1. Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors
- Author
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Michael J. Seminerio, Bahar Noorbakhsh, Andrew Coop, Lidiya Stavitskaya, Rae R. Matsumoto, and Jason R. Healy
- Subjects
Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Convulsants ,Ring (chemistry) ,Biochemistry ,Article ,Mice ,Cocaine ,Seizures ,Phenethylamines ,Drug Discovery ,Ethylamines ,medicine ,Animals ,Receptors, sigma ,Receptor ,Molecular Biology ,Propylamines ,Chemistry ,Organic Chemistry ,Sigma ,Cyclohexanols ,Ligand (biochemistry) ,Receptor selectivity ,Opioid ,Molecular Medicine ,Antagonism ,Selectivity ,Protein Binding ,medicine.drug - Abstract
A series of ring-constrained phenylpropyloxyethylamines, partial opioid structure analogs and derivatives of a previously studied sigma (σ) receptor ligand, was synthesized and evaluated at σ and opioid receptors for receptor selectivity. The results of this study identified several compounds with nanomolar affinity at both σ receptor subtypes. Compounds 6 and 9 had the highest selectivity for both σ receptor subtypes, compared to μ opioid receptors. In addition, compounds 6 and 9 significantly reduced the convulsive effects of cocaine in mice, which would be consistent with antagonism of σ receptors.
- Published
- 2013