LY367385 HCl

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Chemical Structure| 2829282-00-8 同义名 : LY367385 hydrochloride
CAS号 : 2829282-00-8
货号 : A1475061
分子式 : C10H12ClNO4
纯度 : 95%
分子量 : 245.66
MDL号 : MFCD17215678
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(488.48 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 12 mg/mL(48.85 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 LY367385 HCl is a highly selective and potent mGluR1a antagonist. The IC50 for inhibition of quisqualate-induced hydrolysis of phosphatidylinositol (PI) by LY367385 HCl was 8.8 μM, whereas that for inhibition of mGlu5a was greater than 100 μM. LY367385 HCl is known to show neuroprotective, anticonvulsant, and anti-epileptic effects[1][2].During the toxic pulse period, LY367385 HCl combined with NMDA can reduce neuronal degeneration in a concentration-dependent manner, with the maximum reduction in NMDA toxicity ranging from 40% to 60%. LY367385 is more potent than LY367366, and neither compound by itself affects neuronal viability. LY367385 HCl exhibits potent neuroprotective effects, reducing the synergistic effect of (S)-3,5-Dihydroxyphenylglycine (DHPG) by 50% at a concentration of 10 nM. Under experimental conditions with higher concentrations of antagonists, LY367385 HCl can completely antagonize the amplifying effect of DHPG on NMDA toxicity [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.07mL

0.81mL

0.41mL

20.35mL

4.07mL

2.04mL

40.71mL

8.14mL

4.07mL
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.