Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.

D5 receptor:4-15 nM (Ki), D2 receptor:4-15 nM (Ki), 5-HT1A receptor:30 nM (Ki), D3 receptor:0.71 nM (Ki), D4 receptor:4-15 nM (Ki), D1 receptor:83 nM (Ki), 5-HT7 receptor:86 nM (Ki)

Rotigotine对D3 (pKi 9.2) 受体的选择性是D2/D4/D5 (pKi 8.5-8.0) 的10倍高，而对D1受体 (pKi 7.2) 则高出100倍。在原代中脑细胞培养中，Rotigotine (10 μM) 使THir神经元数量减少了40%。在功能性研究中，Rotigotine作为所有多巴胺受体的全效激动剂，但值得注意的是，其对D1受体的激活效力与对D2/D3受体相似 (pEC50 分别为：9.0, 9.4-8.6, 9.7)。Rotigotine (0.01 μM) 轻微保护多巴胺神经元免受MPP+毒性的影响，显著保护多巴胺神经元免受罗腾隆引起的细胞死亡，并显著抑制罗腾隆诱导的ROS产生。

在经过预处理的大鼠中，Rotigotine（0.035/0.1/0.35 mg/kg）以剂量依赖的方式诱导对侧转向行为。相比之下，在未经药物处理的大鼠中，无论是单独使用Rotigotine还是与SCH 39166合用，所诱导的转向行为均较预处理的大鼠减少。

Binding assays are performed in 96-well polypropylene tubes in a final volume of 2?mL for D1 and D4 membranes and 1?mL for D2, D3 and D5 membranes containing: 50?μL radioligand, 10?μL drug/buffer/non-specific binding, buffer (final concentration 50?mM Tris-HCl pH 7.4, MgCl2 2?mM) and membranes (5?μg protein for D2 and D3 and 25?μg protein for D1 and D5). Following 120?min of incubation at 25°C, bound radioligand is determined by rapid vacuum filtration through A/C glass fibre filters presoaked in 0.1% polyethylenimine. The filters are washed four times with 2?mL ice-cold ishing buffer (Tris-HCl 50?mM, pH?7.4 at 4°C) and retained radioactivity is determined by liquid scintillation counting.