N,N'-dibenzhydrylethane-1,2-diamine;hydrochloride | 97075-46-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N,N'-dibenzhydrylethane-1,2-diamine;hydrochloride
• CAS: 97075-46-2
• 化学式: C28H29ClN2
• 分子量: 429.0
• InChiKey: OQWHMBBNPNSOAZ-UHFFFAOYSA-N

物化性质

• 溶解度：
  <46.55mg/ml，DMSO 中；不溶于 H2O

安全信息

• 危险性防范说明：
  P261,P264,P270,P271,P280,P301+P312,P302+P352,P304+P340,P305+P351+P338,P330,P332+P313,P337+P313,P362,P403+P233,P405,P501
• 危险性描述：
  H302,H315,H319,H335

制备方法与用途

生物活性

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。

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.

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.

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.