Abstract
A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma(1) and sigma(2) receptors. Many compounds exhibited nanomolar affinity for sigma(1) subtype receptor with good selectivity over sigma(2). A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.
MeSH terms
-
Animals
-
Brain / metabolism
-
Chemical Phenomena
-
Chemistry, Physical
-
Chromatography, Thin Layer
-
Drug Design
-
Guinea Pigs
-
In Vitro Techniques
-
Indicators and Reagents
-
Magnetic Resonance Spectroscopy
-
Membranes / metabolism
-
Models, Molecular
-
Molecular Conformation
-
Radioligand Assay
-
Receptors, sigma / drug effects*
-
Sigma-1 Receptor
-
Structure-Activity Relationship
Substances
-
Indicators and Reagents
-
Receptors, sigma