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Rotigotine

Cat. No. M3675
Rotigotine Structure
Size Price Availability
10mg USD 80 4-7 Days
50mg USD 280 4-7 Days
100mg USD 400 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Rotigotine is a nonergoline dopamine receptor agonist with structural similarity to dopamine. Rotigotine binds to the D1 through D5 dopamine receptors, having several times more affinity than dopamine does to the D2 and D3 receptors. Rotigotine's high lipid solubility and extended duration of action when applied to the skin in experimental models of PD suggested that rotigotine was a candidate for transdermal application.Randomized clinical studies also have demonstrated the efficacy of rotigotine in improving the symptoms of moderate-to-severe primary RLS.Rotigotine provides minor protection against MPP⁺ and rescues a significant number of THir neurons against rotenone in primary mesencephalic cell cultures relevant to PD.

Protocol
Cell Experiment
Cell lines primary mesencephalic cell
Preparation method To investigate the effect of rotigotine (UCB, Belgium) on the survival of THir neurons, primary mesencephalic cell cultures were treated with different concentrations of rotigotine (0.01, 0.1, 1 and 10 µM) from the 6th DIV for 8 consecutive days. Rotigotine was added with each change of the culture medium every second day from a fresh stock solution (10 mM) prepared in DMSO (0.1% final concentration). To investigate the effect of rotigotine against MPP+ or rotenone-induced cell death, rotigotine was added from the 6th DIV until the 14th DIV as described above and MPP+ (10 µM) or rotenone (20 nM) were co-administered on the 12th DIV for 48 h.
Concentrations 0.01, 0.1, 1 and 10 μM
Incubation time 48 h
Animal Experiment
Animal models Sprague-Dawley rats
Formulation 1:10 ratio of dimethyl sulfoxide (DMSO) and 5% dextrose
Dosages 0.5 or 3 mg/kg
Administration s.c.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 315.47
Formula C19H25NOS
CAS Number 99755-59-6
Purity >99%
Solubility DMSO
Storage at -20°C
References

Rotigotine transdermal system: developing continuous dopaminergic delivery to treat Parkinson's disease and restless legs syndrome.
Benitez A, et al. Ann N Y Acad Sci. 2014 Aug 21. PMID: 25145951.

Neuroprotective effect of rotigotine against complex I inhibitors, MPP⁺ and rotenone, in primary mesencephalic cell culture.
Radad K, et al. Folia Neuropathol. 2014;52(2):179-86. PMID: 25118903.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Rotigotine supplier, Dopamine Receptor, inhibitors

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