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From ?4?2 Nicotinic Ligands to the Discovery of ?1 Receptor Ligands: Pharmacophore Analysis and Rational Design.


ABSTRACT: Comparative analyses of the pharmacophoric elements required for ?1 and nicotinic ligands led to the identification of a potent and selective ?1 ligand (15). Compound 15 displayed high selectivity for the ?1 receptor (Ki, ?1 = 4.1 nM, Ki, ?2 = 1312 nM) with moderate binding affinity for the DAT (Ki = 373 nM) and NET (Ki = 203 nM) in the PDSP broad screening panel of common CNS neurotransmitter transporters and receptors. The key finding in this present work is that a subtle structural modifica tion could be used as a tool to switch a ligand's selectivity between nAChRs and sigma receptors.

SUBMITTER: Yu LF 

PROVIDER: S-EPMC3638970 | BioStudies | 2012-01-01

REPOSITORIES: biostudies

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