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

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.

罗替戈汀, SPM 962, Neupro, N-0923, N-0437

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 250 mg/mL (792.47 mM), Sonication is recommended.

Ethanol: 59 mg/mL (187.02 mM), Sonication is recommended.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.34 mM), Sonication is recommended.