Abstract
We have investigated a series of 7-azaindoles as potential partial agonists of the alpha4beta2 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.
MeSH terms
-
Alkaloids / chemistry
-
Alkaloids / metabolism
-
Animals
-
Aza Compounds / chemical synthesis
-
Aza Compounds / chemistry
-
Aza Compounds / pharmacokinetics
-
Aza Compounds / pharmacology
-
Azocines / chemistry
-
Azocines / metabolism
-
Brain / metabolism
-
Indoles / chemical synthesis
-
Indoles / chemistry*
-
Indoles / pharmacokinetics
-
Indoles / pharmacology*
-
Kinetics
-
Neurons / metabolism
-
Nicotinic Agonists / chemical synthesis
-
Nicotinic Agonists / chemistry*
-
Nicotinic Agonists / pharmacokinetics
-
Nicotinic Agonists / pharmacology*
-
Quinolizines / chemistry
-
Quinolizines / metabolism
-
Radioligand Assay
-
Rats
-
Receptors, Nicotinic / chemistry
-
Receptors, Nicotinic / metabolism
Substances
-
7-azaindole dimer
-
Alkaloids
-
Aza Compounds
-
Azocines
-
Indoles
-
Nicotinic Agonists
-
Quinolizines
-
Receptors, Nicotinic
-
nicotinic receptor alpha4beta2
-
cytisine