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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。
AMN082图片
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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM2.1484 mL10.7421 mL21.4841 mL
5 mM0.4297 mL2.1484 mL4.2968 mL
10 mM0.2148 mL1.0742 mL2.1484 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。