AMN082

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AMN082

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。

CAS NO:

97075-46-2

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

AMN082 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 有效抑制 cAMP 积累并刺激 GTPγS 结合 (EC₅₀, 64-290 nM)。AMN082 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, a selective, orally active, and brain penetrantmGluR7agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC₅₀values, 64-290 nM) at transfected mammalian cells expressingmGluR7. AMN082 shows selectivity over othermGluRsubtypes and selected ionotropic glutamate receptors. Antidepressant effects^[1]^[2].

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^[2].

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)^[1].
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^[3].

Animal Model:	Male Swiss mice (20-25g)^[3]
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.

分子量

465.46

性状

Solid

Formula

C₂₈H₃₀Cl₂N₂

CAS 号

97075-46-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。