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Tiagabine hydrochloride | GABA transporter 1 (GAT1) inhibitor

Tiagabine (145821-59-6) is a clinically useful anticonvulsant.1 It is also used to treat anxiety/panic disorder2 and neuropathic pain3. Tiagabine inhibits GABA-reuptake (IC50 [3H]GABA uptake = 67 nM) via inhibiting GABA transporter 1(GAT1) blocking both neuronal and glial GABA re-uptake.4,5

References/Citations
1) Schacter (1999) A Review of the Antiepileptic Drug Tiagabine, Clin. Neuropharmacol. 22 312
2) Schwartz and Nihalani (2006) Tiagabine in anxiety disorders, Expert Opin. Pharmacother. 7 1977
3) Novak et al. (2001) Treatment of Painful Sensory Neuropathy With Tiagabine: A Pilot Study, Clin. Auton. Res. 11 357
4) Braestrup et al. (1990) (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. 54 639
5) Nielsen et al. (1991) Characterization of Tiagabine (NO-328), a New Potent and Selective GABA Uptake Inhibitor, Eur. J. Pharmacol. 196 257

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Catalog#  10-4384-0010

$35.00
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CAS:
145821-59-6
Catalog Number:
10-4384
Activity:
GABA transporter 1 (GAT1) inhibitor
Chemical Name:
(3R)-1-[4,4-Bis(3-methylthiophen-2-yl)but-3-enyl]piperidine-3-carboxylic acid
Alternate Name:
NO-328
Molecular Weight:
412.00
Molecular Formula:
C20H25NO2S2 • HCl
Solubility:
Soluble in DMSO (up toat least 25 mg/ml), in Ethanol (up to at least 25 mg/ml) or in Water (up to at least 30 mg/ml)
Physical Properties:
Off-white or beige solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO, ethanol, or distilled water may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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