Oxo-bridged isomers of aza-trishomocubane sigma (σ) receptor ligands: synthesis, in vitro binding, and molecular modeling
Author(s)
Banister, Samuel D
Moussa, Iman A
Jordan, Meredith JT
Coster, Mark J
Kassiou, Michael
Griffith University Author(s)
Year published
2010
Metadata
Show full item recordAbstract
Isomeric oxo-bridged analogs of aza-trishomocubane sigma (s) receptor ligands were synthesized and shown to display a reduced affinity for the s receptor. In the case of phenethyl derivative 4, there was a concomitant introduction of high-affinity for the a2C adrenergic receptor, and moderate affinity for the dopamine transporter. Molecular modeling was undertaken to rationalize these results.Isomeric oxo-bridged analogs of aza-trishomocubane sigma (s) receptor ligands were synthesized and shown to display a reduced affinity for the s receptor. In the case of phenethyl derivative 4, there was a concomitant introduction of high-affinity for the a2C adrenergic receptor, and moderate affinity for the dopamine transporter. Molecular modeling was undertaken to rationalize these results.
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Journal Title
Bioorganic & Medicinal Chemistry Letters
Volume
20
Issue
1
Subject
Medicinal and biomolecular chemistry
Biologically active molecules
Organic chemistry
Pharmacology and pharmaceutical sciences