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N, N –Disubstituted piperazines and homopiperazines: Synthesis and affinities at α4β2* and α7* neuronal nicotinic acetylcholine receptors.
- Source :
-
Journal of Enzyme Inhibition & Medicinal Chemistry . Dec2006, Vol. 21 Issue 6, p667-680. 14p. 6 Diagrams, 4 Charts. - Publication Year :
- 2006
-
Abstract
- 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. [ABSTRACT FROM AUTHOR]
- Subjects :
- *PIPERAZINE
*NICOTINIC receptors
*CHOLINERGIC receptors
*PYRIDINE
*BIOSYNTHESIS
Subjects
Details
- Language :
- English
- ISSN :
- 14756366
- Volume :
- 21
- Issue :
- 6
- Database :
- Academic Search Index
- Journal :
- Journal of Enzyme Inhibition & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23463225
- Full Text :
- https://doi.org/10.1080/14756360600900513