MW:193.24
溶解性:DSMO 39 mg/mL Water <1 mg/ml Ethanol 39 mg/mL
纯度:>99%
描述:
MPEP (6-methyl-2-(phenylethynyl)-pyridine ) is a potent, systemically and selective non-competitive active antagonists of the mGluR5 subtype. MPEP shows no effects on other related targets including recombinant mGluR1b, group II or III mGluRs or ionotropic glutamate receptors. MPEP may cause a small reduction in glutamate evoked responses in Xenopus oocytes expressing recombinant hNMDA1A/2B receptors, but this reduction was not considered signicant. MPEP can provide neuroprotection against glutamate- or NMDA-induced toxicity in cultured rat cortical neurones in vitro. As a mGlu 5 receptor antagonists, MPEP can reverse the hyperalgesia associated with in?ammation effectively in nervous system disease models, such as inflammatory pain models. These effects are primarily mediated by mGlu 5 receptors expressed on the peripheral terminals of sensory neurons. [3]
参考文献:
[1] Salt, T. E., K. E. Binns, et al. (1999). "Antagonism of the mGlu5 agonist 2-chloro-5-hydroxyphenylglycine by the novel selective mGlu5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP) in the thalamus." Br J Pharmacol 127(5): 1057-1059.
[2] O'Leary, D. M., V. Movsesyan, et al. (2000). "Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism." Br J Pharmacol 131(7): 1429-1437.
[3] Chau, P., B. Soderpalm, et al. (2011). "The mGluR5 antagonist MPEP elevates accumbal dopamine and glycine levels; interaction with strychnine-sensitive glycine receptors." Addict Biol 16(4): 591-599.
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