AMN082 free base是一种口服有效、可透过血脑屏障的选择性代谢型谷氨酸受体7(mGluR7)变构激动剂。它通过结合受体的跨膜变构位点,在表达mGluR7的细胞中有效抑制cAMP积累并刺激GTPγS结合(EC50为64-290nM),且对其他谷氨酸受体亚型具有高选择性,从而发挥抗抑郁作用。
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2~8℃避光保存,有效期3年。
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[2]Mitsukawa K, Yamamoto R, Ofner S, Nozulak J, Pescott O, Lukic S, Stoehr N, Mombereau C, Kuhn R, McAllister KH, van der Putten H, Cryan JF, Flor PJ. A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo. Proc Natl Acad Sci U S A. 2005 Dec 20;102(51):18712-7. doi: 10.1073/pnas.0508063102. Epub 2005 Dec 9. PMID: 16339898; PMCID: PMC1317946.





