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

MPAM-15 是一种可穿透血脑屏障的阿片受体​泛正构变构调节剂 (PAM),相比 δORκOR,对 μOR 具有 ≥16 倍的选择性。MPAM-15 可作为抗伤害感受增强剂和镇痛剂,在小鼠模型中通过脑室内给药和腹腔给药均观察到其活性。MPAM-15 可用于疼痛相关研究。

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MPAM-15

MPAM-15 Chemical Structure

CAS No. : 312632-55-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

MPAM-15 (10 μM) 可增强表达人 μ 阿片受体 (μOR) 的 HEK293T 细胞中 DAMGO 诱导的 cAMP 抑制作用,将该激动剂的 pEC50 从 8.8 提升至 9.9[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MPAM-15 (1.5-5 μM;侧脑室给药;单次给药) 在 52℃ 热板试验中可使小鼠产生剂量依赖性镇痛作用[1]
MPAM-15 (15-30 mg/kg;腹腔注射;单次给药) 本身无镇痛作用,但能显著增强低剂量吗啡的镇痛效果,且可避免吗啡引发的副作用[1]

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.
分子量

450.95

Formula

C27H27ClO4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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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产品名称:
MPAM-15
目录号:
HY-181956
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