1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. 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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MPAM-15

MPAM-15 Chemical Structure

CAS No. : 312632-55-6

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Description

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[1].

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.

In Vivo

MPAM-15 (1.5-5 μM; intracerebroventricular administration; single dose) produces a dose-dependent analgesic effect in mice in the 52°C hot-plate test[1].
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.

Animal Model: C57BL/6J (male and female, 8 to 10 weeks old)[1]
Dosage: 1.5 μM; 2.5 μM; 5 μM
Administration: i.c.v.; single dose
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).
Animal Model: C57BL/6J (male and female, 8 to 10 weeks old)[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

450.95

Formula

C27H27ClO4

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MPAM-15
Cat. No.:
HY-181956
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