Sumatriptan-d₅  (Synonyms: GR 43175 free base-d₅)

Sumatriptan-d₅ is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research^[1][2][3][4].

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].

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

Sumatriptan (600 μg/kg, i.p. or 0.06 μg in 5 μL, i.t.) reverses nitroglycerin-induced thermal hypersensitivity in mice^[5].

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

300.43

C₁₄H₁₆D₅N₃O₂S

103628-46-2

O=S(C([2H])([2H])C1=CC2=C(NC=C2CCN(C([2H])([2H])[2H])C)C=C1)(NC)=O

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]. K L Dechant, et al. Sumatriptan. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the acute treatment of migraine and cluster headache. Drugs. 1992 May;43(5):776-98.  [Content Brief]

  [3]. Razzaque Z, et al. Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol. 1999 Jan;47(1):75-82.  [Content Brief]

  [4]. S J Peroutka, et al. Sumatriptan (GR 43175) interacts selectively with 5-HT1B and 5-HT1D binding sites. Eur J Pharmacol. 1989 Apr 12;163(1):133-6.  [Content Brief]

  [5]. Bates EA, et al. Sumatriptan alleviates nitroglycerin-induced mechanical and thermal allodynia in mice. Cephalalgia. 2010 Feb;30(2):170-8.  [Content Brief]