Loreclezole

Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.

Product information

CAS Number: 117857-45-1

Molecular Weight: 274.53

Formula: C10H6Cl3N3

Synonym:

R 72063

Chemical Name: 1-[(Z)-2-chloro-2-(2,4-dichlorophenyl)ethenyl]-1H-1,2,4-triazole

Smiles: ClC1C=C(Cl)C=CC=1/C(/Cl)=C/N1C=NC=N1

InChiKey: XGLHZTBDUXXHOM-WMZJFQQLSA-N

InChi: InChI=1S/C10H6Cl3N3/c11-7-1-2-8(9(12)3-7)10(13)4-16-6-14-5-15-16/h1-6H/b10-4-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 110 mg/mL (400.68 mM; Need ultrasonic). H2O : < 0.1 mg/mL (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

Loreclezole (10, 25, 50 or 75 mg/kg, i.p. 60 min before measurement of seizure threshold ) results in a dosedependent rise in seizure threshold as measured by the dose of pentylenetetrazolrequired to produce a convulsion 60 min later. Loreclezole also has the least effect on loss of muscle tone as measured by the “pull-up” test.

References:

1. Wingrove PB, 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. Proc Natl Acad Sci U S A. 1994 May 10;91(10):4569-73.
2. Sanna E, et al. Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60.
3. Green AR, et al. A behavioural and neurochemical study in rats of the pharmacology of loreclezole, a novel allosteric modulator of the GABAA receptor. Neuropharmacology. 1996;35(9-10):1243-50.

Products are for research use only. Not for human use.