Author/Authors :
Markian M. Stec، نويسنده , , Yunxin Bo، نويسنده , , Partha P. Chakrabarti، نويسنده , , Lillian Liao، نويسنده , , Mqhele Ncube، نويسنده , , Nuria Tamayo، نويسنده , , Rami Tamir، نويسنده , , Narender R. Gavva، نويسنده , , James J.S. Treanor، نويسنده , , Mark H. Norman، نويسنده ,
Abstract :
Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of 1. Compounds were identified that maintained potency, had good pharmacokinetic properties, and improved solubility relative to 1.
Keywords :
trpv1 , VR1 , Vanilloid receptor , Transient receptor potential , ion channel , AMG 517
