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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 312632-55-6
- 分子式: C27H27ClO4
- 分子量:450.95
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Opioid Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
μ Opioid Receptor/MOR |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 312632-55-6
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分子量 450.95
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MPAM-15 関連分類
HY-181956 関連分類
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