A series of N,N-disubstituted piperazines were prepared and evaluated for binding to α4β2* and α7* neuronal nicotinic acetylcholine receptors using rat striatum and whole brain membrane preparations, respectively. This series of compounds exhibited selectivity for α4β2* nAChRs and did not interact with the α7* nAChRs subtype. The most potent analogues were compounds 8b and 8f (Ki=32 μM). Thus, linking together a pyridine π-system and a cyclic amine moiety via a piperazine ring affords compounds with low affinity, but good selectivity for α4β2* nicotinic receptors.
|Number of pages||4|
|Journal||Bioorganic and Medicinal Chemistry Letters|
|State||Published - Jan 6 2003|
Bibliographical noteFunding Information:
This work was supported by grants from the National Natural Science Foundation of China and the National Institute on Drug Abuse (DA 10934, DA00399, and DA 07304).
ASJC Scopus subject areas
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry