AMN 082 dihydrochloride|97075-46-2|-陌孚医药/Medlife

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AMN 082 dihydrochloride

目录号: PC14566 纯度: ≥98%

CAS No. :97075-46-2

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中文名称

AMN 082 dihydrochloride

英文名称

AMN 082 dihydrochloride

英文别名

1,2-Ethanediamine, N,N'-bis(diphenylmethyl)-, dihydrochloride;AMN 082 dihydrochloride;N,N'-Bis(diphenylmethyl)-1,2-ethanediamine dihydrochloride

Cas No.

97075-46-2

分子式

C₂₈H₂₈N₂^.₂[HCl]

分子量

465.46

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀ values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.

性状

Solid

体外研究(In Vitro)

Preincubation of the synaptosomes with AMN082 (1 μM) for 10 min before 4-aminopyridine treatment efficiently inhibits the 4-aminopyridine-evoked release of glutamate, without altering the basal release of glutamate.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

AMN082 (6 mg/kg; p.o.) induces stress hormone increases in an mGluR7-dependent fashion in mGluR7 mice (C57BL/6 genetic background).
AMN082 (1.25-5.0 mg/kg, i.p.; 30 min before every Cocaine or Morphine injection during repeated drug administration or before Cocaine or Morphine challenge) dose-dependently attenuates the development, as well as the expression of Cocaine or Morphine locomotor sensitization.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Swiss mice (20-25g)
Dosage:	1.25, 2.5, 5.0 mg/kg
Administration:	I.p.; given 30 min prior to Cocaine (10 mg/kg) or Morphine (10 mg/kg) challenge on day 17 or 20, respectively
Result:	Significantly attenuated the expression of Cocaine-induced locomotor sensitization; Attenuated the induction of Morphine-induced sensitization.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Mitsukawa K, et al. A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo. Proc Natl Acad Sci U S A. 2005;102(51):18712-18717. [Information]

[2]. Wang CC, et al. Metabotropic glutamate 7 receptor agonist AMN082 inhibits glutamate release in rat cerebral cortex nerve terminal. Eur J Pharmacol. 2018;823:11-18. [Information]

[3]. Jenda M, et al. AMN082, a metabotropic glutamate receptor 7 allosteric agonist, attenuates locomotor sensitization and cross-sensitization induced by cocaine and morphine in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2015;57:166-175. [Information]

溶解度数据

体外研究:

DMSO : 33.33 mg/mL (71.61 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1484 mL	10.7421 mL	21.4841 mL
5 mM	0.4297 mL	2.1484 mL	4.2968 mL
10 mM	0.2148 mL	1.0742 mL	2.1484 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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