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Submit ReviewSKF 89976A hydrochloride
Description: Potent GAT-1 inhibitor; brain penetrant
Chemical Name: 1-(4,4-Diphenyl-3-butenyl)-3-piperidinecarboxylic acid hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for SKF 89976A hydrochloride
SKF 89976A hydrochloride is 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
Compound Libraries for SKF 89976A hydrochloride
SKF 89976A hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SKF 89976A hydrochloride
| M. Wt | 371.91 |
| Formula | C22H25NO2.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 85375-15-1 |
| PubChem ID | 6917797 |
| InChI Key | SNGGBKYQZVAQKA-UHFFFAOYSA-N |
| Smiles | Cl[H].OC(=O)C1CCCN(CC\C=C(\C2=CC=CC=C2)C2=CC=CC=C2)C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SKF 89976A hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 with gentle warming | ||
| DMSO | 37.19 | 100 |
Preparing Stock Solutions for SKF 89976A hydrochloride
The following data is based on the product molecular weight 371.91. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.69 mL | 13.44 mL | 26.89 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for SKF 89976A hydrochloride
References for SKF 89976A hydrochloride
References are publications that support the biological activity of the product.
Ali et al (1985) Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem. 28 653 PMID: 2985785
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
If you know of a relevant reference for SKF 89976A hydrochloride, please let us know.
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1 Citation for SKF 89976A hydrochloride
Citations are publications that use Tocris products. Selected citations for SKF 89976A hydrochloride include:
Sousa et al (2011) Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration: implications for the effects of δ9-tetrahydrocannabinol on spatial memory. Neuropsychopharmacology 36 472 PMID: 20927050
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.