| Description | Loreclezole hydrochloride, an antiepileptic compound, functions as a selective modulator of GABA A receptors. Specifically, it acts as a positive allosteric modulator on receptors containing β2 or β3-subunits. |
| 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[3]. Animal Model: Adult male Lister Hooded rats[3]. Dosage: 10, 25, 50 or 75 mg/kg. Administration: IP, 60 min before measurement of seizure threshold. Result: Resulted in a dosedependent rise in seizure threshold as measured by the dose of pentylenetetrazolrequired to produce a convulsion 60 min later. |
| Synonyms | R 72063 hydrochloride, Loreclezole hydrochloride |
| molecular weight | 310.99 |
| Molecular formula | C10H7Cl4N3 |
| CAS | 2227372-56-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| 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. |