2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. KOR agonist 8

KOR agonist 8 (Compound 8a) 是一种 κ-阿片受体 (KOR) 激动剂和抗伤害感受剂，对人 KOR 的 Ki 值为 5.3 nM，对人 KOR 的 EC50 值为 43.1 nM 和 9236 nM，具有 MOR/KOR 和 DOR/KOR 亚型选择性。KOR agonist 8 可用于疼痛相关研究。

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KOR agonist 8

KOR agonist 8 Chemical Structure

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KOR agonist 8 相关抗体

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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

KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research[1].

体外研究
(In Vitro)

KOR agonist 8 (Compound 8a) (30 min) 在 CHO 细胞膜上对 KOR 表现出高选择性结合亲和力，其 Ki 为 5.3 nM，对 MOR 和 DOR 的选择性超过 100 倍[1]。
KOR agonist 8 (Compound 8a) (15 min) 可通过激活 HEK293-hKOR-GloSensor 细胞中的 KOR 强效抑制 cAMP 的生成，其 EC50 为 43.1 nM，显示出较强的 G 蛋白信号传导效力[1]。
KOR agonist 8 (Compound 8a) (17 h) 在 HTLA 细胞中通过 KOR 招募 β-arrestin 的活性极弱，其 EC50 为 9236 nM，对 G 蛋白信号通路的功能选择性可达 200 倍以上[1]。

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

KOR agonist 8 相关抗体:
体内研究
(In Vivo)

KOR agonist 8 (Compound 8a) (0.2-20 mg/kg; i.p.; single dose) 在小鼠热板试验中呈现剂量依赖性镇痛活性，给药后 3 小时的 ED50 为 8.2 mg/kg (i.p.)[1]。
KOR agonist 8 (0.2-2 mg/kg; i.p.; single dose) 在小鼠腹部收缩试验中表现出剂量依赖性镇痛活性，给药后 3 小时的 ED50 为 0.5 mg/kg (i.p.)[1]。
KOR agonist 8 (2-105 mg/kg; i.p.; single dose) 在小鼠转棒试验中可诱导剂量依赖性运动障碍，2 mg/kg 剂量下仅表现为轻微障碍，而最高至 105 mg/kg (i.p.) 剂量下则出现显著障碍[1]。
Compound 8a (20 mg/kg; i.p.; single dose) 可显著降低小鼠在给药后两个时间段内由新环境诱导的自发活动[1]。
Compound 8a (20 mg/kg; i.p.; single dose) 可在给药后 1 小时和 3 小时均诱导小鼠产生显著的条件性位置厌恶[1]。

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

Animal Model: ICR mice (female, 18-20 g)[1]
Dosage: 0.2, 2, 10, 20 mg/kg
Administration: i.p.; single dose
Result: Produced dose-dependent antinociceptive effects, with an ED50 of 8.2 mg/kg (95% confidence limits: 6.3-10.6 mg/kg) at 3 hours post-administration.
Animal Model: ICR mice (male, 18-20 g)[1]
Dosage: 0.2, 0.5, 1, 2 mg/kg
Administration: i.p.; single dose
Result: Produced dose-dependent antinociceptive effects, with an ED50 of 0.5 mg/kg (95% confidence limits: 0.3-0.8 mg/kg).
Animal Model: ICR mice (male, 18-20 g)[1]
Dosage: 2, 10, 20, 105 mg/kg
Administration: i.p.; single dose
Result: Produced a slight reduction in latency to fall at 2 mg/kg, with progressively more pronounced dose-dependent impairment at higher doses up to 105 mg/kg.
Animal Model: ICR mice (male, 18-20 g)[1]
Dosage: 20 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced locomotor activity during both the 0.5-1.5 hour and 2.5-3.5 hour intervals post-administration.
分子量

576.77

Formula

C38H44N2O3
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

KOR agonist 8 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:

KOR agonist 8KOR agonist8KOR agonist-8Opioid Receptorpainrodent hot-plate assaysHTLA cellsβ-arrestin recruitmentκ-opioid receptorHEK293-hKOR-GloSensor cellsabdominal constriction assaysCHO cell membranesG protein signalingantinociceptive agentInhibitorinhibitorinhibit

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