Abstract: A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma1 and sigma2 receptors. Many compounds exhibited nanomolar affinity for sigma1 subtype receptor with good selectivity over sigma2. 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 sigma1 ligands
COLLINA, SIMONA;LINATI, LAURA;CALLEGARI, ATHOS MARIA;AZZOLINA, ORNELLA
2007-01-01
Abstract
Abstract: A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma1 and sigma2 receptors. Many compounds exhibited nanomolar affinity for sigma1 subtype receptor with good selectivity over sigma2. 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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