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

Mitragynine pseudoindoxyl 是一种口服有效的 μ-阿片受体 (MOR-1，Ki=0.8 nM) 的强效激动剂，和 δ-阿片受体 (DOR-1，Ki=3.0 nM) 的拮抗剂。Mitragynine pseudoindoxyl 对 κ-阿片受体 (KOR-1，Ki=24 nM) 具有中等亲和力，且不招募 β-arrestin-2，通过 G 蛋白介导的信号通路发挥作用，无 β-arrestin-2 相关激活。Mitragynine pseudoindoxyl 通过 μ 激动/δ 拮抗的混合作用机制产生强效疼痛减轻活性，且物理依赖性、呼吸抑制、便秘等副作用低，无奖赏或厌恶行为。Mitragynine pseudoindoxyl 能够减少运动过度，抑制 GI 转运和增强特性，是具有潜力的疼痛缓解剂。

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Mitragynine pseudoindoxyl

Mitragynine pseudoindoxyl Chemical Structure

CAS No. : 2035457-43-1

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Mitragynine pseudoindoxyl 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

查看 Opioid Receptor 亚型特异性产品:

查看所有亚型
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

Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
1.7 nM
Compound: 3; Mitragynine Pseudoindoxyl
Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
[PMID: 27556704]
CHO IC50
31 nM
Compound: 3; Mitragynine Pseudoindoxyl
Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
[PMID: 27556704]
CHO IC50
34 nM
Compound: 3; Mitragynine Pseudoindoxyl
Inhibition of DAMGO-induced beta-arrestin-2 recruitment at mu opioid receptor-1 (unknown origin) expressed in CHO cells preincubated for 30 mins followed by DAMGO addition measured after 90 mins by beta-galactosidase complementation assay
Inhibition of DAMGO-induced beta-arrestin-2 recruitment at mu opioid receptor-1 (unknown origin) expressed in CHO cells preincubated for 30 mins followed by DAMGO addition measured after 90 mins by beta-galactosidase complementation assay
[PMID: 27556704]
CHO IC50
61 nM
Compound: 3; Mitragynine Pseudoindoxyl
Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
[PMID: 27556704]
体外研究
(In Vitro)

Mitragynine pseudoindoxyl (25°C，90 min) 对表达鼠源 MOR-1、DOR-1、KOR-1 的 CHO 细胞具有高亲和力，其中对 MOR-1 和 DOR-1 亲和力最强，Ki 值分别为 MOR-1: 0.8±0.2 nM、DOR-1: 3.0±1.3 nM、KOR-1: 24±0.9 nM[1]。
Mitragynine pseudoindoxyl (30°C，60min) 在阿片受体转染 CHO 细胞中，是 MOR-1 强效完全激动剂、DOR-1 和 KOR-1 拮抗剂，能有效刺激 [35S]GTPγS 结合，且不招募 β-arrestin-2[1]。
Mitragynine pseudoindoxyl (100 pM-30 nM；20 min) 以浓度依赖方式抑制豚鼠回肠电刺激收缩，pD2值为8.96±0.09，效力分别是mitragynine的100倍、吗啡的20倍，该作用可被 Naloxone (HY-17417A) 拮抗[2]。
Mitragynine pseudoindoxyl (1 nM-1 μM) 以浓度依赖方式抑制小鼠输精管电刺激收缩，pD2 值为 7.40，该作用可被 Naltrexone (HY-76711) 和 Naloxone (HY-17417A) 拮抗[2]。
Mitragynine pseudoindoxyl (10 μM，与10 μM DAMGO 联合使用；90 min) 在表达修饰 MOR-1 的 CHO 细胞中，不招募 β-arrestin-2，且能浓度依赖地拮抗 DAMGO (HY-P0210) 诱导的 β-arrestin-2 招募，IC50 值为 34 nM[1]。

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

Mitragynine pseudoindoxyl 相关抗体:
体内研究
(In Vivo)

Mitragynine pseudoindoxyl (0.38 μg；脑室注射；单次)、 (0.76 mg/kg；皮下注射；单次)、 (7.5 mg/kg；口服；单次) 在 CD1、C57BL/6、129Sv6雄性小鼠的热板/辐射热甩尾镇痛模型中，对多种小鼠品系中经不同给药途径均产生强效疼痛缓解作用，皮下注射效果最强。半数有效剂量 (ED50) 分别为 0.38 μg (脑室注射)、0.76 mg/kg (皮下注射)、7.5 mg/kg (口服)[1]。
Mitragynine pseudoindoxyl (1.5 mg/kg；皮下注射；每日 2 次；29 天) 在 CD1 雄性小鼠的镇痛耐受性模型中，镇痛耐受性发展慢，29 天才出现 6 倍 ED50 移位[1]。
Mitragynine pseudoindoxyl (1.5 mg/kg；皮下注射；单次)、(4 mg/kg；皮下注射；单次) 在 CD1雄性小鼠的胃肠道转运模型中，抑制胃肠道转运，但 4 mg/kg 时达到作用平台期，无进一步抑制[1]。
Mitragynine pseudoindoxyl (1.3 mg/kg；腹腔注射；每日 1 次；2 天)、(3.2 mg/kg；腹腔注射；每日 1 次；2 天) 在 CD1 雄性小鼠的条件性位置偏爱/厌恶模型中，无条件性位置偏爱或厌恶[1]。
Mitragynine pseudoindoxyl (1.5 mg/kg；皮下注射；单次) 在 CD1 雄性小鼠的反义寡核苷酸受体下调镇痛模型中靶向 MOR-1 外显子 1 的反义寡核苷酸 (5-10 μg，脑室注射，第 1、3、5 天给药) 显著降低其镇痛作用，DOR-1 和 KOR-1 反义寡核苷酸无影响，证实镇痛依赖 MOR-1 受体[1]。

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

414.49

Formula

C23H30N2O5
CAS 号
性状

固体

颜色

Off-white to pink

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 99.9%

COA (300 KB)

产品使用指南 (1538 KB)
参考文献

Mitragynine pseudoindoxyl 相关分类

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Keywords:

Mitragynine pseudoindoxyl2035457-43-1Opioid ReceptorhYperlocomotionGI transitOxidative MetabolismInhibitorinhibitorinhibit

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