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 No.: 298-45-3
- Formule: C19H19NO4
- Masse moléculaire:325.36
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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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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Masse moléculaire 325.36
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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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