Author/Authors :
Axel R. Stoit، نويسنده , , Arnold P. den Hartog، نويسنده , , Harry Mons، نويسنده , , Sjoerd van Schaik، نويسنده , , Nynke Barkhuijsen، نويسنده , , Cees Stroomer، نويسنده , , Hein K.A.C. Coolen، نويسنده , , Jan-Hendrik Reinders، نويسنده , , Tiny J.P. Adolfs، نويسنده , , Martina van der Neut، نويسنده , , Hiskias Keizer، نويسنده , , Chris G. Kruse، نويسنده ,
Abstract :
We have investigated a series of 7-azaindoles as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (Ki = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation.
Keywords :
Azaindole derivatives , Partial agonist , Nicotinic acetylcholine receptor , Smoke cessation , cognition
