生物活性 | |||
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描述 | AMN082 is a selective, orally active and brain-penetrating mGluR7 agonist that directly activates receptor signalling through allosteric sites in the transmembrane domain. In transfected mGluR7-expressing mammalian cells, AMN082 potently inhibited cAMP accumulation and stimulated GTPγS binding with EC50 values of 64-290 nM. AMN082 is selective for other mGluR subtypes and some ionotropic glutamate receptors. AMN082 exhibits an antidepressant effect[1][2]. Preincubation of synaptosomes with AMN082 (1 μM), 10 min before 4-aminopyridine treatment, effectively inhibited 4-aminopyridine-induced glutamate release without altering basal glutamate release[2]. |
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.21mL |
10.74mL 2.15mL 1.07mL |
21.48mL 4.30mL 2.15mL |
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