MPAM-15
MPAM-15 is a blood-brain barrier-penetrant pan-orthosteric allosteric modulator (PAM) of opioid receptors, with ≥16-fold selectivity for μOR over δOR and κOR. MPAM-15 acts as an anti-nociceptive potentiator and analgesic, and its activity is observed in mouse models via both intracerebroventricular and intraperitoneal administration. MPAM-15 is applicable for pain-related research.
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- CAS No.: 312632-55-6
- Formule: C27H27ClO4
- Masse moléculaire:450.95
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[1]|
μ Opioid Receptor/MOR |
In Vitro
MPAM-15 (10 μM) potentiates DAMGO-induced cAMP inhibition in HEK293T cells expressing human μOR, increasing the agonist's pEC50 from 8.8 to 9.9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MPAM-15 (15-30 mg/kg; i.p.; single administration) exerts no analgesic effect on its own, but it significantly potentiates the analgesic effect of low-dose morphine and prevents the side effects induced by morphine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male and female, 8 to 10 weeks old)[1]
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Dosage:1.5 μM; 2.5 μM; 5 μM
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Administration:i.c.v.; single dose
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Result:Increased response latencies to ~45 s (1.5 μM), ~55 s (2.5 μM), and ~50 s (5 μM) at 10 minutes post-injection.
Increased response latencies to ~35 s (1.5 μM), ~45 s (2.5 μM), and ~40 s (5 μM) at 15 minutes post-injection.\nEnhanced morphine-induced antinociception in a dose-dependent manner, with the 5 μM dose producing the longest and highest analgesic effect.
Increased response latency to ~70 s at 10 minutes post-injection, ~65 s at 15 minutes, and ~45 s at 30 minutes post-injection (5 μM dose).
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Animal Model:C57BL/6J (male and female, 8 to 10 weeks old)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.p.; single dose
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Result:Significantly enhanced the analgesic effect of low-dose morphine (3 and 5 mg/kg), and the combined effect was comparable to that of high-dose morphine (10 mg/kg) used alone.
Did not cause constipation, respiratory depression, or addiction.
Chemical Information
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CAS No. 312632-55-6
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Masse moléculaire 450.95
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Formule C27H27ClO4
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SMILES
O=C1C(C(C2=CC=C(C3=CC(Cl)=CC=C3)O2)C4=C(CC(C)(C)CC4=O)O5)=C5CC(C)(C)C1
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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.
Protocole
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)