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编 号：F366783
分子式：C19H15N3O3
分子量：333.34
分子式：C19H15N3O3
分子量：333.34
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CAS No: 479077-02-6
产品详情
生物活性：
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
体内研究：
MMPIP (10 mg/kg) attenuates the amplitude of the acoustic startle response and markedly enhances the prepulse-induced inhibition of the acoustic startle response (up to 137% of control).MMPIP (10 mg/kg) rescues the MK-801 (0.1 mg/kg)-induced cognitive impairments, by improving the choice accuracy.Zamifenacin exhibits short elimination half-lives (plasma 1.16 h, brain 1.75 h) following i.p. administration (10 mg/kg) in mice.
体外研究：
MMPIP inhibits L-(+)-2-amino-4-phosphonobutyric acid (L-AP4; 0.5 mM)-induced intracellular Ca2+mobilization in Chinese hamster ovary (CHO) cells coexpressing rat mGluR7 with Gα15 (IC550=26 nM) . In CHO cells expressing rat mGluR7, MMPIP inhibits L-AP4-induced inhibition of forskolin-stimulated cAMP accumulation (IC50 220 nM).MMPIP also antagonizes L-AP4-induced inhibition of cAMP accumulation with an IC50 of 610 nM in CHO-human mGluR7/Gα15.
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
体内研究：
MMPIP (10 mg/kg) attenuates the amplitude of the acoustic startle response and markedly enhances the prepulse-induced inhibition of the acoustic startle response (up to 137% of control).MMPIP (10 mg/kg) rescues the MK-801 (0.1 mg/kg)-induced cognitive impairments, by improving the choice accuracy.Zamifenacin exhibits short elimination half-lives (plasma 1.16 h, brain 1.75 h) following i.p. administration (10 mg/kg) in mice.
体外研究：
MMPIP inhibits L-(+)-2-amino-4-phosphonobutyric acid (L-AP4; 0.5 mM)-induced intracellular Ca2+mobilization in Chinese hamster ovary (CHO) cells coexpressing rat mGluR7 with Gα15 (IC550=26 nM) . In CHO cells expressing rat mGluR7, MMPIP inhibits L-AP4-induced inhibition of forskolin-stimulated cAMP accumulation (IC50 220 nM).MMPIP also antagonizes L-AP4-induced inhibition of cAMP accumulation with an IC50 of 610 nM in CHO-human mGluR7/Gα15.
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