Loreclezole hydrochloride
Biological Activity
Subtype-selective GABAA receptor modulator. Acts as a positive allosteric modulator of β2 or β3-subunit containing receptors. Also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.
Technical Data
| M. Wt | 311 |
| Formula | C10H6Cl3N3.HCl |
| Storage | Desiccate at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 117857-45-1 |
| PubChem ID | 45073437 |
| InChI Key | AWKSVFLKVCVVFQ-MDZFRNKHSA-N |
| Smiles | Cl[H].Cl\C(=C/N1C=NC=N1)C1=C(Cl)C=C(Cl)C=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 1.37 | 5mM with gentle warming | |
| ethanol | 1.37 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 311. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 3.22 mL | 16.08 mL | 32.15 mL |
| 5 mM | 0.64 mL | 3.22 mL | 6.43 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.22 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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References
References are publications that support the products' biological activity.
Donnelly and Macdonald (1996) Loreclezole enhances apparent desensitisation of recombinant GABAA receptor currents. Neuropharmacology 35 1233 PMID: 9014138
Fisher et al (2000) Loreclezole inhibition of recombinant α1β1γ2L GABAA receptor single channel currents. Neuropharmacology 39 235 PMID: 10670419
Smith et al (2004) Compounds exhibiting selective efficacy for different β subunits of human recombinant γ-aminobutyric acidA receptors. J.Pharmacol.Exp.Ther. 311 601 PMID: 15210837
Thomet et al (2000) Loreclezole as a simple functional marker for homomeric ρ type GABAC receptors. Eur.J.Pharmacol. 408 R1 PMID: 11080529
If you know of a relevant reference for Loreclezole hydrochloride, please let us know.
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Keywords: Loreclezole hydrochloride, supplier, Subtype-selective, GABAA, receptor, modulators, Receptors, positive, allosteric, PAM, GABAA, Receptors, Tocris Bioscience
1 Citation for Loreclezole hydrochloride
Citations are publications that use Tocris products. Selected citations for Loreclezole hydrochloride include:
Kotak et al (2008) Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex. Mol Med 18 2098 PMID: 18222937
Do you know of a great paper that uses Loreclezole hydrochloride from Tocris? If so please let us know.
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