Author/Authors :
Taekyu Lee، نويسنده , , Albert J. Robichaud، نويسنده , , Kristopher E. Boyle، نويسنده , , Yimin Lu، نويسنده , , David W. Robertson، نويسنده , , Keith J. Miller، نويسنده , , Larry W. Fitzgerald، نويسنده , , John F. McElroy، نويسنده , , Brian L. Largent، نويسنده ,
Abstract :
The discovery of N-substituted-pyridoindolines and their binding affinities at the 5-HT2A, 5-HT2C and D2 receptors, and in vivo efficacy as 5-HT2A antagonists is described. The structure–activity relationship of a series of core tetracyclic derivatives with varying butyrophenone sidechains is also discussed. This study has led to the identification of potent, orally bioavailable 5-HT2A/D2 receptor dual antagonists as potential atypical antipsychotics.
