A series of N, N-disubstituted piperazines and homopiperazines were prepared and evaluated for binding to natural α4β2* and α7* neuronal nicotinic acetylcholine receptors (nAChRs) using whole brain membrane. Some compounds exhibited good selectivity for α4β2* nAChRs and did not interact with the α7* nAChRs subtype. The most potent analogs were compounds 8-19 (Ki = 10.4 μM), 8-13 (Ki = 12.0 μM), and 8-24 (Ki = 12.8 μM). Thus, linking together a pyridine π-system and a cyclic amine moiety via a homopiperazine ring affords compounds with low affinity but with good selectivity for α4β2* nAChRs.
|Number of pages||14|
|Journal||Journal of Enzyme Inhibition and Medicinal Chemistry|
|State||Published - Dec 2006|
Bibliographical noteFunding Information:
This work was supported by grants from the National Natural Science Foundation of China and the National Institute on Drug Abuse (DA017548).
- Neuronal nicotinic acetylcholine receptors
- α4β* receptors
ASJC Scopus subject areas
- Drug Discovery