M119
M119 (NSC 119910) is a Gβγ subunit and PLCβ3 inhibitor with selective activity toward μ-opioid receptor-related pathways. M119 selectively inhibits Gβγ-dependent PLCβ3 activation, reduces inositol phosphate production, and enhances μ-opioid receptor-mediated antinociception. M119 attenuates acute μ-opioid receptor agonist-induced antinociceptive tolerance and physical dependence in mice. M119 can be used for pain-related research.
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- CAS No.: 500533-94-8
- Formule: C20H18O7
- Masse moléculaire:370.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
μ Opioid Receptor/MOR |
PLC |
In Vitro
M119 (10-30 µM; 30 min) concentration-dependently inhibits µ-opioid receptor (hMOR-CHO cell)-mediated inositol phosphate production, with significant inhibition observed at 10 µM and 30 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
M119 (100 nM; intracerebroventricular injection; single administration; given 30 minutes prior to Naloxone treatment) significantly attenuates acute Naloxone (HY-17417A)-induced physical dependence in mice, reducing the withdrawal jumping response triggered by the μ-opioid receptor antagonist by approximately 68%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (male, 20-30 g)[1]
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Dosage:100 nM (coadministered with intracerebroventricular agonists); 100 mg/kg (administered immediately before subcutaneous μ-opioid receptor agonist)
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Administration:i.c.v.; single dose; coadministered with agonists; i.p.; single dose; administered immediately before subcutaneous μ-opioid receptor agonist
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Result:Produced a 10-fold leftward shift in μ-opioid receptor agonist's antinociceptive dose-response curve.
Produced a sevenfold leftward shift in μ-opioid receptor agonist DAMGO's dose-response curve, with DAMGO's ED50 decreasing from 0.07 nmol to 0.01 nM.
Produced a twofold leftward shift in κ-opioid receptor agonist U50,488's dose-response curve, with U50,488's ED50 decreasing from 37 nmol to 17 nM.
Had no significant effect on antinociception mediated by δ1-selective agonist DPDPE or δ2-selective agonist Deltorphin II.
Produced a fourfold leftward shift in μ-opioid receptor agonist's antinociceptive dose-response curve, with μ-opioid receptor agonist's ED50 decreasing from 5.0 mg/kg to 1.3 mg/kg.
Had no effect on baseline tail-withdrawal latencies.
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Animal Model:ICR mice (male, 20-30 g)[1]
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Dosage:100 nM
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Administration:i.c.v.; single dose; administered 30 min before Naloxone
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Result:Reduced μ-opioid receptor antagonist-induced withdrawal jumps from an average of 71 to 23.
Chemical Information
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CAS No. 500533-94-8
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Masse moléculaire 370.35
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Formule C20H18O7
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SMILES
O=C(C1CCCCC1C2=C3C=CC(C(O)=C3OC4=C2C=CC(O)=C4O)=O)O
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Synonyms
NSC 119910
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Mathews JL, et al. A novel Gbetagamma-subunit inhibitor selectively modulates mu-opioid-dependent antinociception and attenuates acute morphine-induced antinociceptive tolerance and dependence. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2008 Nov 19;28(47):12183-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
M119 Related Classifications
HY-177218 Related Classifications
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