei, P; Misra, A; Mizrahi, J; Muller, M; Porter, RHP; Richter, H; Taylor, S; Vickers, SP

authors

abstract

  • Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT(2) receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT(2C) receptor agonists.

publication date

  • August 1, 2005

webpage

published in

keywords

  • Animals
  • Eating
  • Indoles
  • Injections, Subcutaneous
  • Pyrazines
  • Pyridines
  • Rats
  • Rats, Wistar
  • Serotonin 5-HT2 Receptor Agonists
  • Serotonin Receptor Agonists
  • Structure-Activity Relationship

Location

  • England

Digital Object Identifier (DOI)

start page

  • 3604

end page

  • 3608

volume

  • 15

issue

  • 15