TY - JOUR
T1 - Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor
AU - Shonberg, Jeremy
AU - Lane, Jonathan Robert David
AU - Scammells, Peter John
AU - Capuano, Benvenuto
PY - 2013
Y1 - 2013
N2 - 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.
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.
UR - http://pubs.rsc.org.ezproxy.lib.monash.edu.au/en/Content/ArticleLanding/2013/MD/c3md00154g#!divAbstract
U2 - 10.1039/c3md00154g
DO - 10.1039/c3md00154g
M3 - Article
VL - 4
SP - 1290
EP - 1296
JO - RSC Medicinal Chemistry
JF - RSC Medicinal Chemistry
SN - 2632-8682
IS - 9
ER -