Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372442 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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
Authors
Samuel D. Banister, Iman A. Moussa, Meredith J.T. Jordan, Mark J. Coster, Michael Kassiou,