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    Rotigotine (N-0437; N-0923)
    Rotigotine (N-0437; N-0923)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1253
    CAS #: 99755-59-6Purity ≥98%

    Description: Rotigotine (N-0437; N-0923) is a potent, non-selective and dopamine receptor full agonist, used in the treatment of Parkinson's disease and restless legs syndrome. Rotigotine is dopamine D2 and D3 receptor agonist with Ki values of 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors.

    References: Curr Med Res Opin. 2016;32(1):77-85.

    Related CAS #: 99755-59-6 (free base)   125572-93-2 (HCl) 

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    Molecular Weight (MW)315.47
    FormulaC19H25NOS 
    CAS No.99755-59-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 63 mg/mL (199.7 mM)
    Water: <1 mg/mL
    Ethanol: 63 mg/mL (199.7 mM)
    Other info

    Chemical Name: (S)-6-(propyl(2-(thiophen-2-yl)ethyl)amino)-5,6,7,8-tetrahydronaphthalen-1-ol

    InChi Key: KFQYTPMOWPVWEJ-INIZCTEOSA-N

    InChi Code: InChI=1S/C19H25NOS/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21/h3-7,13,16,21H,2,8-12,14H2,1H3/t16-/m0/s1

    SMILES Code: OC1=C2CC[[email protected]@H](CC2=CC=C1)N(CCC)CCC3=CC=CS3           

    Synonyms N0923, N-0923, N 0923


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    In Vitro

    In vitro activity: Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors. Rotigotine exhibits antiparkinsonian acitivity.


    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 VivoIn primed rats, Rotigotine (N-0437; N-0923; 0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.
    Animal modelRats
    Formulation & DosageTwo weeks after the 6-OHDA lesions, rats are primed with apomorphine (0.5 mg/kg s.c.). Rats showing less than 150 contralateral rotations during the 1 h testing period are excluded from the study. Three days after priming, rats are divided into different experimental groups and treated with different doses of the dopamine receptor agonists (Rotigotine or pramipexole) alone or in combination with dopamine D1 (SCH 39166) or D2 (eticlopride) receptor antagonists as reported: saline+Rotigotine (0.035 mg/kg s.c., n=9; 0.1 mg/kg s.c., n=9; 0.35 mg/kg s.c., n=8); SCH 39166 (0.1 mg/kg s.c.)+Rotigotine (0.035 mg/kg s.c., n=5; 0.1 mg/kg s.c., n=7; 0.35 mg/kg s.c., n=5); eticlopride (0.1 mg/kg s.c.) + Rotigotine (0.1 mg/kg s.c., n=5; 0.35 mg/kg s.c., n=5); Saline+pramipexole (0.035 mg/kg s.c., n=5; 0.1 mg/kg s.c., n=12; 0.35 mg/kg s.c., n=7); SCH 39166 (0.1 mg/kg s.c.)+pramipexole (0.035 mg/kg s.c., n=5; 0.1 mg/kg s.c., n=6; 0.35 mg/kg s.c., n=6); eticlopride (0.1 mg/kg s.c.)+pramipexole (0.1 mg/kg s.c., n=7; 0.35 mg/kg s.c., n=5).
    References

    [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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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    Changes of RBDQ-HK individual items before and after stable rotigotine treatment. J Clin Sleep Med. 2016 Oct 15; 12(10): 1403–1409.
     

    An external file that holds a picture, illustration, etc.
Object name is ijn-11-6547Fig7.jpg

    In vivo and ex vivo fluorescence images of organs of mice. Int J Nanomedicine. 2016; 11: 6547–6559.
     

    Rotigotine

    In vitro release studies of rotigotine from free rotigotine, rotigotine NPs and rotigotine Lf-NPs.



    Rotigotine
    In vitro cytotoxicity of free rotigotine, rotigotine NPs and rotigotine Lf-NPs. Int J Nanomedicine. 2016; 11: 6547–6559.


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