Dopamine D3 receptor biased agonist
Dopamine D3 receptor biased agonist. Preferentially signals via the G protein-dependent pathway (EC50 values for G protein and β-arrestin-dependent signaling are 1.1 and 50.2 μM, respectively). Exhibits selectivity for D3 over D2 receptors. Improves motor deficits in rodent Parkinson's disease models and ameliorates L-DOPA induced abnormal involuntary movements.
Xu et al (2017) Functional characterization of a novel series of biased signaling dopamine D3 receptor agonists. ACS Chem.Neurosci. 8 486 PMID:27801563 |Simms et al (2016) In vivo characterization of a novel dopamine D3 receptor agonist to treat motor symptoms of Parkinson's disease. Neuropharmacology 100 106 PMID:25896768
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