Author/Authors :
Susan M. Westaway، نويسنده , , Ying-Kit Chung، نويسنده , , John B. Davis، نويسنده , , Vicky Holland، نويسنده , , Jeffrey C. Jerman، نويسنده , , Stephen J. Medhurst، نويسنده , , Harshad K. Rami، نويسنده , , Geoffrey Stemp، نويسنده , , Alexander J. Stevens، نويسنده , , Mervyn Thompson، نويسنده , , Kim Y. Winborn، نويسنده , , James Wright، نويسنده ,
Abstract :
Starting from the high throughput screening hit (3), novel N-tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl carboxamides have been identified as potent antagonists of the ion channel TRPV1. The N-quinolinylnicotinamide (46) showed excellent potency at human, guinea pig and rat TRPV1, a favourable in vitro DMPK profile and activity in an in vivo model of inflammatory pain.
