• 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： -20℃

• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *