AMN082 free base|83027-13-8|-陌孚医药/Medlife

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AMN082 free base

目录号: PL07117 纯度: ≥99%

CAS No. :83027-13-8

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中文名称	AMN082 free base
中文别名	2-甲基噻唑-4-甲酰胺;N,N-双(二苯基甲基)乙烯二胺
英文名称	AMN082 free base
英文别名	1,2-Ethanediamine,N¹,N²-bis(diphenylmethyl)-;AMN 082 DIHYDROCHLORIDE;AMN 082 dihydrochloride,N,N'-Bis(diphenylmethyl)-1,2-ethanediaminedihydrochloride;1,4-bis-phthaloyltetrazene;1,4-Bisphthalyl-tetrazen;N,N'-Bis(diphenylMethyl)-1,2-ethanediaMinedihydrochloride;N,N'-diazenediyl-bis-phthalimide;N,N'-Dibenzhydryl-aethylendiamin;N,N'-dibenzhydryl-ethane-1,2-diamine;N,N'-dibenzhydryl-ethylenediamine;Phthalimide,N,N'-azodi
Cas No.	83027-13-8
分子式	C₂₈H₃₀Cl₂N₂
分子量	465.46
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	AMN082 free base 是一种选择性，具有口服活性，可透过血脑屏障的 mGluR7 激动剂，通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上，AMN082 free base 有效抑制 cAMP 积累并刺激 GTPγS 结合 (EC₅₀, 64-290 nM)。AMN082 free base 对其他 mGluR 亚型和选择性离子型谷氨酸受体具有选择性。具有抗抑郁作用。
生物活性	AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC 50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
性状	Solid
IC50 & Target[1][2]	mGluR7
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. 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 injection during repeated drug administration or before Cocaine challenge) dose-dependently attenuates the development, as well as the expression of Cocaine locomotor sensitization. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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. [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.

溶解度数据	In Vitro: DMSO : 12.5 mg/mL (31.84 mM; ultrasonic and warming and heat to 60°C)配制储备液

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