5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐

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 (pEC ₅₀ respectively: 9.0, 9.4-8.6, 9.7). 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. .