| Identification | Back Directory | [Name]
MMPIP (hydrochloride) | [CAS]
1215566-78-1 | [Synonyms]
242084
CS-1472
CS-2104
SB-242084 HCl
MMPIP hydrochloride (479077-02-6 Free base)
6-chloro-5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-2,3-dihydroindole-1-carboxamide
MMPIP hydrochloride,MMPIP,system,nervous,neuropathic,behavior,pain,inhibit,central,glutamate,cognitive,allosteric,Metabotropic glutamate receptors,Inhibitor,metabotropic,mGluR,mGluR7 | [Molecular Formula]
C19H16ClN3O3 | [MOL File]
1215566-78-1.mol | [Molecular Weight]
369.802 |
| Hazard Information | Back Directory | [Description]
MMPIP is a reversible allosteric antagonist of the metabotropic glutamate receptor 7 (mGluR7) that blocks agonist-induced calcium mobilization (IC50 = 26 nM). It does not affect other mGlu receptors. The modulation of mGluR7 by MMPIP is context dependent, in that it is not observed in all known mGluR7 signaling pathways. MMPIP has been used to investigate the role of mGluR7 in cocaine-mediated reward signaling, attention and impulse control, and cognitive behavior in mice and rats. MMPIP also reversibly inhibits constitutive activity of mGluR7 in sympathetic neurons from the rat superior cervical ganglion. | [Uses]
MMPIP Hydrochloride is a reversible allosteric antagonist of the metabotropic glutamate receptor 7 (mGluR7) that blocks agonist-induced calcium mobilization. | [Definition]
ChEBI: 6-chloro-5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-2,3-dihydroindole-1-carboxamide;dihydrochloride is an organic molecular entity, an indole alkaloid and a pyridine. It has a role as a receptor modulator. | [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]. | [IC 50]
mGlu7 | [References]
[1] GENTAROH SUZUKI. In vitro pharmacological characterization of novel isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 323 1: 147-156. DOI: 10.1124/jpet.107.124701
[2] COLLEEN M NISWENDER. Context-dependent pharmacology exhibited by negative allosteric modulators of metabotropic glutamate receptor 7.[J]. Molecular Pharmacology, 2010, 77 3: 459-468. DOI: 10.1124/mol.109.058768
[3] XIA LI. Metabotropic Glutamate Receptor 7 Modulates the Rewarding Effects of Cocaine in Rats: Involvement of a Ventral Pallidal GABAergic Mechanism[J]. Neuropsychopharmacology, 2009, 34 7: 1783-1796. DOI: 10.1038/npp.2008.236
[4] ABIGAIL BENN E S J R. Investigating glutamatergic mechanism in attention and impulse control using rats in a modified 5-choice serial reaction time task.[J]. PLoS ONE, 2014: e115374. DOI: 10.1371/journal.pone.0115374
[5] ENZA PALAZZO. MMPIP, an mGluR7-selective negative allosteric modulator, alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.[J]. PAIN?, 2015, 156 6: 1060-1073. DOI: 10.1097/j.pain.0000000000000150
[6] KAMMERMEIER P J. Constitutive activity of metabotropic glutamate receptor 7.[J]. BMC Neuroscience, 2015, 16: 17. DOI: 10.1186/s12868-015-0154-6 |
|
| Company Name: |
Cckinase, Inc.
|
| Tel: |
+1 (732)236-3202 |
| Website: |
www.cckinase.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|