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Submit ReviewLoreclezole hydrochloride
Description: Subtype-selective GABAA modulator
Chemical Name: (Z)-1-[2-Chloro-2-(2,4-dichlorophenyl)ethenyl]-1H-1,2,4-triazole hydrochloride
Purity: ≥99% (HPLC)
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 | 2227372-56-5 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 1.37 | 5 with gentle warming | |
| ethanol | 1.37 | 5 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 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 |
|---|---|---|---|
| 0.05 mM | 64.31 mL | 321.54 mL | 643.09 mL |
| 0.25 mM | 12.86 mL | 64.31 mL | 128.62 mL |
| 0.5 mM | 6.43 mL | 32.15 mL | 64.31 mL |
| 2.5 mM | 1.29 mL | 6.43 mL | 12.86 mL |
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References
References are publications that support the biological activity of the product.
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, Loreclezole hydrochloride supplier, Subtype-selective, GABAA, receptor, modulators, Receptors, positive, allosteric, PAM, 117857-45-1, 1295, Tocris Bioscience
2 Citations for Loreclezole hydrochloride
Citations are publications that use Tocris products. Selected citations for Loreclezole hydrochloride include:
Lemos et al (2011) Stress-hyperresponsive WKY rats demonstrate depressed dorsal raphe neuronal excitability and dysregulated CRF-mediated responses. Neuropsychopharmacology 36 721 PMID: 21160465
Kotak et al (2008) Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex. Mol Med 18 2098 PMID: 18222937
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