2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. MOR antagonist 2 hydrochloride

MOR antagonist 2 hydrochloride 是一种具有血脑屏障透过性的 μ 阿片受体 (MOR) 拮抗剂，其在 MOR 上的 IC50 为 28.37 nM，EC50 为 4.25 nM，Ki 为 0.18 nM。MOR antagonist 2 hydrochloride可稳定 MOR 的非活性构象以降低受体激活水平。MOR antagonist 2 hydrochloride 可在小鼠温水甩尾试验中拮抗镇痛作用。MOR antagonist 2 hydrochloride 在阿片戒断症状小鼠中诱导的阿片戒断症状 (湿狗样抖动、爪震颤) 较少。MOR antagonist 2 hydrochloride 可用于阿片类物质使用障碍的研究。

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MOR antagonist 2 hydrochloride

MOR antagonist 2 hydrochloride Chemical Structure

CAS No. : 3075862-29-9

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MOR antagonist 2 hydrochloride 相关抗体

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder[1].

IC50 & Target[1]

μ Opioid Receptor/MOR

28.37 nM (IC50)

μ Opioid Receptor/MOR

4.25 nM (EC50)

μ Opioid Receptor/MOR

0.18 nM (Ki)

体外研究
(In Vitro)

MOR antagonist 2 hydrochloride (Compound 7) (1.5 h) 对 MOR 具有高结合亲和力 (Ki = 0.18 nM)，在 CHO 细胞膜制备物中对 KOR (Ki = 2.93 nM) 的选择性是其 16 倍，对 DOR (Ki = 30.44 nM) 的选择性是其 169 倍[1]。
MOR antagonist 2 hydrochloride (1.5 h) 是一种 MOR 低效能部分激动剂，在[35S]-GTPγS 结合实验中 EC50 = 4.25 nM[1]。
MOR antagonist 2 hydrochloride 在人源肝脏 S9 组分中表现出较高的代谢稳定性，在人源和小鼠血浆中均具有较高的血浆蛋白结合率[1]。
MOR antagonist 2 hydrochloride 表现出良好的被动肠道通透性，基线外排水平极低，并且在 Caco-2 细胞中可作为 P-gp 和 BCRP 转运蛋白的底物[1]。

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

MOR antagonist 2 hydrochloride 相关抗体:
体内研究
(In Vivo)

MOR antagonist 2 hydrochloride (10 mg/kg; s.c.; once) 在温水尾部浸泡小鼠中降低 MPE，是一种高效的 μ 阿片受体拮抗剂，其 AD50 为 0.09 mg/kg[1]。
Compound 7 (0.1-5 mg/kg; s.c.; once) 在阿片类药物戒断小鼠中引发的阿片类戒断症状 (湿狗样抖动和爪震颤) 显著少于等效及更高剂量的 Naloxone (HY-17417A)，同时保持相当的 μ 阿片受体拮抗剂活性[1]。

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

Animal Model: Swiss Webster (male, 6-8 weeks old, 25-35 g)[1]
Dosage: 10 mg/kg
Administration: s.c.; once
Result: Demonstrated dose-dependent antagonism of morphine-induced antinociception, with an AD50 value of 0.09 mg/kg (95% CI: 0.06-0.14 mg/kg).
Reduced the maximum possible effect (MPE) of morphine in a dose-dependent manner, with near-complete antagonism observed at 1 and 4 mg/kg.
Animal Model: Swiss Webster (male, 6-8 weeks old, 25-35 g, morphine pellet implantation-induced opioid tolerance)[1]
Dosage: 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg
Administration: s.c.
Result: Induced significantly fewer wet dog shakes than naloxone (1 mg/kg, s.c.) at 0.1 mg/kg.
Induced significantly fewer wet dog shakes and paw tremors than naloxone (1 mg/kg, s.c.) at 0.5 mg/kg, 1 mg/kg, and 5 mg/kg.
Caused significantly fewer wet dog shakes and paw tremors than naloxone at 1 mg/kg even at 5 mg/kg.
分子量

523.02

Formula

C28H31ClN4O4
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

MOR antagonist 2 hydrochloride 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.

Keywords:

MOR antagonist 23075862-29-9MOR antagonist2MOR antagonist-2Opioid Receptorμ-opioid receptor AntagonistCHO cellSwiss Webster mice
Inhibitorinhibitorinhibit

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