| 12467625 |
Chen J, Norrholm S, Dwoskin LP, Crooks PA, Bai D: N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2 (*) and alpha7 (*) neuronal nicotinic acetylcholine receptors. Bioorg Med Chem Lett. 2003 Jan 6;13(1):97-100.
A series of N,N-disubstituted piperazines were prepared and evaluated for binding to alpha4beta2 (*) and alpha7 (*) neuronal nicotinic acetylcholine receptors using rat striatum and whole brain membrane preparations, respectively. This series of compounds exhibited selectivity for alpha4beta2 (*) nAChRs and did not interact with the alpha7 (*) nAChRs subtype. The most potent analogues were compounds 8b and 8f (K (i)=32 microM). Thus, linking together a pyridine pi-system and a cyclic amine moiety via a piperazine ring affords compounds with low affinity, but good selectivity for alpha4beta2 (*) nicotinic receptors. |
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