Chemical Name:6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridin
yl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide
dihydrochloride
Biological Activity:
5-HT2C receptor antagonist that
displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B
receptors respectively (pKi values are 9.0, 7.0 and 6.8 for 5-HT2C,
5-HT2B and 5-HT2A respectively). Also displays
selectivity over a range of other 5-HT, dopamine and adrenergic receptors.
Brain penetrant; exerts anxiolytic-like activity.
Bromidgeet al
(1997)
6-Chloro-5-methyl-1-[[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-indoline
(SB-242084): the first selective and brain penetrant 5-HT2C receptor
antagonist. J.Med.Chem. 40 3494. Kennetet al
(1997) SB 242084, a selective and brain penetrant 5-HT2C receptor
antagonist. Neuropharmacol. 36 609. Daltonet al
(2006) Serotonin 1B and 2C receptor interactions in the modulation of feeding
behaviour in the mouse. Psychopharmacol. 185 45.
Selective 5-HT7 receptor antagonist that displays > 100-fold selectivity over a range of other receptors. Reverses the hypothermic effect of 5-CT in mice following i.p. administration.
