Rotigotine

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM); has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor; behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50) in functional assay; also demonstrates significant affinity at α-adrenergic (α2B, Ki=27 nM) and serotonin receptors (5-HT1A Ki=30 nM); significantly attenuates MPTP-induced acute cell degeneration in mouse model.Parkinson's Disease Approved(In Vitro):Rotigotine (0.01-10 μM) slightly protects dopaminergic neurons against MPP+ toxicity dopamine, protects dopaminergic neurons against rotenone-induced cell death and significantly inhibits ROS production by rotenone.(In Vivo):Rotigotine (0.1-5 mg/kg; i.h.; for 14 days; male Sprague–Dawley rats) has antidepressant effect.