1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Mu opioid receptor antagonist 9

Mu opioid receptor antagonist 9 是一种强效、选择性强且可穿透血脑屏障的 μ- 阿片受体 (MOR) 拮抗剂,其 Ki 为 77.3 nM。Mu opioid receptor antagonist 9 对 κ- 阿片受体 (KOR) 和 δ- 阿片受体 (DOR) 具有选择性。Mu opioid receptor antagonist 9 能有效阻断精神活性物质的镇痛作用。Mu opioid receptor antagonist 9 可以逆转精神活性物质诱导的小鼠呼吸抑制。Mu opioid receptor antagonist 9 可用于阿片类药物使用障碍 (OUD) 的研究。

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Mu opioid receptor antagonist 9

Mu opioid receptor antagonist 9 Chemical Structure

CAS No. : 3058600-77-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a Ki of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD)[1].

IC50 & Target[1]

μ Opioid Receptor/MOR

77.3 nM (Ki)

κ Opioid Receptor/KOR

681 nM (Ki)

δ Opioid Receptor/DOR

4182 nM (Ki)

体外研究
(In Vitro)

Mu opioid receptor antagonist 9 (compound 53) (15 分钟) 抑制 DAMGO (HY-P0210) 和精神活性物质在 mMOR-CHO 细胞中诱导的钙流,IC50 值分别为 33.6 和 4.51 μM[1]

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

体内研究
(In Vivo)

Mu opioid receptor antagonist 9 (1-10 mg/kg;皮下注射;单次给药) 可阻断精神活性物质在小鼠温水尾浸疼痛模型中的镇痛作用[1]
Mu opioid receptor antagonist 9 (1-32 mg/kg;皮下注射;精神活性物质给药后 20 分钟单次给药) 在小鼠全身容积描记法研究中显示出对精神活性物质诱导的呼吸抑制的强效逆转作用[1]

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

Animal Model: Male Swiss Webster mice(6-8-week-old) subcutaneous injected with psychoactive substances[1]
Dosage: 1, 2, 4, 5, 10 mg/kg
Administration: s.c.; single dose
Result: Blocked the antinociception of morphine at a dose of 10 mg/kg. showed AD50s of 2.02 mg/kg (95% CL) against 10 mg/kg morphine, and 4.02 mg/kg (95% CL) against 0.1 mg/kg fentanyl.
Animal Model: Male Swiss Webster mice(6-8-week-old) subcutaneous injected with psychoactive substances[1]
Dosage: 1, 3.2, 10, 32 mg/kg
Administration: s.c.; single dose at 20min post-fentanyl
Result: Demonstrated a potent reversal effect on fentanyl-induced respiratory depression at both 10 and 32 mg/kg doses. Increased both respiratory frequency and tidal volume. Showed beneficial effect within a short time frame, appearing 10 min postadministration for the 32 mg/kg dose and 15 min postadministration for the 10 mg/kg dose.
分子量

374.90

Formula

C21H27ClN2O2

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

Mu opioid receptor antagonist 9 相关分类

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  • 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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Mu opioid receptor antagonist 9
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HY-179282
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