SKF 89976A hydrochloride
Cat. No. 1081
Chemical Name: 1-(4,4-Diphenyl-3-butenyl)-3-piperi
Biological ActivityA potent GABA uptake inhibitor, selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo.
Licensing InformationSold with the permission of GlaxoSmithKline
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Krause and Schwarz (2005) Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol.Pharmacol. 68 1728. PMID: 16150932.
Murali Dha (1996) On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg.Med.Chem.Lett. 6 1535.
Ali et al (1985) Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem. 28 653. PMID: 2985785.
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