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.
体外研究
MMPIP inhibits L-(+)-2-amino-4-phosphonobutyric acid (L-AP4; 0.5 mM)-induced intracellular Ca 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.
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.
分子式
C19H16ClN3O3
分子量
333.34
CAS号
479077-02-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.