Galanthaminone - CAS 510-77-0
Catalog number: 510-77-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C17H19NO3
Molecular Weight:
285.34
COA:
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Targets:
AChE
Description:
Galantamine is a competitive and reversible cholinesterase(AChE) inhibitor, which is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.
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Purity:
>98%
Synonyms:
(-)-Narwedine; Narwedin
MSDS:
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1.Pharmacokinetics of galanthamine in humans and corresponding cholinesterase inhibition.
Bickel U1, Thomsen T, Weber W, Fischer JP, Bachus R, Nitz M, Kewitz H. Clin Pharmacol Ther. 1991 Oct;50(4):420-8.
Measurements were done to determine the plasma concentrations of galanthamine and two of its metabolites, as well as the corresponding inhibition of acetylcholinesterase activity in erythrocytes after applying 5 and 10 mg galanthamine hydrobromide as a constant-rate intravenous infusion for 30 minutes and single oral doses of 10 mg in eight healthy male volunteers. The data obtained revealed first-order pharmacokinetics, complete oral bioavailability, and a mean terminal half-life of 5.68 hours (95% confidence interval, 5.17 to 6.25 hours). Renal clearance accounted for only 25% of the total plasma clearance (CL = 0.34 L.kg-1.hr-1). Only negligible quantities of the putative metabolites, epigalanthamine and galanthaminone, were detected in blood and urine. The inhibition of acetylcholinesterase activity was closely correlated with the pharmacokinetics of galanthamine, a median maximal value of 53% being achieved by applying 10 mg galanthamine intravenously.
2.Pharmacokinetics of galanthamine hydrobromide after single subcutaneous and oral dosage in humans.
Mihailova D1, Yamboliev I, Zhivkova Z, Tencheva J, Jovovich V. Pharmacology. 1989;39(1):50-8.
Galanthamine hydrobromide (Nivalin, dose 10 mg) was given subcutaneously and orally to 8 volunteers. Galanthamine and its metabolites were quantified in plasma and urine by reversed-phase HPLC. An unusual two-stage absorption and biexponential drug decline were observed. Galanthamine plasma peaks (1.24 micrograms/ml after subcutaneous and 1.15 micrograms/ml after oral doses) were reached 2 h following administration, the t1/2(beta) values being 5.70 and 5.26 h, respectively. Minor epigalanthamine and galanthaminone plasma levels were detected. An almost complete urinary recovery of galanthamine and its metabolites was obtained within 72 h. The plasma AUC, Cmax, tmax and ka suggest that the subcutaneous and oral Nivalin formulations are bioequivalent.
3.Stereoselectivity of cholinesterase inhibition by galanthamine and tolerance in humans.
Thomsen T1, Bickel U, Fischer JP, Kewitz H. Eur J Clin Pharmacol. 1990;39(6):603-5.
The effect of galanthamine (GAL) and its 2 major metabolites on human cholinesterases has been explored. Epigalanthamine, a diastereomer of GAL, was 130-times less potent in vitro in its effect on acetylcholinesterase (AChE) in erythrocytes than the parent compound, and it did not differ significantly from the ketone galanthaminone. In vivo, the maximal 36-55% inhibition of AChE was approached 30 min after oral administration of 10 mg GAL. The duration of the catalytic inhibition corresponded to an elimination half-life of approximately 5-7 h. GAL was well tolerated in 8/8 healthy volunteers, and 3/4 Alzheimer patients tolerated the drug up to a daily dose of 40 mg.
4.In vitro metabolism of galanthamine hydrobromide (Nivalin) by rat and rabbit liver homogenate.
Mihailova D, Velkov M, Zhivkova Z. Eur J Drug Metab Pharmacokinet. 1987 Jan-Mar;12(1):25-30.
The metabolism of galanthamine hydrobromide (Nivalin) was investigated in rat and rabbit liver homogenates. Experiments were carried out varying several parameters of incubation: substrate (galanthamine hydrobromide, galanthamine, galanthaminone and epigalanthamine), cofactor enrichment (NADPH, NADP/G-6-P, NAD), pH (7.4 and 9.3), time of incubation. Substrates and metabolites were identified and quantitatively determined by GC/MS. In vitro metabolism in rat liver homogenate was negligible. The experiments with rabbit liver homogenate indicated, that galanthamine was actively metabolised the major metabolites being the oxidised product - galanthaminone, and the isomer of galanthamine - epigalantamine. The experimental results show that the metabolism of galanthamine is substrate and product stereoselective.
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CAS 510-77-0 Galanthaminone

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