(Rac)-Rotigotine

(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor. IC50 & Target:Ki: Dopamine receptor; 5-HT receptor^[1][2] In Vitro: Rotigotine has a 10-fold selectivity for D3 (pK_i=9.2) receptors compared with D2, D4 and D5 (pK_i=8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK_i=7.2). 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].
.