A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to r1 and r2 receptors. Many compounds exhibited nanomolar affinity for r1 subtype receptor with good selectivity over r2. A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.
Design, synthesis, and SAR analysis of novel selective sigma(1) ligands
PREZZAVENTO, Orazio;RONSISVALLE, Giuseppe;
2007-01-01
Abstract
A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to r1 and r2 receptors. Many compounds exhibited nanomolar affinity for r1 subtype receptor with good selectivity over r2. A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.File in questo prodotto:
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