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Submit ReviewCI 966 hydrochloride
Description: Selective inhibitor of GAT-1
Chemical Name: 1-[2-[bis[4-(Trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for CI 966 hydrochloride
CI 966 hydrochloride is a selective inhibitor of the GABA transporter GAT-1 (IC50 values are 0.26 and 1.2 μM at cloned human and rat GAT-1 respectively). Displays over 200-fold selectivity over GAT-2 and GAT-3. Centrally active upon systemic administration in vivo. Anticonvulsive and neuroprotective.
Compound Libraries for CI 966 hydrochloride
CI 966 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CI 966 hydrochloride
| M. Wt | 509.87 |
| Formula | C23H21F6NO3.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 110283-66-4 |
| PubChem ID | 198692 |
| InChI Key | NUQWSOWKRTZJTO-UHFFFAOYSA-N |
| Smiles | Cl.OC(=O)C1=CCCN(CCOC(C2=CC=C(C=C2)C(F)(F)F)C2=CC=C(C=C2)C(F)(F)F)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 CI 966 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 10 | ||
| DMSO | 100 |
Preparing Stock Solutions for CI 966 hydrochloride
The following data is based on the product molecular weight 509.87. 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 | 1.96 mL | 9.81 mL | 19.61 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.92 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets for CI 966 hydrochloride
References for CI 966 hydrochloride
References are publications that support the biological activity of the product.
Borden et al (1994) Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur.J.Pharmacol. 269 219 PMID: 7851497
Ebert et al (1990) Systemic CI-966, a new gamma-aminobutyric acid uptake blocker, enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. Can.J.Physiol.Pharmacol. 68 1194 PMID: 2276082
Radulovic et al (1993) Pharmacokinetics, mass balance, and induction potential of novel GABA uptake inhibitor, CI-966 HCl, in laboratory animals. Pharm.Res. 10 1442 PMID: 8272405
If you know of a relevant reference for CI 966 hydrochloride, please let us know.
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Citations for CI 966 hydrochloride
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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!
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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.