Article ID Journal Published Year Pages File Type
1372442 Bioorganic & Medicinal Chemistry Letters 2010 4 Pages PDF
Abstract

Isomeric oxo-bridged analogs of aza-trishomocubane sigma (σ) receptor ligands were synthesized and shown to display a reduced affinity for the σ receptor. In the case of phenethyl derivative 4, there was a concomitant introduction of high-affinity for the α2C adrenergic receptor, and moderate affinity for the dopamine transporter. Molecular modeling was undertaken to rationalize these results.

Graphical abstractThe in vitro σ receptor affinity of aza-trishomocubyl hemiaminals, and their isomeric oxo-bridged analogues, is rationalized using molecular modeling.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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