Author/Authors :
James Crawforth، نويسنده , , Simon Goodacre، نويسنده , , Robert Maxey، نويسنده , , Sylvie Bourrain، نويسنده , , Smita Patel، نويسنده , , Rosemarie Marwood، نويسنده , , Desmond OʹConnor، نويسنده , , Richard Herbert، نويسنده , , Peter Hutson، نويسنده , , Michael Rowley، نويسنده ,
Abstract :
A series of 3-(4-piperidinyl)- and 3-(8-aza-bicyclo[3.2.l]oct-3-yl)-2-phenyl-1H-indoles have been prepared and evaluated as ligands for the h5-HT2A receptor. 3-(8-Phenethyl-8-aza-bicyclo[3.2.l]oct-3-yI)-2-phenyl-1H-indole is a high-affinity (1.2 nM), selective (>800 fold over h5-HT2C and hD2 receptors) antagonist at the h5-HT2A receptor with oral bioavailability in rats.
