Rotigotine

SKU: orb1223463

Description

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM); has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor; behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50) in functional assay; also demonstrates significant affinity at α-adrenergic (α2B, Ki=27 nM) and serotonin receptors (5-HT1A Ki=30 nM); significantly attenuates MPTP-induced acute cell degeneration in mouse model.Parkinson's Disease Approved(In Vitro):Rotigotine (0.01-10 μM) slightly protects dopaminergic neurons against MPP+ toxicity dopamine, protects dopaminergic neurons against rotenone-induced cell death and significantly inhibits ROS production by rotenone.(In Vivo):Rotigotine (0.1-5 mg/kg; i.h.; for 14 days; male Sprague–Dawley rats) has antidepressant effect.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 99755-59-6
• MW: 315.4729
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₅NOS
• SMILES: CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O
• Target: Dopamine Receptor
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Rotigotine (0.1-5 mg/kg; i.h.; for 14 days; male Sprague–Dawley rats) has antidepressant effect. Animal model: Male Sprague–Dawley rats. Dosage: 0.1, 0.5, 1, and 5 mg/kg. Administration: Subcutaneous injection; for 14 days. Result: Had antidepressant effect at a dose of 1 mg/kg or less.
• In Vitro:
  Rotigotine (0.01-10 μM) slightly protects dopaminergic neurons against MPP+ toxicity dopamine, protects dopaminergic neurons against rotenone-induced cell death and significantly inhibits ROS production by rotenone.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

N-0923 | SPM 962

Quick Database Links

Gene Symbol

Dopamine Receptor