Oxo-bridged isomers of aza-trishomocubane sigma (σ) receptor ligands: synthesis, in vitro binding, and molecular modeling
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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.
Bioorganic & Medicinal Chemistry Letters
Biologically Active Molecules