Ropinirole-d₁₄ hydrochloride  (Synonyms: SKF 101468-d₁₄ hydrochloride)

Ropinirole-d₁₄ hydrochloride is deuterated labeled Ropinirole hydrochloride (HY-B0623A). Ropinirole (SKF 101468) hydrochloride is an orally active, potent D₃/D₂ receptor agonist with a K_i of 29 nM for D₂ receptor. Ropinirole hydrochloride has pEC₅₀s of 7.4, 8.4 and 6.8 for hD₂, hD₃ and hD₄ receptors, respectively. Ropinirole hydrochloride has no affinity for the D₁ receptors. Ropinirole hydrochloride has the potential for Parkinson's disease^[1][2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Ropinirole hydrochloride has affinity for D₃ receptors of 10-20 fold higher than the D₂ and D₄ receptors. Ropinirole hydrochloride is weakly active at alpha 2-adrenoceptors and 5-HT₂ receptors but inactive at 5-HT₁, benzodiazepine and gamma-aminobutyric acid receptors or alpha 1 and beta-adrenoceptors^[2][3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ropinirole (0.1-10 mg/kg; i.p.) decreases intracranial self-stimulation (ICSS) thresholds and induces anxiolytic- and antidepressive-like effects without affecting motor activity or spatial memory^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

310.92

C₁₆H₁₁D₁₄ClN₂O

1276197-10-4

91374-20-8

[2H]C([2H])([2H])C([2H])([2H])C([2H])([2H])N(C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])CCC1=C2C(NC(C2)=O)=CC=C1.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Mavrikaki M, et al. Ropinirole regulates emotionality and neuronal activity markers in the limbic forebrain. Int J Neuropsychopharmacol. 2014 Dec;17(12):1981-93.  [Content Brief]

  [3]. Eden, R.J., et al., Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav, 1991. 38(1): p. 147-54.  [Content Brief]