Oxo-bridged isomers of aza-trishomocubane sigma (σ) receptor ligands: synthesis, in vitro binding, and molecular modeling

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Banister, Samuel D
Moussa, Iman A
Jordan, Meredith JT
Coster, Mark J
Kassiou, Michael
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2010
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Abstract

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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Bioorganic & Medicinal Chemistry Letters

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20

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1

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Medicinal and biomolecular chemistry

Biologically active molecules

Organic chemistry

Pharmacology and pharmaceutical sciences

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