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Bicuculline methobromide

Cat. No. M30436
Bicuculline methobromide Structure
Synonym:

(+)-Bicuculline methobromide; d-Bicuculline methobromide

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Biological Activity

Bicuculline methobromide is a selective GABAA Receptor antagonist with an IC50 value of 3 μM. Bicuculline methobromide induces clonic tonic convulsions in mammals and can also be used to block Ca2+ activated potassium channels. Bicuculline methobromide can be used in studies of epilepsy and other related psychiatric disorders.

Chemical Information
Molecular Weight 462.29
Formula C21H20BrNO6
CAS Number 66016-70-4
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] Xian Xiao, et al. Neuropharmacology. 2-Guanidine-4-methylquinazoline acts as a novel competitive antagonist of A type γ-aminobutyric acid receptors

[2] Qing Hui Chen, et al. Hypertension. Sympathoexcitation by PVN-injected bicuculline requires activation of excitatory amino acid receptors

[3] D M Sokal, et al. Neuropharmacology. Multi-neuronal recordings reveal a differential effect of thapsigargin on bicuculline- or gabazine-induced epileptiform excitability in rat hippocampal neuronal networks

[4] A J Reeve, et al. J Neurophysiol. Spinal effects of bicuculline: modulation of an allodynia-like state by an A1-receptor agonist, morphine, and an NMDA-receptor antagonist

[5] R D Smith, et al. Brain Res. Bicuculline and picrotoxin block phase advances induced by GABA agonists in the circadian rhythm of locomotor activity in the golden hamster by a phaclofen-insensitive mechanism

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

 
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