Author/Authors :
Duncan Shaw، نويسنده , , Gary G. Chicchi، نويسنده , , Jason M. Elliott، نويسنده , , Marc Kurtz، نويسنده , , Denise Morrison، نويسنده , , Mark P. Ridgill، نويسنده , , Nicola Szeto، نويسنده , , Alan P. Watt، نويسنده , , Angela R. Williams، نويسنده , , Christopher J. Swain، نويسنده ,
Abstract :
The in vivo properties of a series of 2-arylindole NK1 antagonists have been improved, by modification of the amide substituent. The 1-(2-methoxyphenyl)piperazine amide was identified as a major area of metabolism in the lead compound 1. Replacement of this amine moiety by a 4-benzyl-4-hydroxypiperidine resulted in a compound 18 with reduced clearance and improved central duration of action.
