| 产品描述： | Loreclezole is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit-containing receptors |
| 靶点： |
GABA Receptor;GABAReceptor |
| 体外研究： |
Loreclezole, at concentrations above 6 microM, enhanced the degree and rate of apparent desensitization of the whole-cell current in a concentration-dependent manner [1]. The action of loreclezole depends on the type of beta subunit present in the receptor complex; receptors containing beta 2 or beta 3 subunits have > 300-fold higher affinity for loreclezole than receptors containing a beta 1 subunit . |
| 体内研究： |
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. |
| 参考文献： |
1. Donnelly JL, et al. Loreclezole enhances apparent desensitization of recombinant GABAA receptor currents. Neuropharmacology. 1996;35(9-10):1233-41. 2. 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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.643 ml |
18.213 ml |
36.426 ml |
| 5 mM |
0.729 ml |
3.643 ml |
7.285 ml |
| 10 mM |
0.364 ml |
1.821 ml |
3.643 ml |
| 50 mM |
0.073 ml |
0.364 ml |
0.729 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
