|Related Categories||Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cephalon,|
|optical activity||[α]/D -8.5 to 10°, c = 1 in H2O|
|color||white to tan|
|solubility||H2O: ≥14 mg/mL|
Tiagabine hydrochloride was used to study serotoninergic transmission in G1 cells.1
Tiagabine hydrochloride is an anticonvulsant and selective GABA reuptake inhibitor through inhibition of the synaptic GABA transporter GAT1.
Tiagabine increases the synaptic GABA and enhances the neuronal inhibition. It is effective as adjunctive treatment of epilepsy and anxiety disorders.
Fast synaptic transmission requires a mechanism for rapid removal of transmitter molecules from the synaptic cleft, a task most often accomplished by transmitter clearance or degradation. High affini...
1. A novel compound N(1),N(5)-(Z)-N(10)-(E)-tri-p-coumaroylspermidine isolated from Carthamus tinctorius L. and acting by serotonin transporter inhibition. Zhao G, Gai Y, Chu WJ, et al. Eur. Neuropsychopharmacol. 19(10), 749-58, (2009)
The selective GAT inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABAA receptor agonist gaboxadol Madsen, K.K., et al. J. Pharmacol. Exp. Ther., (2011)
Pregabalin effect on steady-state pharmacokinetics of carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate, valproate, and tiagabine. Bockbrader, H.N., et al. Epilepsia 52, 405-409, (2011)
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