Author/Authors :
Graeme Semple، نويسنده , , Britt-Marie Andersson، نويسنده , , Vijay Chhajlani، نويسنده , , Jennie Georgsson، نويسنده , , Magnus Johansson، نويسنده , , Marcel Lindschoten، نويسنده , , Fritof Pontén، نويسنده , , Asa Rosenquist، نويسنده , , Henrik S?rensen، نويسنده , , Lars Swanson، نويسنده , , Marianne Swanson، نويسنده ,
Abstract :
A new series of 3-aryl pyridone based kappa opioid receptor agonists was designed and synthesised, based on an understanding of the classical kappa opioid receptor pharmacophore. The most potent of the new compounds were comparable to U-69,593 in receptor affinity, selectivity and functional agonist effect at the cloned human kappa opioid receptor.