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Puberulin 是一种香豆素类物质及具有口服有效性的镇痛剂。Puberulin 存在于 Choisya ternata var. Sundance 中。Puberulin 可在小鼠模型中对化学性和热源性致痛剂发挥镇痛活性,且该活性不涉及阿片受体或毒蕈碱受体。Puberulin 可用于神经源性疼痛的研究。

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Puberulin

Puberulin Chemical Structure

CAS No. : 57419-60-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Puberulin is a coumarin compound and an orally effective analgesic. Puberulin is present in Choisya ternata var. Sundance. Puberulin exerts analgesic activity against chemical and heat-induced pain agents in mouse models, and this activity does not involve opioid receptors or muscarinic receptors. Puberulin can be used in the research of neuropathic pain[1].

体外研究
(In Vitro)

Puberulin (25-300 μg/mL) 在 HPLC 定量分析中表现出良好的线性关系,其回归系数大于 0.99[1]
Puberulin 是通过逆流色谱法从 Choisya ternata var. Sundance 乙醇提取物中成功分离得到的无色结晶固体,其纯度经 HPLC 验证[1]

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

体内研究
(In Vivo)

Puberulin (0.3-10 mg/kg;口服;单次给药) 在雄性 Swiss Webster 小鼠中对福尔马林诱导的神经源性疼痛表现出剂量依赖性镇痛活性,在 10 mg/kg 口服剂量下可使舔爪持续时间最大减少 68%[1]
Puberulin (0.3-10 mg/kg;口服;单次给药) 可在 0.3 mg/kg 和 1 mg/kg 口服剂量下对雄性 Swiss Webster 小鼠的谷氨酸 (HY-14608) 诱导疼痛发挥镇痛活性,但 10 mg/kg 剂量下无此作用[1]
Puberulin (10 mg/kg;口服;单次给药) 在雄性 Swiss Webster 小鼠中,10 mg/kg 口服剂量下对辣椒素诱导的疼痛无镇痛活性[1]
Puberulin (0.3-10 mg/kg;口服;单次给药) 在雄性 Swiss Webster 小鼠中展现出中枢镇痛活性,在 0.3 mg/kg、1 mg/kg 和 10 mg/kg 的口服剂量下可显著提高热板痛觉阈值[1]
Puberulin (1 mg/kg;口服;单次给药) 在雄性 Swiss Webster 小鼠中表现出中枢镇痛活性,该 1 mg/kg 口服剂量的作用不依赖阿片受体介导,因为纳洛酮无法抑制其效应[1]
Puberulin (1 mg/kg;口服;单次给药) 在雄性 Swiss Webster 小鼠中表现出中枢镇痛活性,该 1 mg/kg 口服剂量的作用不由毒蕈碱受体介导,因为阿托品无法抑制其效应[1]

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

Animal Model: Swiss Webster (male, 2 months old, 20-25 g, formalin-induced acute pain model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced formalin-induced neurogenic nociception by 62% at 0.3 mg/kg, 53% at 1 mg/kg, and 68% at 10 mg/kg.
Did not affect the inflammatory pain phase (15-30 minutes post-formalin injection).
Animal Model: Swiss Webster (male, 2 months old, 20-25 g, glutamate-induced nociception model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Inhibited glutamate-induced nociception at 0.3 mg/kg and 1 mg/kg.
Showed no effect at 10 mg/kg.
Animal Model: Swiss Webster (male, 2 months old, 20-25 g, hot plate thermal nociception model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Significantly increased the nociception threshold, as shown by elevated AUC values relative to vehicle control at 0.3 mg/kg, 1 mg/kg, and 10 mg/kg.
Animal Model: Swiss Webster (male, 2 months old, 20-25 g, hot plate thermal nociception model, muscarinic receptor mechanism assessment)[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose
Result: Atropine (muscarinic receptor antagonist) did not interfere with the antinociceptive effect, as shown by no significant difference in AUC between puberulin-only and puberulin+atropine groups.
分子量

290.31

Formula

C16H18O5

CAS 号
结构分类
初始来源
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
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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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Puberulin
目录号:
HY-N19281
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