XAP044

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

XAP044 是一种 mGlu7 选择性拮抗剂，可抑制野生型小鼠脑切片中的外侧杏仁核长时程增强 (LTP)，在 88 nm 处具有半最大阻断。

XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm.(In Vitro):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 .(In Vivo):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 .

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Neuroscience

GluR

TRPV1

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196928-50-4

380.137

C15H9IO4

>98% (HPLC)

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Oc1ccc2c(c1)occ(Oc1ccc(I)cc1)c2=O

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(-20℃)

With Ice Pack

≥ 2 years