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

Jeremy Shonberg, Jonathan Robert David Lane, Peter John Scammells, Benvenuto Capuano

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

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 D-2 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.
Original languageEnglish
Pages (from-to)1290 - 1296
Number of pages7
JournalMedChemComm
Volume4
Issue number9
DOIs
Publication statusPublished - 2013

Cite this

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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 D-2 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.",
author = "Jeremy Shonberg and Lane, {Jonathan Robert David} and Scammells, {Peter John} and Benvenuto Capuano",
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Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor. / Shonberg, Jeremy; Lane, Jonathan Robert David; Scammells, Peter John; Capuano, Benvenuto.

In: MedChemComm, Vol. 4, No. 9, 2013, p. 1290 - 1296.

Research output: Contribution to journalArticleResearchpeer-review

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AU - Shonberg, Jeremy

AU - Lane, Jonathan Robert David

AU - Scammells, Peter John

AU - Capuano, Benvenuto

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AB - 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 D-2 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.

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SP - 1290

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JO - MedChemComm

JF - MedChemComm

SN - 2040-2503

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