Galanthaminone | CAS:510-77-0 | Manufacturer ChemFaces

Galanthaminone

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Description:

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.

Targets:

AChR | IL Receptor

In vitro:

European Journal of Drug Metabolism and Pharmacokinetics,1987,12(1):25-30.

In vitro metabolism of galanthamine hydrobromide (Nivalin®) by rat and rabbit liver homogenate[Reference: WebLink]

The metabolism of galanthamine hydrobromide (Nivalin®) was investigated in rat and rabbit liver homogenates.
METHODS AND RESULTS:
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.
CONCLUSIONS:
The experimental results show that the metabolism of galanthamine is substrate and product stereoselective.

In vivo:

Clin Pharmacol Ther. 1991 Oct;50(4):420-8.

Pharmacokinetics of galanthamine in humans and corresponding cholinesterase inhibition.[Pubmed: 1914378]

METHODS AND RESULTS:
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.
CONCLUSIONS:
Analysis of in vitro and ex vivo concentration responses revealed no differences, indicating that no metabolites of galanthamine exert additional inhibition of acetylcholinesterase activity.

Galanthaminone Description

Source:	The bulbs of Lycoris radiata
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Product Name	Galanthaminone
Price:	$318 / 10mg
CAS No.:	510-77-0
Catalog No.:	CFN90742
Molecular Formula:	C₁₇H₁₉NO₃
Molecular Weight:	285.3 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:	The bulbs of Lycoris radiata
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF
Similar structural:	Comparison (Web) (SDF)
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library IL Receptor Inhibitor Library AChR Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	3.5051 mL	17.5254 mL	35.0508 mL	70.1016 mL	87.6271 mL
5 mM	0.701 mL	3.5051 mL	7.0102 mL	14.0203 mL	17.5254 mL
10 mM	0.3505 mL	1.7525 mL	3.5051 mL	7.0102 mL	8.7627 mL
50 mM	0.0701 mL	0.3505 mL	0.701 mL	1.402 mL	1.7525 mL
100 mM	0.0351 mL	0.1753 mL	0.3505 mL	0.701 mL	0.8763 mL

CFN98548	Pseudolycorine	29429-03-6	289.33	C₁₆H₁₉NO₄
CFN99730	Lycorine chloride	2188-68-3	323.78	C₁₆H₁₇NO₄Cl
CFN93030	Ungeremine	72510-04-4	266.27	C₁₆H₁₂NO₃+
CFN90745	Lycoramine	21133-52-8	289.4	C₁₇H₂₃NO₃
CFN91708	O-Desmethyl galanthamine	60755-80-8	273.3	C₁₆H₁₉NO₃
CFN90743	Galantamine	357-70-0	287.4	C₁₇H₂₁NO₃
CFN90744	Galantamine hydrobromide	1953-04-4	368.3	C₁₇H₂₂BrNO₃
CFN91709	Galanthamine 10-Oxide(Galanthamine N-Oxide)	134332-50-6	303.4	C₁₇H₂₁NO₄
CFN91707	O-Acetylgalanthamine	25650-83-3	329.4	C₁₉H₂₃NO₄
CFN90742	Galanthaminone	510-77-0	285.3	C₁₇H₁₉NO₃