MMPIP

MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (K_B 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^[1][2]. In Vitro: 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 G_α15 (IC5₅₀=26 nM) ^[1].
In CHO cells expressing rat mGluR7, MMPIP inhibits L-AP4-induced inhibition of forskolin-stimulated cAMP accumulation (IC₅₀ 220 nM)^[1].
MMPIP also antagonizes L-AP4-induced inhibition of cAMP accumulation with an IC₅₀ of 610 nM in CHO-human mGluR7/G_α15^[1]. In Vivo: 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)^[2].
MMPIP (10 mg/kg) rescues the MK-801 (0.1 mg/kg)-induced cognitive impairments, by improving the choice accuracy^[2].
Zamifenacin exhibits short elimination half-lives (plasma 1.16 h, brain 1.75 h) following i.p. administration (10 mg/kg) in mice^[2].