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Submit ReviewAMN 082 dihydrochloride is a the first selective mGlu7 agonist. Potently inhibits cAMP accumulation and stimulates GTPγS binding in recombinant cells and on membranes expressing mGlu7 (EC50 = 64 - 290 nM). Selective over other mGluR subtypes and selected ionotropic glutamate receptors up to 10 μM. Acts via a novel allosteric site and is orally active and brain penetrant. Reduces haloperidol-induced catalepsy in rats.
View important information regarding the usage of AMN 082 dihydrochloride.
AMN 082 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 465.45 |
公式 | C28H28N2.2HCl |
储存 | Desiccate at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 97075-46-2 |
PubChem ID | 11698390 |
InChI Key | YRQCDCNQANSUPB-UHFFFAOYSA-N |
Smiles | Cl.Cl.C(CNC(C1=CC=CC=C1)C1=CC=CC=C1)NC(C1=CC=CC=C1)C1=CC=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 46.55 | 100 | |
water | 0.93 | 2 温和加热 |
以下数据基于产品分子量 465.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.15 mL | 10.74 mL | 21.48 mL |
5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
10 mM | 0.21 mL | 1.07 mL | 2.15 mL |
50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Greco et al (2010) Metabotropic glutamate 7 receptor subtype modulates motor symptoms in rodent models of Parkinson's disease. J.Pharmacol.Exp.Ther. 332 1064 PMID: 19940105
Flor et al (2005) AMN082, the first selective mGluR7 agonist: activation of receptor signaling via an allosteric site in the transmembrane domain modulates stress parameters in vivo. Neuropharmacology 49 244
Mitsukawa et al (2005) A selective metabotropic glutamate receptor 7 agonist: Activation of receptor signaling via an allosteric site modulates stress parameters in vivo. Proc.Natl.Acad.Sci.USA 102 18712
If you know of a relevant reference for AMN 082 dihydrochloride, please let us know.
关键词: AMN 082 dihydrochloride, AMN 082 dihydrochloride supplier, selective, mGlu7, mGluR7, agonists, mGlur, Group, III, Receptors, Glutamate, Metabotropic, AMN082, dihydrochloride, (Metabotropic), 2385, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AMN 082 dihydrochloride 的部分引用包括:
Jantas et al (2018) New evidences for a role of mGluR7 in astrocyte survival: Possible implications for neuroprotection. Neuropharmacology 141 223 PMID: 30170084
Shao et al (2019) Activating metabotropic glutamate receptor-7 attenuates visceral hypersensitivity in neonatal maternally separated rats. Int J Mol Med 43 761 PMID: 30569115
Broadstock et al (2012) Antiparkinsonian potential of targeting group III metabotropic glutamate receptor subtypes in the rodent substantia nigra pars reticulata. Br J Pharmacol 165 1034 PMID: 21627638
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AMN 082 was used to test a (potential) impact of metabotropic glutamate receptors on the effect of 5HT-1B receptors on neurotransmitter vesicle release in interneuronal synapse. Picture: membrane capacitance fluctuation of living neuron after series of electrical stimuli delivered to acute neural tissue. Left: control. Right: activation of metabotropic glutamate receptors (with 1 μM CHPG, 1 μM (RS)-3,5-DHPG and 1 μM AMN 082), GABA-B receptors and ACh receptors does not show a significant effect. Grey traces: individual recordings; red: averaged trace.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.