Loreclezole |
| Catalog No.GC14045 |
Loreclezole is a sedative and anticonvulsant drug that acts as a positive allosteric modulator of GABAA receptors, selectively stimulating receptors containing β2 or β3 subunits.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 117857-45-1
Sample solution is provided at 25 µL, 10mM.
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Loreclezole is a sedative and anticonvulsant drug that acts as a positive allosteric modulator of GABAA receptors, selectively stimulating receptors containing β2 or β3 subunits[1]. Loreclezole is also an effective negative modulator of ρ1 GABAC receptors, with an IC50 of 0.5µM[2].
In vitro, Loreclezole (3-30µM) treatment of L929 fibroblasts increased the apparent desensitization degree and rate of whole-cell currents in a concentration-dependent manner at concentrations above 6µM. This effect is voltage-independent and is enhanced with increasing GABA concentrations[3].
In vivo, Loreclezole (5 mg/kg) administered intraperitoneally in amygdala-kindled epilepsy model rats significantly reduced seizure occurrences and afterdischarge duration[4]. In Lister Hooded rats, Loreclezole (0, 25, 50, or 75 mg/kg) dose-dependently increased the seizure threshold[5]. Loreclezole (50 mg/kg) administered orally in β2N265S transgenic mice did not show significant protective effects against pentylenetetrazol (PTZ)-induced seizures[6].
References:
[1] Wingrove P B, Wafford K A, Bain C, et al. The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit[J]. Proceedings of the National Academy of Sciences, 1994, 91(10): 4569-4573.
[2] Johnston G A R. Medicinal chemistry and molecular pharmacology of GABA-C receptors[J]. Current topics in medicinal chemistry, 2002, 2(8): 903-913.
[3] Donnelly J L, Macdonald R L. Loreclezole enhances apparent desensitization of recombinant GABAA receptor currents[J]. Neuropharmacology, 1996, 35(9-10): 1233-1241.
[4] Borowicz K K, Sawiniec A, Czuczwar S J. Interaction of loreclezole with conventional antiepileptic drugs in amygdala-kindled rats[J]. European neuropsychopharmacology, 2004, 14(3): 251-257.
[5] Green A R, Misra A, Murray T K, et al. A behavioural and neurochemical study in rats of the pharmacology of loreclezole, a novel allosteric modulator of the GABAA receptor[J]. Neuropharmacology, 1996, 35(9-10): 1243-1250.
[6]Groves J O, Guscott M R, Hallett D J, et al. The role of GABAAβ2 subunit‐containing receptors in mediating the anticonvulsant and sedative effects of loreclezole[J]. European Journal of Neuroscience, 2006, 24(1): 167-174.
Cell experiment [1]: | |
Cell lines | L929 fibroblasts |
Preparation method | Dissolve Loreclezole in 100% DMSO and add to the external solution at concentrations 3-30µM. Currents were recorded with an EPC-7 or an Axopatch 1-B patch clamp amplifier, recorded on hard disk using the Axotape Program and stored on VHS or Beta tape. |
Reaction Conditions | 3-30µM |
Applications | Loreclezole at concentrations above 6μM, enhanced the degree and rate of apparent desensitization of the whole-cell current in a concentration-dependent manner. |
Animal experiment [2]: | |
Animal models | Amygdala-kindled rats |
Preparation method | Loreclezole(5mg/kg), diphenylhydantoin and clonazepam were suspended in 1% Tween 80 solution. All drugs were administered intraperitoneally. |
Dosage form | 5mg/kg; i.p. |
Applications | Loreclezole administered at 5mg/kg, significantly diminished seizure and after discharge durations in amygdala-kindled rats. |
References: | |
| Cas No. | 117857-45-1 | SDF | |
| Chemical Name | (E)-1-(2-chloro-2-(2,4-dichlorophenyl)vinyl)-1H-1,2,4-triazole hydrochloride | ||
| Canonical SMILES | Cl/C(C(C(Cl)=C1)=CC=C1Cl)=C/N2N=CN=C2.Cl | ||
| Formula | C10H6Cl3N3 | M.Wt | 274.53 |
| Solubility | >30mg/ml in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6426 mL | 18.2129 mL | 36.4259 mL |
| 5 mM | 728.5 μL | 3.6426 mL | 7.2852 mL |
| 10 mM | 364.3 μL | 1.8213 mL | 3.6426 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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