AMN 082 dihydrochloride 是可口服,可透过血脑屏障的选择性mGluR7激动剂,通过跨膜区的变构位点直接激活受体信号,具有抗抑郁作用。
产品描述
AMN 082 dihydrochloride is a selective metabotropic glutamate mGlu7 receptor agonist reported to exhibit antidepressant activity.
体外活性
AMN082 inhibited 4-aminopyridine-evoked glutamate release and this phenomenon was blocked by the metabotropic glutamate mGlu7 receptor antagonist MMPIP.?Moreover, western blot analysis and immunocytochemistry confirmed the presence of presynaptic metabotropic glutamate mGlu7 receptor proteins.?The effect of AMN082 on the 4-aminopyridine-evoked release of glutamate was prevented by chelating the extracellular Ca2+ ions and the vesicular transporter inhibitor.[1]
体内活性
Pretreatment of animals with the lower doses of 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 attenuated the development, as well as the expression of cocaine or morphine locomotor sensitization.[2]
Cas No.
97075-46-2
分子式
C28H30Cl2N2
分子量
465.46
别名
AMN 082 dihydrochloride;AMN082
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years