From a4ß2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design

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From a4ß2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design

Comparative analyses of the pharmacophoric elements required for σ1 and nicotinic ligands led to the identification of a potent and selective σ1 ligand (15). Compound 15 displayed high selectivity for the σ1 receptor (Ki, σ1 = 4.1 nM; Ki, σ2 = 1312 nM) with moderate binding affinity for the DAT (Ki...

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Bibliographic Details
Main Authors:	Yu, L., Zhang, H., Gunosewoyo, Hendra, Kozikowski, A.
Format:	Journal Article
Published:	American Chemical Society 2012
Subjects:	broad screening sigma-1 receptor alkoxyisoxazole Nicotinic acetylcholine receptor pharmacophore
Online Access:	http://hdl.handle.net/20.500.11937/17442

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