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pubmed:abstractText |
In an effort to probe the steric influence of C5 substitution of the pyridine ring on CNS binding affinity, analogues of 1 substituted with a bulky moiety--such as phenyl, substituted phenyl, or heteroaryl-were synthesized and tested in vitro for neuronal nicotinic acetylcholine receptor binding affinity. The substituted analogues exhibited Ki values ranging from 0.055 to 0.69 nM compared to a Ki value of 0.15 nM for compound 1. Assessment of functional activity at subtypes of neuronal nicotinic acetylcholine receptors led to identify several agonists and antagonists.
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pubmed:affiliation |
Neurological and Urological Diseases Research, D-47W, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. nanhorng.lin@abbott.com
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