Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 3, Issue 12, Pages 1054-1058Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml3002715
Keywords
Nicotinic acetylcholine receptor; sigma-1 receptor; alkoxyisoxazole; pharmacophore; broad screening
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Funding
- National Institute of Mental Health [U19MH085193]
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Comparative analyses of the pharmacophoric elements required for sigma 1 and nicotinic ligands led to the identification of a potent and selective sigma 1 ligand (15). Compound 15 displayed high selectivity for the sigma 1 receptor (K-i, sigma 1 = 4.1 nM; K-i, sigma 2 = 1312 nM) with moderate binding affinity for the DAT (K-i = 373 nM) and NET (K-i = 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 modification could be used as a tool to switch a ligand's selectivity between nAChRs and sigma receptors.
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