Loreclezole hydrochloride  (Synonyms: R 72063 hydrochloride)

Loreclezole hydrochloride, an antiepileptic compound, is a selective GABA_A receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors^[1][2].

GABA_A receptor^[1].

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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

310.99

C₁₀H₇Cl₄N₃

2227372-56-5

ClC1=CC=C(/C(Cl)=C/N2N=CN=C2)C(Cl)=C1.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]