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

Bulbocapnine Chemical Structure

CAS No. : 298-45-3

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Description

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].

Cellular Effect
Cell Line Type Value Description References
PC-12 IC50
27 μM
Compound: 4, (S)-Bulbocapnine
Reduction of dopamine level in catecholamine-inducing rat PC12 cells
Reduction of dopamine level in catecholamine-inducing rat PC12 cells
[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.

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

Bulbocapnine (5 mg/kg; i.v.; single dose) significantly antagonizes the adrenergic inhibitory actions of M-7, apomorphine, N,N-dimethyldopamine, and cocaine-potentiated dopamine on cardioaccelerator nerve-induced heart rate increases, reduces the pressor response to N,N-dimethyldopamine, but does not antagonize dopamine's pressor response or alter cocaine-modified dopamine chronotropic effects[1].

MedChemExpress (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.
Molecular Weight

325.36

Formula

C19H19NO4

CAS No.
SMILES

OC1=C2C3=C(OCO4)C4=CC5=C3[C@](N(CC5)C)([H])CC2=CC=C1OC

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Bulbocapnine
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HY-N18279
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