化合物XAP044 T21995

Product Introduction
Bioactivity


英文名: XAP044

描述: XAP044 是高效的选择性mGlu7拮抗剂。代谢型谷氨酸受体亚型 7 是哺乳动物 CNS 中神经传递的重要突触前调节剂。它在啮齿动物行为测试中表现出较好的大脑暴露、广谱抗应激、抗抑郁以及抗焦虑作用。

体外活性: Previous study showed that in contrast to all previous mGlu7-selective drugs, XAP044 did not act through the seven-transmembrane region but rather via a binding pocket localized in mGlu7's extracellular Venus flytrap domain, a region identified for orthosteric agonist binding, which was suggested by the chimeric receptor studies in recombinant cell line assays [1].

体内活性: In rodent behavioral paradigms, XAP044 demonstrated good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy. In addition, XAP044 could reduce freezing during acquisition of Pavlovian fear and innate anxiety, which was consistent with the phenotypes of mGlu7-deficient mice. Moreover, XAP044 was able to inhibit lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm. It was alos found that there was no effect of XAP044 on LTP of mGlu7-deficient mice, suggesting that such pharmacological effect was mGlu7-dependent [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (157.84 mM)


关键字: mGlu7 | neurotransmission | XAP044 | brain exposure | CNS | XAP-044 | inhibit | mGluR | antidepressant | Metabotropic glutamate receptors | wide spectrum | XAP 044 | anti-stress | Inhibitor | anxiolytic-like

相关产品: (S)-3,4-DCPG HCl | Direct Blue 1 | CDPPB | DMeOB | LY 456236 hydrochloride | VU0360172 | VU-1545 | mGluR3 modulator-1 | Pomaglumetad methionil anhydrous | MPEP

相关库: Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Antidepressant Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途