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Zolantidine dimaleate

Cat. No. M27690
Zolantidine dimaleate Structure
Synonym:

SKF 95282 dimaleate

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Biological Activity

Zolantidine dimaleate (SKF 95282 dimaleate) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine dimaleate induces antinociception.

Chemical Information
Molecular Weight 613.68
Formula C30H35N3O9S
CAS Number 104076-39-3
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] L B Hough, et al. Biochem Pharmacol. Actions of the brain-penetrating H2-antagonist zolantidine on histamine dynamics and metabolism in rat brain

[2] K R Gogas, et al. J Pharmacol Exp Ther. Inhibition of naloxone-resistant antinociception by centrally administered H2-antagonists

[3] K R Gogas, et al. J Pharmacol Exp Ther. A role for histamine and H2-receptors in opioid antinociception

[4] L B Hough, et al. Brain Res. Zolantidine-induced attenuation of morphine antinociception in rhesus monkeys

[5] L B Hough, et al. Eur J Pharmacol. Inhibition of morphine antinociception by centrally administered histamine H2 receptor antagonists

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Keywords: Zolantidine dimaleate, SKF 95282 dimaleate supplier, Histamine Receptor, inhibitors, activators


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