Author/Authors :
Kim Y. Avenell، نويسنده , , Izzy Boyfield، نويسنده , , Martyn C. Coldwell، نويسنده , , Michael S. Hadley، نويسنده , , Maureen A. M. Healy، نويسنده , , Philip M. Jeffrey، نويسنده , , Christopher N. Johnson، نويسنده , , David J. Nash، نويسنده , , Graham J. Riley، نويسنده , , Emma E. Scott، نويسنده , , Stephen A. Smith، نويسنده , , Rachel Stacey، نويسنده , , Geoffrey Stemp، نويسنده , , Kevin M. Thewlis، نويسنده ,
Abstract :
Starting from a series of 2-aminotetralins 1, a novel series of N-[4-(4-phenylbenzoylamino)butyl]-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine D3 receptor has been designed. The effect of ligand chirality on binding affinity has been established. Selected derivatives (e.g. 2o, 2p) show high functional selectivity and enhanced in vivo properties compared to 1.
