LY 367385
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:8.8 μM
LY 367385是一种选择性的mGlu1a受体拮抗剂,用于阻断君子氨酸诱导的磷酸肌醇水解。
mGlu家族G蛋白偶联谷氨酸受体目前包括八个成员。3,5- dihydroxyphenylglycine可以特异性激活I组mGlu受体,已发现其调节脊椎动物大脑的多重效应。
体外:与LY367385的活性相比,该新型化合物LY367366在低微摩尔浓度下拮抗mGlu1a和5受体,但在较高浓度下也募集其他亚型。LY367366具有神经保护能力,普遍比LY357385效力低。这一事实表明,mGlu1受体抑制剂是具有显著神经保护作用的药物[1]。
体内:昏睡小鼠和DBAr2小鼠侧脑室注射(i.c.v.)给药LY 367385和AIDA,局灶给药至GEPR下丘。250 nmol 的LY 367385经i.c.v给药后,在昏睡小鼠中这两种化合物显著减少脑电图中自发棘波放电和慢波放电的发生率。50 nmol 的LY 367385在30到60分钟抑制自发棘波放电和慢波放电。在DBAr2小鼠中,两种化合物都产生对声音诱发阵挛性发作的迅速、瞬态抑制。在遗传性癫痫易感大鼠中,两种化合物都降低声音诱发阵挛性发作。结果表明,mGlu1受体拮抗剂是潜在的抗惊厥工具,mGlu1受体的激活可能导致各种癫痫综合征 [2]。
临床试验:目前尚未进行临床研究。
参考文献:
[1]. Bruno V, Battaglia G, Kingston A, O'Neill MJ, Catania MV, Di Grezia R, Nicoletti F. 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.
[2]. Chapman AG, Yip PK, Yap JS, Quinn LP, Tang E, Harris JR, Meldrum BS. 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.
Physical Appearance | White solid |
Storage | Desiccate at RT |
M.Wt | 209.2 |
Cas No. | 198419-91-9 |
Formula | C10H11NO4 |
Solubility | <20.92mg/ml in 1.1eq. NaOH |
Chemical Name | (S)-4-(amino(carboxy)methyl)-3-methylbenzoic acid |
SDF | Download SDF |
Canonical SMILES | OC([C@H](C1=CC=C(C(O)=O)C=C1C)N)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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