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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- No. CAS: 298-45-3
- Fòrmula: C19H19NO4
- Peso molecular:325.36
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Almacenamiento:
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Actividad biológica
Descripciòn
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] |
In Vitro
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 % | / | / |
In Vivo
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.
Chemical Information
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No. CAS 298-45-3
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Peso molecular 325.36
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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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.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bulbocapnine Related Classifications
HY-N18279 Related Classifications
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