| Name | Rotigotine- |
| Description | 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. |
| Kinase Assay | 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. |
| In vitro | The selectivity of Rotigotine for D3 (pKi 9.2) receptors is higher 10-fold than D2/D4/D5 (pKi 8.5-8.0) and 100-fold than D1 receptors (pKi 7.2). Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. In functional studies, Rotigotine behaves as a full agonist at all dopamine receptors but notably, the potency for stimulation of D1 receptors is similar to that for D2/D3 receptors (pEC50 respectively: 9.0, 9.4-8.6, 9.7). 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. |
| In vivo | In primed rats, Rotigotine (0.035/0.1/0.35 mg/kg) dose-dependently induces contralateral turning behavior. In drug-naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 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.
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| Keywords | α2B-adrenergic | SPM-962 | SPM962 | Serotonin Receptor | Rotigotine- | Rotigotine | receptor | N0923 | N0437 | N 0923 | N 0437 | Inhibitor | inhibit | DopamineReceptor | Dopamine Receptor | dopamine | D3 | D2 | Beta Receptor | AdrenergicReceptor | Adrenergic Receptor | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT1A | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Dapoxetine hydrochloride | Cefaclor monohydrate | Hexamethonium Bromide | Octopamine hydrochloride | 1,8-Cineole | L-DOPA | Isoprenaline hydrochloride | Creatine | D-Mannitol | Mianserin hydrochloride | Cinchonidine |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | GPCR Compound Library | Anti-Cancer Drug Library |
United States
