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Rotigotine-

Catalog No. T6647 CAS 99755-59-6

Synonyms: Neupro, N-0923, N-0437, SPM 962

Rotigotine 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.

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Rotigotine-, CAS 99755-59-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 71.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 268.00
100 mg	In stock	$ 397.00
200 mg	In stock	$ 582.00
500 mg	In stock	$ 913.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.76%

Purity: 99.59%

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Description	Rotigotine 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.
Targets&IC50	D 2 Receptor:4-15 nM (Ki), D 5 Receptor:4-15 nM (Ki), 5-HT 1A Receptor:30 nM (Ki), D 3 Receptor:0.71 nM (Ki), D 4 Receptor:4-15 nM (Ki), D 1 Receptor:83 nM (Ki), 5-HT 7 Receptor:86 nM (Ki)
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.
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.

Synonyms	Neupro, N-0923, N-0437, SPM 962
Molecular Weight	315.47
Formula	C19H25NOS
CAS No.	99755-59-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 59 mg/mL (187 mM)

Ethanol: 59 mg/mL (187 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35. 2. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. 3. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91. 4. Radad K, Scheller D, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP⁺ and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86.

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Keywords

Rotigotine- 99755-59-6 GPCR/G Protein Neuroscience 5-HT Receptor Dopamine Receptor Adrenergic Receptor Rotigotine dopamine 5-HT1A Neupro receptor N0923 Serotonin Receptor N-0923 N 0923 Beta Receptor 5-hydroxytryptamine Receptor N0437 N-0437 α2B-adrenergic Inhibitor N 0437 inhibit SPM 962 inhibitor

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