SKF 89976A hydrochloride

Cat. No. 1081

SKF 89976A hydrochloride C22H25NO2.HCl [85375-15-1]

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Chemical Name: 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride

Biological Activity

A 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 Information

Sold with the permission of GlaxoSmithKline

Technical Data

M.Wt:
371.91
Formula:
C22H25NO2.HCl
Solubility:
Soluble to 100 mM in water with gentle warming and to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
85375-15-1

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 / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

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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