Bulbocapnine
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.
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- CAS 番号: 298-45-3
- 分子式: C19H19NO4
- 分子量:325.36
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-12 | IC50 |
27 μM
Compound: 4, (S)-Bulbocapnine
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Reduction of dopamine level in catecholamine-inducing rat PC12 cells
Reduction of dopamine level in catecholamine-inducing rat PC12 cells
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[PMID: 17228858] |
体外実験
Bulbocapnine (5-40 μM; 6-60 h) dose-dependently reduces dopamine content in PC12 cells, with an IC50 of 26.7 μM[2].
Bulbocapnine (20 μM; 6-12 h) inhibits TH activity by 24.4% and reduces Ca2+ concentration by 12.9% in PC12 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | AUC | Bioavailability | Cmax | Tmax |
|---|---|---|---|---|---|---|
| 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 | 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 | 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 | i.v. | 280 μg·h/mL | 54 % | / | / |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:(weight 2-4 kg; anesthetized)[1]
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Dosage:5 mg/kg
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Administration:i.v.; single dose
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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.
化学情報
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CAS 番号 298-45-3
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分子量 325.36
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分子式 C19H19NO4
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SMILES
OC1=C2C3=C(OCO4)C4=CC5=C3[C@](N(CC5)C)([H])CC2=CC=C1OC
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
純度とドキュメンテーション
参考文献
[1]. Ilhan M, et al. Bulbocapnine's ability to antagonize the adrenergic inhibitory action of dopamine and analogs. Eur J Pharmacol. 1975;33(1):13-18. [Content Brief]
[2]. Shin JS, et al. Inhibitory effects of bulbocapnine on dopamine biosynthesis in PC12 cells. Neurosci Lett. 1998;244(3):161-164. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Bulbocapnine 関連分類
HY-N18279 関連分類
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