Biological descriptionA potent GABA uptake inhibitor, highly selective for GAT-1 (IC50 values are 0.13 (hGAT-1), 550 ( rGAT-2), 944 ( hGAT-3) and 7210 μM (hBGT-1)). Brain penetrant, orally active and anticovulsant in vivo.
Also available in simple stock solutions (ab146705) - add 1 ml of water to get an exact, ready-to-use concentration.
Chemical name1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
Storage instructionsShipped at Room Temperature. Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in water to 100 mM and in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Krause S & Schwarz W Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol Pharmacol68:1728-35 (2005).
Read more (PubMed: 16150932) »
Borden LA et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol269:219-24 (1994).
Read more (PubMed: 7851497) »
Swinyard EA et al. Anticonvulsant profiles of the potent and orally active GABA uptake inhibitors SK&F 89976-A and SK&F 100330-A and four prototype antiepileptic drugs in mice and rats. Epilepsia32:569-77 (0).
Read more (PubMed: 1831122) »