A6605
AMN082
≥98% (HPLC), solid
别名:
N,N′-Dibenzhydrylethane-1,2-diamine dihydrochloride
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关于此项目
经验公式(希尔记法):
C28H28N2 · 2HCl
化学文摘社编号:
分子量:
465.46
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
方案
≥98% (HPLC)
表单
solid
储存条件
desiccated
颜色
white to off-white
溶解性
DMSO: ≥5 mg/mL
储存温度
−20°C
SMILES字符串
Cl[H].Cl[H].C(CNC(c1ccccc1)c2ccccc2)NC(c3ccccc3)c4ccccc4
InChI
1S/C28H28N2.2ClH/c1-5-13-23(14-6-1)27(24-15-7-2-8-16-24)29-21-22-30-28(25-17-9-3-10-18-25)26-19-11-4-12-20-26;;/h1-20,27-30H,21-22H2;2*1H
InChI key
YRQCDCNQANSUPB-UHFFFAOYSA-N
应用
AMN082 is a selective allosteric mGluR 7 receptor agonist and has been used to study the role of this glutamate receptor type in the medial prefrontal cortex in mice. AMN082 inhibits forskolin-stimulated cAMP accumulation, and stimulates not only GTPγS binding but also the release of stress hormones.
生化/生理作用
AMN082 is a selective allosteric mGluR 7 receptor agonist and first selective pharmacological tool for mGluR7. AMN082 inhibits forskolin-stimulated cAMP accumulation (EC50 = 64 nM) and stimulates GTPγS binding (EC50 = 290 nM) similar to L-AP4 and greater than L-glutamate. Thus, AMN082 is a "full agonist" and acts at an allosteric site in the transmembrane domain of mGluR7. AMN082 has no effects at other mGluR′s up to 10 μM and stimulates release of stress hormones (corticosterone and ACTH) and is orally active and brain penetrable.
AMN082 is a selective allosteric mGluR 7 receptor agonist and first selective pharmacological tool for mGluR7. AMN082 stimulates the release of stress hormones (corticosterone and ACTH), orally active and brain penetrable.
储存分类代码
13 - Non Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
法规信息
新产品
此项目有
David A Slattery et al.
Behavioural brain research, 328, 57-61 (2017-04-11)
Pharmacological modulation of metabotropic glutamate receptor subtype 5 (mGluR5) and 7 (mGluR7) was shown to attenuate the acquisition and to facilitate the extinction of cued and contextual, non-social, fear. Using the allosteric mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine (MPEP) and the allosteric mGluR7
Stefania Risso Bradley et al.
Pharmacology, biochemistry, and behavior, 101(1), 35-40 (2011-12-06)
Currently prescribed antidepressants affect the reuptake and/or metabolism of biogenic amines. Unfortunately for patients, these treatments require several weeks to produce significant symptom remission. However, recently it has been found that ketamine, a dissociative anesthetic agent that noncompetitively antagonizes NMDA
Tomoteru Yamasaki et al.
EJNMMI research, 3(1), 54-54 (2013-07-23)
Metabotropic glutamate 7 (mGlu7) receptor is a crucial target protein for the development of pharmaceuticals against central nervous system disorders. In the present study, we synthesized [11C]MMPIP, a putative radioligand for mGlu7 (binding constant KB = 30 nM), and evaluated
Karolina Podkowa et al.
Neuropharmacology, 141, 214-222 (2018-08-27)
Scopolamine, a muscarinic cholinergic receptor antagonist, exerts fast and prolonged antidepressant effects in the clinic. In contrast, the current treatments for major depressive disorder (MDD) require long-term drug administration. On the other hand, the sole use of scopolamine might be
Katarzyna Stachowicz et al.
Neuroscience letters, 741, 135435-135435 (2020-11-11)
Our earlier study demonstrated, that antidepressant-like and also cognitive action of MTEP, a metabotropic glutamate receptor subtype 5 (mGluR5) antagonist, was influenced by cyclooxygenase-2 (COX-2) inhibition in mice. We detected a decrease in the mGluR7 protein level in the hippocampus
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