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AMN 082 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMN 082 dihydrochloride图片
CAS NO:97075-46-2
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
AMN 082 dihydrochloride 是一种选择性、口服活性和脑渗透性 mGluR7 激动剂,通过跨膜结构域中的变构位点直接激活受体信号传导。
Cas No.97075-46-2
化学名N1,N2-dibenzhydrylethane-1,2-diamine dihydrochloride
Canonical SMILESC(C1=CC=CC=C1)(C2=CC=CC=C2)NCCNC(C3=CC=CC=C3)C4=CC=CC=C4.Cl.Cl
分子式C28H28N2.2HCl
分子量465.45
溶解度<46.55mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AMN 082 dihydrochloride is an specific allosteric agonist of mGluR7 [1]. In the absence of orthosteric agonist, AMN 082 activated the human mGlu7 receptor with an EC50 of 64 nM in vitro [2].

MGlu receptors belong to the family 3 G-protein coupled receptors (GPCRs) [2]. The GPCR metabotropic glutamate receptor 7 (mGluR7) is widely expressed in the nervous system. MGluR7 is implicated in many physiological processes such as synaptic plasticity and neuroprotection [1].

Dissociated hippocampal cultured neurons had been transfected with N-terminally myc-tagged mGluR7a were used in the assay. In these neurons, treatment with AMN082 at concentrations ranging from 0.5-1 μM strikingly caused robust mGluR7 internalization. The receptor internalization was increased to 291 ± 30% of control levels. The binding site of AMN082 on mGluR7 is distinct from the glutamate binding pocket on the receptor, conventional competitive antagonists are not able to prevent the activation of the allosteric agonist to the receptor [1].

In vivo, treatment with AMN082 was shown to penetrate into the brain and hence it modulated the level of stress hormones (ACTH and cortisol) in wild type animal. But these effects were not found in the mGluR7 ko mouse [2].

References:
[1].  Pelkey KA, Yuan X, Lavezzari G, et al. mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082. Neuropharmacology, 2007, 52(1): 108-117.
[2].  Gasparini F, Spooren W. Allosteric modulators for mGlu receptors. Current neuropharmacology, 2007, 5(3): 187-194.