MMPIP hydrochloride

Names

[ Name ]:
MMPIP hydrochloride

[Synonym ]:
1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-, hydrochloride (1:2)
6-Chloro-5-methyl-N-{6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl}-1-indolinecarboxamide dihydrochloride
6-Chloro-5-methyl-N-{6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl}indoline-1-carboxamide dihydrochloride

Biological Activity

[Description]:

MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

[Target]

mGlu7

[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 Gα15 (IC50=26 nM) [1]. In CHO cells expressing rat mGluR7, MMPIP inhibits L-AP4-induced inhibition of forskolin-stimulated cAMP accumulation (IC0 220 nM)[1]. MMPIP also antagonizes L-AP4-induced inhibition of cAMP accumulation with an IC0 of 610 nM in CHO-human mGluR7/Gα15[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, brain 1.75 h) following i.p. administration (10 mg/kg) in mice[2].

[References]

[1]. Gentaroh Suzuki, et al. In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists. J Pharmacol Exp Ther. 2007 Oct;323(1):147-56.

[2]. Paulina Cieślik, et al. Negative Allosteric Modulators of mGlu 7 Receptor as Putative Antipsychotic Drugs. Front Mol Neurosci. 2018 Sep 20;11:316.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₁₆ClN₃O₃

[ Molecular Weight ]:
467.776

[ Exact Mass ]:
466.072998

Related Compounds

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