Tiagabine hydrochloride | GABA transporter 1 (GAT1) inhibitor

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 to at 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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO, ethanol, or distilled water may be stored at -20° for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
10 mg$35.00
50 mg$125.00

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

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 to at 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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO, ethanol, or distilled water may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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