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| | [2H5]-Tiagabine hydrochloride Basic information |
| Product Name: | [2H5]-Tiagabine hydrochloride | | Synonyms: | [2H5]-Tiagabine hydrochloride;Tiagabine-[d5] hydrochloride;Tiagabine hydrochloride salt;3-Piperidinecarboxylic acid, 1-[4,4-bis(3-methyl-2-thienyl)-3-buten-1-yl-1,1,2,2,3-d5]-, hydrochloride (1:1), (3R)-;Tiagabine-[D5] Hydrochloride (Standard) | | CAS: | 1253297-72-1 | | MF: | C20H20D5NO2S2.ClH | | MW: | 417.04 | | EINECS: | | | Product Categories: | | | Mol File: | 1253297-72-1.mol | ![[2H5]-Tiagabine hydrochloride Structure](CAS/20240320/GIF/1253297-72-1.gif) |
| | [2H5]-Tiagabine hydrochloride Chemical Properties |
| Melting point | 182-185 °C(Solv: isopropanol (67-63-0)) |
| | [2H5]-Tiagabine hydrochloride Usage And Synthesis |
| 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 |
| | [2H5]-Tiagabine hydrochloride Preparation Products And Raw materials |
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