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

7 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

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