2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Methocinnamox

Methocinnamox (M-CAM) 是一种选择性的、长效的 μ-阿片受体 (MOR) 拮抗剂，其 Ki 为 0.6 nM。Methocinnamox 与 MOR 的结合持续时间极长，这种长效性源于其与MOR 正构位点的非共价结合，导致受体功能持续阻断，需依赖新受体合成才能恢复功能。Methocinnamox 对 κ-阿片受体 (KOR) (Ki = 4.9 nM) 和 δ-阿片受体 (DOR) (Ki = 2.2 nM) 均有可逆性拮抗作用，并且对这些受体不表现出内在激动剂活性。Methocinnamox 可用于逆转和预防阿片过量和使用障碍。

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Methocinnamox

Methocinnamox Chemical Structure

CAS No. : 117339-76-1

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Methocinnamox 相关抗体

Top Publications Citing Use of Products

查看 Opioid Receptor 亚型特异性产品:

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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

Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a Ki of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (Ki = 4.9 nM) and delta-opioid receptor (DOR) (Ki = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction[1][2][3].

IC50 & Target[3]

μ Opioid Receptor/MOR

0.6 nM (Ki)

κ Opioid Receptor/KOR

4.9 nM (Ki)

δ Opioid Receptor/DOR

2.2 nM (Ki)

体外研究
(In Vitro)

Methocinnamox 与小鼠脑组织中的 μ 受体紧密结合，解离速度极慢，但对 δ 和 κ 受体的结合位点无影响[3]。
Methocinnamox 能够不可逆地阻断 DAMGO (HY-P0210)、精神活性化合物和吗啡对转染人 μ 阿片受体的 HEK293 细胞中 cAMP 蓄积的抑制作用[3]。

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

Methocinnamox 相关抗体:
体内研究
(In Vivo)

Methocinnamox (10 mg/kg，皮下注射，单剂量) 可有效抵消大鼠在吗啡介导的多种作用 (镇痛、呼吸抑制、胃肠道抑制和体温变化)，且单次给药后拮抗作用可持续超过两周[1]。
Methocinnamox (0.0001-10 mg/kg，静脉注射或 10 mg/kg，静脉注射和皮下注射，单次给药) 可有效逆转和保护精神活性化合物引起的大鼠呼吸抑制[2]。
Methocinnamox (0.32 mg/kg，皮下注射，单次给药，或每 12 天一次，共 5 次；0.032 mg/kg，每日一次，共 21 天) 可降低恒河猴阿片类药物的自我给药行为[3]。

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

Animal Model: Paw inflammation and mechanical sensitivity, gastrointestinal transit and physical dependence and withdrawal model established in male Sprague-Dawley rats[1]
Dosage: 10 mg/kg
Administration: Subcutaneous injection (s.c.), single dose
Result: Significantly reduced the analgesic effect of morphine on paw inflammation and this antagonistic effect persisted for at least 15 days.
Blocked the increase in body temperature caused by morphine, with the effect lasting for more than 15 days.
Completely blocked the inhibitory effect of morphine on gastrointestinal peristalsis until 21 days.
Did not result in a longer or more severe withdrawal syndrome.
Animal Model: Reversal of psychoactive compound assay established in adult male Sprague-Dawley rats[2]
Dosage: 0.0001, 0.001, 0.01, 0.1, 1, 10 mg/kg (i.v.) and 10 mg/kg (i.v.) and (s.c)
Administration: Intravenous injection (i.v.) and subcutaneous injection (s.c.), single dose
Result: Dose-dependently rapidly reversed severe respiratory depression.
Provide long-lasting protection and effectively prevent the "re-anesthesia" phenomenon that occurs after rescue.
Exhibited a significantly longer duration of action when administered subcutaneously (s.c.) compared to intravenous (i.v.) administration at the same dose.
Animal Model: Self-Administration model established in rhesus monkeys[3]
Dosage: 0.032 mg/kg and 0.32 mg/kg
Administration: Subcutaneous injection (s.c.), single dose, or once every 12 days for 5 doses (0.32 mg/kg); once daily for 21 days (0.032 mg/kg)
Result: Effectively and selectively blocked the reinforcing effects (euphoria) of opioid agent.
Reduced the relative reinforcing value of opioid drugs, making non-drug rewards (such as food) more attractive.
Did not impair advanced cognitive functions such as working memory or attention.
had no significant effect on the cardiovascular system and body temperature regulation at 3.2 mg/kg.
分子量

484.59

Formula

C30H32N2O4
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

Methocinnamox 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

Methocinnamox117339-76-1M-CAMOpioid ReceptorBehavioral pharmacologymethocinnamoxopioid use disorderopioidsoverdoseInhibitorinhibitorinhibit

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