(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial the 5-HT1A receptor agonist.

D1 receptor:83 nM (Ki), 5-HT2B receptor:27 nM (Ki), 5-HT1A receptor:30 nM (Ki), D4 receptor:3.9-15 nM (Ki), D3 receptor:0.71 nM (Ki), D5 receptor:5.4 nM (Ki), D2 receptor:13.5 nM (Ki)

In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC50?respectively: 9.0, 9.4-8.6, 9.7)[1]. Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 μM) slightly protects dopaminergic neurons against MPP+?toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone[4]. .