Rotigotine-

SKU: orb1300587

Description

Rotigotine (N-0923) is a non-ergot dopamine agonist used to treat Parkinson's disease and restless legs syndrome via a transdermal patch. It is employed in neuroscience research to study dopaminergic pathways in both in vitro receptor binding assays and in vivo models of movement disorders, with no significant association with drug-induced liver injury.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 99755-59-6
• MW: 315.47
• Purity: 99.76% (May vary between batches)
• Formula: C₁₉H₂₅NOS
• SMILES: OC1=C2C(C[C@@H](N(CCC3=CC=CS3)CCC)CC2)=CC=C1
• Target: Dopamine Receptor,Adrenergic Receptor,5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.34 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:75 mg/mL (237.74 mM);Ethanol:59 mg/mL (187.02 mM)

Bioactivity

• Target IC50:
  D1 receptor:83 nM (Ki)|D3 receptor:0.71 nM (Ki)|5-HT7 receptor:86 nM (Ki)|D2 receptor:4-15 nM (Ki)|D5 receptor:4-15 nM (Ki)|5-HT1A receptor:30 nM (Ki)|D4 receptor:4-15 nM (Ki)
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-HT1A, 5-HT Receptor, AdrenergicReceptor, Adrenergic Receptor, 5HTReceptor, 5-hydroxytryptamine Receptor, 5HT Receptor, D2, D3, dopamine, Dopamine, Dopamine Receptor, DopamineReceptor, Beta Receptor, Inhibitor, N 0437, N 0923, inhibit, N0437, N-0437, N0923, N-0923, Neupro, α2B-adrenergic, Rotigotine, Rotigotine-, SPM 962, SPM962, SPM-962, Serotonin Receptor, receptor

Compound Identifiers

PubChem CID

59227