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479077-02-6

479077-02-6 structure
479077-02-6 structure
  • Name: MMPIP
  • Chemical Name: 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-yl-[1,2]oxazolo[4,5-c]pyridin-4-one
  • CAS Number: 479077-02-6
  • Molecular Formula: C19H15N3O3
  • Molecular Weight: 369.80200
  • Catalog: Signaling Pathways GPCR/G Protein mGluR
  • Create Date: 2016-02-21 00:41:37
  • Modify Date: 2024-01-09 18:23:47
  • 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[1][2].

Name 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-yl-[1,2]oxazolo[4,5-c]pyridin-4-one
Synonyms S14-1930
Thioperamide
6-(4-Methoxyphenyl)-5-methyl-3-(4-pyridinyl)-isoxazolo[ 4,5-c]pyridin-4(5H)-one
Description 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[1][2].
Related Catalog
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.

Molecular Formula C19H15N3O3
Molecular Weight 369.80200
Exact Mass 369.08800
PSA 70.15000
LogP 4.06610
Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Hazard Codes T+
RIDADR UN 2811 6.1 / PGIII