| Bioactivity | Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors[1][2]. | ||||||||||||
| Target | GABAA receptor. | ||||||||||||
| 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: | ||||||||||||
| Name | Loreclezole | ||||||||||||
| CAS | 117857-45-1 | ||||||||||||
| Formula | C10H6Cl3N3 | ||||||||||||
| Molar Mass | 274.53 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Loreclezole
CAS: 117857-45-1 F: C10H6Cl3N3 W: 274.53
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modula
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