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Bullatine A

Cat. No. M19177
Bullatine A Structure
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Biological Activity

Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.

Chemical Information
Molecular Weight 343.5
Formula C22H33NO2
CAS Number 1354-84-3
Form Solid
Solubility (25°C) DMSO 12.5 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hong-Yan Tang, et al. Zhongguo Zhong Yao Za Zhi. [In vitro recovery rate of bullatine A microdialysis probe]

[2] Qian Huang, et al. J Ethnopharmacol. Concurrent bullatine A enhances morphine antinociception and inhibits morphine antinociceptive tolerance by indirect activation of spinal κ-opioid receptors

[3] Qian Huang, et al. J Neuroinflammation. Bullatine A stimulates spinal microglial dynorphin A expression to produce anti-hypersensitivity in a variety of rat pain models

[4] Shi-Yong Teng, et al. Biomed Chromatogr. Development and validation of an LC-MS/MS method for the determination of bullatine A in rat plasma: application to a pharmacokinetic study

[5] Jun Li, et al. Brain Res Bull. Bullatine A, a diterpenoid alkaloid of the genus Aconitum, could attenuate ATP-induced BV-2 microglia death/apoptosis via P2X receptor pathways

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