| Identification | Back Directory | [Name]
[2H5]-Tiagabine hydrochloride | [CAS]
1253297-72-1 | [Synonyms]
Tiagabine-[d5] hydrochloride
Tiagabine hydrochloride salt
[2H5]-Tiagabine hydrochloride | [Molecular Formula]
C20H20D5NO2S2.ClH | [MOL File]
1253297-72-1.mol | [Molecular Weight]
417.04 |
| Hazard Information | Back Directory | [Uses]
Tiagabine-d5 (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). 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][2]. | [References]
[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. DOI:10.1177/1060028018797110
[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. DOI:10.1111/j.1471-4159.1990.tb01919.x
[3] Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40. PMID:18007567
[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. DOI:10.1016/j.neuint.2006.09.004 |
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