"目錄號: HY-14609A
GPCR/G Protein-
MPEP是mGlu5受體非競爭性拮抗劑淹接,IC50為36 nM,還是mGlu4受體的正向變構(gòu)調(diào)節(jié)劑。
mGluR
相關(guān)產(chǎn)品
CTEP-LY341495-LY354740-LY404039-RG7090-Mavoglurant-MPEP Hydrochloride-Dipraglurant-Topiramate-JNJ-40411813-L-Glutamine-FITM-JNJ16259685-MTEP hydrochloride-(S)-MCPG-
生物活性
Description
MPEP is a potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. IC50 value: 36 nMTarget: mGluR5Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.
References
[1].D'Souza, Manoranjan S.; Markou, Athina Metabotropic glutamate receptor 5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP) microinfusions into the nucleus accumbens shell or ventral tegmental area attenuate the reinforcing effects of nicotine in rats.
[2].Chau, Peipei; Soederpalm, Bo; Ericson, Mia The mGluR5 antagonist MPEP elevates accumbal dopamine and glycine levels; interaction with strychnine-sensitive glycine receptors. Addiction Biology (2011), 16(4), 591-599.
[3].Inta, Dragos; Filipovic, Dragana; Lima-Ojeda, Juan M. et al. The mGlu5 receptor antagonist MPEP activates specific stress-related brain regions and lacks neurotoxic effects of the NMDA receptor antagonist MK-801: Significance for the use as anxiolytic/ant