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LY367385

产品编号 T15818 CAS 198419-91-9

LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with < 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.

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LY367385, CAS 198419-91-9

规格	价格/CNY		货期	数量
10 mg	￥ 4,160		4-5周
50 mg	￥ 17,300		4-5周

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其他形式的 LY367385:

LY367385 hydrochloride
询价
(±)-LY367385
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.
靶点活性	mGluR1a:8.8 μM
体外活性	LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se and it also displays effective neuroprotective effects, causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse decreases neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 fully antagonized the amplification of NMDA toxicity by DHPG under experimental conditions at higher concentrations of the antagonist[2].
体内活性	LY367385 produces a rapid, transient suppression of sound-induced clonic seizures (ED50 = 12 nM, i.c.v., 5 min), in DBA/2 mice. LY367385 significantly decreases the incidence of spontaneous spike and wave discharges on the electroencephalogram in lethargic mice, from 30 to >150 min after the administration of LY367385, 250 nM, i.c.v. LY367385 has been administered intracerebroventricularly (i.c.v.) to DBA/2 mice and lethargic mice (lh/lh), and focally into the inferior colliculus of genetically epilepsy prone rats (GEPR). LY367385 reduces sound-induced clonic seizures, in genetically epilepsy prone rats. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3].

分子量	209.2
分子式	C10H11NO4
CAS No.	198419-91-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Clark et al. (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors. Bioorg.Med.Chem.Lett. November 1997, 7 (21): 2777-2780. 2. Bruno V, et al. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 receptors. Neuropharmacology. 1999 Feb;38(2):199-207. 3. Chapman AG, et al. Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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