切换导航

LY341495

现货
Catalog No.
A3577
代谢型谷氨酸受体拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 920.00
Ship with 10-15 days
10mg
¥ 1,600.00
Ship with 10-15 days
50mg
¥ 6,010.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

LY341495 is a highly potent and selective antagonist of group II metabotropic glutamate receptors with IC50 values of 21 nM and 14 nM for mGlu2 and mGlu3 receptors, respectively [1].

Glutamate is the major excitatory neurotransmitter that regulates neuronal plasticity and maintains fast synaptic transmission. The aberrant glutamate pathway has been found in a serious of neurological?problems, such as cognitive disorders, epilepsy and AD. As a selective inhibitor of group II metabotropic glutamate receptors (including mGlu2 and mGlu3), LY341495 acts as a competitive antagonist to regulate the transmission of glutamate [1 and 2].

In the functional assays, LY341495 at concentrations of 0.1 μM and 30 nM completely reversed the ACPD-induced inhibition of cAMP formation which was stimulated by forskolin in mGlu2 expressing cells and mGlu3 expressing cells, respectively. In RGT cells expressing group III mGlu receptors (mGlu4, 6, 7 and 8), LY341495 showed significant reversion of L-AP4-inhibited cAMP formation stimulated by forskolin. For mGlu4a, 7a and 8, the IC50 value of LY341495 were 22, 0.99 and 0.173 μM, respectively, which were 5 to 1000-fold higher than that for mGlu2 and mGlu3. For the group I mGlu receptors (mGlu1a and 5a), the IC50 values were 6.8 and 8.2 μM, respectively. Besides that, LY341495 was found to reversibly eliminate the long-term synaptic depression induced by DHPG in rats’ hippocampal slices [1 and 2].

In animal experiments, LY341495 was found to have effects on the post-training recognition memory. It was reported that the administration of LY341495 at different doses showed different efficacies on rats’ recognition memory. Rats treated with LY341495 at doses of 0.3, 1 and 3 mg/kg displayed a significant lower level of discrimination while LY341495 at doses of 0.05 and 0.1 mg/kg exerted a reversion of the recognition memory extinction and showed no impairment of the recognition memory [3].

References:
[1] Kingston A E, Ornstein P L, Wright R A, et al.  LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology, 1998, 37(1): 1-12.
[2] Fitzjohn S M, Bortolotto Z A, Palmer M J, et al.  The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology, 1998, 37(12): 1445-1458.
[3] Pitsikas N, Kaffe E, Markou A.  The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behavioural brain research, 2012, 230(2): 374-379.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt353.38
Cas No.201943-63-7
FormulaC20H19NO5
SynonymsLY 341495; LY-341495
SolubilityLimited solubility, soluble in DMSO
Chemical Name(1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid
SDFDownload SDF
Canonical SMILESC1C(C1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

U87细胞系

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

72h,1 μM

实验结果

目前已经确定U87细胞以谷氨酸依赖性方式增殖,药物LY341495为代谢型谷氨酸受体的抑制剂,抑制胶质瘤细胞的增殖。Iressa与LY341495共同使用有效抑制细胞增殖。

动物实验[2]:

动物模型

雄性6周龄Sprague-Dawley大鼠

剂量

3 mg/kg;腹腔内注射

实验结果

我们测试了LY341495在强迫游泳实验(FST)中的抗不动作用。LY341495显著降低不动行为(F(3,36)= 3.05;P < 0.05,n = 10)。结果分析表明,3 mg/kg LY341495处理的大鼠的不动时间显著缩短(P <0.05)。为了研究在测试期间AMPA受体传递的行为相关性,在测试前30分钟注射NBQX。NBQX对LY341495诱导的不动时间具有显著效应(F(3,36)= 3.60;P < 0.05,n = 10)。结果分析显示,剂量为3和10 mg/kg的NBQX显著抑制LY341495的抗不动作用(P < 0.05)。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Yelskaya Z, Carrillo V, Dubisz E, et al. Synergistic Inhibition of Survival, Proliferation, and Migration of U87 Cells with a Combination of LY341495 and Iressa[J]. PloS one, 2013, 8(5): e64588.

[2] Koike H1, Chaki S2. Requirement of AMPA receptor stimulation for the sustained antidepressant activity of ketamine and LY341495 during the forced swim test in rats. Behav Brain Res. 2014 Sep 1;271:111-5. doi: 10.1016/j.bbr.2014.05.065. Epub 2014 Jun 5.

质量控制

质量控制和MSDS

批次:

化学结构

LY341495