Tiagabine-d₄ hydrochloride  (Synonyms: NO050328-dd₄ hydrochloride; NO328-d₄ hydrochloride; TGB-d₄ hydrochloride)

Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC₅₀s of 67, 446 and 182 nM for [³H]GABA uptake in Synaptosomes, Neurons and Glia, respectively^[1].

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.

416.03

C₂₀H₂₂D₄ClNO₂S₂

O=C(C1C([2H])N(CC/C=C(C2=C(C)C=CS2)/C3=C(C)C=CS3)C([2H])C([2H])C1[2H])O.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]. Braestrup C, et al. (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier. J Neurochem. 1990 Feb;54(2):639-47.  [Content Brief]

  [3]. Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40.  [Content Brief]

  [4]. Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70.  [Content Brief]