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Issue 9, 2013
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Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor

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Abstract

Bivalent ligands represent useful tools to investigate the phenomenon of GPCR dimerization. We synthesized bivalent ligands based on (R)-apomorphine with variations in spacer length, and assessed these compounds in functional and binding assays at the dopamine D2 receptor. The results present novel SAR for bivalent ligands targeting the D2R, and identify a relationship for spacer length with ligand potency, efficacy and affinity.

Graphical abstract: Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor

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Article information


Submitted
03 Jun 2013
Accepted
16 Jul 2013
First published
18 Jul 2013

Med. Chem. Commun., 2013,4, 1290-1296
Article type
Concise Article

Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor

J. Shonberg, J. R. Lane, P. J. Scammells and B. Capuano, Med. Chem. Commun., 2013, 4, 1290
DOI: 10.1039/C3MD00154G

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