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Ropinirole is a potent dopamine D2 receptor agonist (Ki = 29 nM in a radioligand binding assay).1 It is selective for D2 over D1 dopamine receptors (Ki = >100,000 nM) as well as a panel of adrenergic, serotonin, benzodiazepine, and GABA receptors (IC50s = >9,000 nM). Ropinirole reduces spontaneous locomotor activity in mice at doses less than 50 mg/kg but increases it at a dose of 100 mg/kg. It also induces contralateral asymmetry in an open field test in 6-OHDA-lesioned mice. Ropinirole (0.01-1 mg/kg) reverses locomotor deficits and restores interest in novel stimuli in a marmoset model of Parkinson's disease induced by MPTP. Formulations containing ropinirole have been used for the treatment of Parkinson's disease motor dysfunction.
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1. Preclinical pharmacology of ropinirole (SK&F 101468-