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.
For research use only. We do not sell to patients.
- CAS No.: 298-45-3
- Formula: C19H19NO4
- Molecular Weight:325.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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] |
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.
| 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 % | / | / |
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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CAS No. 298-45-3
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Molecular Weight 325.36
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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)
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