2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor Adrenergic Receptor
  4. Bulbocapnine

Bulbocapnine 是一种阿朴啡异喹啉生物碱，具有多巴胺受体 (Dopamine Receptor) 和 α-肾上腺素能受体 (Adrenergic Receptor) 拮抗作用和抗过氧化作用。Bulbocapnine 对酪氨酸羟化酶 (TH) 的 Ki 值为 0.20 mM。Bulbocapnine 可降低细胞内的多巴胺含量，抑制 TH 活性，降低 Ca2+ 浓度。Bulbocapnine 可拮抗多巴胺对刺激右侧心加速神经节后神经引起的心率加快产生剂量依赖性抑制作用。

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Bulbocapnine

Bulbocapnine Chemical Structure

CAS No. : 298-45-3

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Bulbocapnine 相关抗体

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bulbocapnine is an aporphine isoquinoline alkaloid that exerts antagonistic effects on dopamine Receptor) and α-adrenergic receptors, as well as anti-peroxidative effects. The Ki value of bulbocapnine for tyrosine hydroxylase (TH) is 0.20 mM. Bulbocapnine reduces intracellular dopamine content, inhibits TH activity, and decreases Ca2+ concentration. Bulbocapnine antagonizes the dose-dependent inhibitory effect of dopamine on the heart rate acceleration induced by stimulating the postganglionic fibers of the right cardiac accelerator nerve[1][2].

体外研究
(In Vitro)

Bulbocapnine (5-40 μM; 6-60 h) 可剂量依赖性降低 PC12 细胞内的多巴胺含量，其 IC50 为 26.7 μM[2]。
Bulbocapnine (20 μM; 6-12 h) 可使 PC12 细胞中 TH 活性抑制 24.4%，Ca2+ 浓度降低 12.9%[2]。

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

Bulbocapnine 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route AUC Bioavailability Cmax Tmax
Rat[2] 10 mg/kg p.o. / / 26 μg/mL 4 h
Rat[2] 10 mg/kg p.o. / / 26 μg/mL 4 h
Rat[2] 10 mg/kg p.o. / / 26 μg/mL 4 h
Rat[2] 3.2 mg/kg p.o. 126 μg·h/mL 91 % 12 μg/mL 2 h
Rat[2] 3.2 mg/kg p.o. 126 μg·h/mL 91 % 12 μg/mL 2 h
Rat[2] 3.2 mg/kg p.o. 126 μg·h/mL 91 % 12 μg/mL 2 h
Rat[2] 3.2 mg/kg i.v. 125 μg·h/mL 91 % / /
Rat[2] 3.2 mg/kg i.v. 125 μg·h/mL 91 % / /
Rat[2] 3.2 mg/kg i.v. 125 μg·h/mL 91 % / /
Dog[2] 1.0 mg/kg p.o. 99 μg·h/mL 72 % 2.5 μg/mL 1.5 h
Dog[2] 1.0 mg/kg p.o. 99 μg·h/mL 72 % 2.5 μg/mL 1.5 h
Dog[2] 1.0 mg/kg p.o. 99 μg·h/mL 72 % 2.5 μg/mL 1.5 h
Dog[2] 1.0 mg/kg i.v. 108 μg·h/mL 78 % / /
Dog[2] 1.0 mg/kg i.v. 108 μg·h/mL 78 % / /
Dog[2] 1.0 mg/kg i.v. 108 μg·h/mL 78 % / /
Monkey[2] 5.0 mg/kg p.o. 207 μg·h/mL 52 % 16 μg/mL 2 h
Monkey[2] 5.0 mg/kg p.o. 207 μg·h/mL 52 % 16 μg/mL 2 h
Monkey[2] 5.0 mg/kg p.o. 207 μg·h/mL 52 % 16 μg/mL 2 h
Monkey[2] 5.0 mg/kg i.v. 280 μg·h/mL 54 % / /
Monkey[2] 5.0 mg/kg i.v. 280 μg·h/mL 54 % / /
Monkey[2] 5.0 mg/kg i.v. 280 μg·h/mL 54 % / /
体内研究
(In Vivo)

Bulbocapnine (5 mg/kg; i.v.; single dose) 在猫中可显著拮抗 M-7、Apomorphine (HY-12723)、N,N-二甲基多巴胺增强的多巴胺对心加速神经诱导心率升高的肾上腺素能抑制作用，降低对 N,N-二甲基多巴胺的升压反应，但不会拮抗多巴胺的升压反应或改变可卡因修饰的多巴胺变时效应[1]。

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

Animal Model: (weight 2-4 kg; anesthetized)[1]
Dosage: 5 mg/kg
Administration: i.v.; single dose
Result: Significantly antagonized the inhibitory effects of M-7, apomorphine, and N,N-dimethyldopamine on heart rate tachycardia induced by neurostimulation.
Significantly reduced the increase in blood pressure induced by N,N-dimethyldopamine.
分子量

325.36

Formula

C19H19NO4
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

Bulbocapnine 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Bulbocapnine298-45-3Dopamine ReceptorAdrenergic ReceptorBeta Receptoraporphine isoquinoline alkaloiddopamine Receptorantagonisticα-adrenergic receptorsantagonisticantiperoxidantPC12 cellsCat
Inhibitorinhibitorinhibit

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