AMN082|cas:97075-46-2|西域试剂

AMN082,99.73%

产品编号：Bellancom-103565| CAS NO：97075-46-2| 分子式：C₂₈H₃₀Cl₂N₂| 分子量：465.46

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货号	价格	库存与货期
Bellancom-103565	￥1700.00	杭州北京（现货）
Bellancom-103565	￥2800.00	杭州北京（现货）
Bellancom-103565	￥5800.00	杭州北京（现货）
Bellancom-103565	￥9300.00	杭州北京（现货）
Bellancom-103565	￥14800.00	杭州北京（现货）

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AMN082

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 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.

体外研究

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.

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

体内研究

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.

西域 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.

体内研究

西域 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.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式