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Galanthaminone

Cat. No. M30214
Galanthaminone Structure
Synonym:

(-)-Narwedine; Narwedin

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Biological Activity

Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.

Chemical Information
Molecular Weight 285.34
Formula C17H19NO3
CAS Number 510-77-0
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] J KOIZUMI, et al. Chem Pharm Bull (Tokyo). GALANTHAMINE CHEMISTRY. V. FORMATION OF HYDROXYAPOGALANTHAMINE FROM GALANTHAMINONE AND THE SYNTHESIS OF ITS TRIMETHYL ETHER

[2] D Mihailova, et al. Eur J Drug Metab Pharmacokinet. In vitro metabolism of galanthamine hydrobromide (Nivalin) by rat and rabbit liver homogenate

[3] D Mihailova, et al. Pharmacology. Pharmacokinetics of galanthamine hydrobromide after single subcutaneous and oral dosage in humans

[4] T Thomsen, et al. Eur J Clin Pharmacol. Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans

[5] U Bickel, et al. Clin Pharmacol Ther. Pharmacokinetics of galanthamine in humans and corresponding cholinesterase inhibition

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Keywords: Galanthaminone, (-)-Narwedine; Narwedin supplier, AChR/AChE, inhibitors, activators


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