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Bicuculline methiodide

Cat. No. M30053
Bicuculline methiodide Structure
Synonym:

(+)-Bicuculline methiodide; d-Bicuculline methiodide

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Biological Activity

Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.

Chemical Information
Molecular Weight 509.29
Formula C21H20INO6
CAS Number 40709-69-1
Solubility (25°C) DMSO 150 mg/mL (ultrasonic)
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Dur-Zong Hsu, et al. Shock. Bicuculline methiodide attenuates hepatic injury and decreases mortality in septic rats: role of cytokines

[2] P Mares, et al. Epilepsy Res. Convulsant action of systemically administered glutamate and bicuculline methiodide in immature rats

[3] S W Johnson, et al. Neurosci Lett. Bicuculline methiodide potentiates NMDA-dependent burst firing in rat dopamine neurons by blocking apamin-sensitive Ca2+-activated K+ currents

[4] M P Remler, et al. Epilepsia. Bicuculline methiodide in the blood-brain barrier-epileptogen model of epilepsy

[5] A W Barolet, et al. Can J Physiol Pharmacol. Antagonist actions of bicuculline methiodide and picrotoxin on extrasynaptic gamma-aminobutyric acid receptors

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Keywords: Bicuculline methiodide, (+)-Bicuculline methiodide; d-Bicuculline methiodide supplier, GABA Receptor, inhibitors, activators


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