Product Description: Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter with a Ki of ∼0.1 μM. Tiagabine hydrochloride potently and selectively inhibits GABA reuptake with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in synaptosomes, neurons and glia, respectively. Tiagabine hydrochloride has neuroprotective properties[1][2][3][4][5][6][7][8].
Applications: Neuroscience-Neuromodulation
Formula: C20H26ClNO2S2
References: [1]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. /[2]Henjum S, Hassel B. High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int. 2007 Jan;50(2):365-70. /[3]Sheehan DV, Sheehan KH, Raj BA, Janavs J. An open-label study of tiagabine in panic disorder. Psychopharmacol Bull. 2007;40(3):32-40./[4]Masuda N, Peng Q, Li Q, Jiang M, Liang Y, Wang X, Zhao M, Wang W, Ross CA, Duan W. Tiagabine is neuroprotective in the N171-82Q and R6/2 mouse models of Huntington's disease. Neurobiol Dis. 2008 Jun;30(3):293-302./[5]Liu J, Huang D, Xu J, Tong J, Wang Z, Huang L, Yang Y, Bai X, Wang P, Suo H, Ma Y, Yu M, Fei J, Huang F. Tiagabine Protects Dopaminergic Neurons against Neurotoxins by Inhibiting Microglial Activation. Sci Rep. 2015 Oct 26;5:15720./[6]Sindelar M, Lutz TA, Petrera M, Wanner KT. Focused pseudostatic hydrazone libraries screened by mass spectrometry binding assay: optimizing affinities toward γ-aminobutyric acid transporter 1. J Med Chem. 2013 Feb 14;56(3):1323-40./[7]Giardina W J, Decker M W, Porsolt R D, et al. An evaluation of the GABA uptake blocker tiagabine in animal models of neuropathic and nociceptive pain. Drug development research, 1998, 44(2-3): 106-113./[8]Javaid S, Alqahtani F, Ashraf W, Anjum SMM, Rasool MF, Ahmad T, Alasmari F, Alasmari AF, Alqarni SA, Imran I. Tiagabine suppresses pentylenetetrazole-induced seizures in mice and improves behavioral and cognitive parameters by modulating BDNF/TrkB expression and neuroinflammatory markers. Biomed Pharmacother. 2023 Apr;160:114406.
CAS Number: 145821-59-6
Molecular Weight: 412.01
Compound Purity: 99.44
Research Area: Neurological Disease
Solubility: DMSO : ≥ 53 mg/mL/H2O : 100 mg/mL (ultrasonic)
Target: GABA Receptor;Trk Receptor
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