Home Neuronal Signaling AChR inhibitor Galanthamine For research use only.

Galanthamine

Synonyms: Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine

Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.

Galanthamine Chemical Structure

Galanthamine Chemical Structure

CAS No. 357-70-0

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Galanthamine Related Products

Signaling Pathway

AChR Signaling Pathways

AChR Signaling Pathway

Biological Activity

Description Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
Targets
AChE [1]
(Cell-free assay)
0.35 μM
In vitro
In vitro Galantamine shows reversible, competitive acetylcholinesterase inhibiting and nicotinic acetylcholinergic receptor modulatory properties[2]. Galantamine reduced the release of reactive oxygen species (up to 50%) and prevented loss in mitochondrial activity. Galantamine treatment resulted in a significant inhibition of H2O2-induced nitrite generation. Galantamine also concentration-dependently inhibited AChE activity (28–88%) in H2O2–SK-N-SH cells after 24 h. This drug, which facilitates cholinergic neurotransmission, is also neuroprotective by lowering oxidative injury[3].
Cell Research Cell lines SK-N-SH cells
Concentrations 0.1-100 μM
Incubation Time 24 h
Method Cells are seeded in 96-multiwell dishes at a density of 100,000 cells/ml (100 ml in each well) for cytotoxicity and fluorescence detection or in six-well dishes (1 ml in each well) for measuring NO production and acetylcholinesterase (AChE) activity. Cells are treated with the drugs in serum-free DMEM. Experiments are carried out 24–48 h after cells are seeded. Cells are exposed for 2 h, either to H2O2 (500 μM), or galantamine alone (0.1-100 μM), or to the combination of H2O2 plus galantamine. As no change in AChE activity is seen after 2 h, SK-N-SH cells are also incubated with galantamine for 24 h.
In Vivo
In vivo Generally, oral absorption was rapid, with maximal plasma levels reached within 2 h in all species. Absolute oral bioavailability of a gavage dose was high in rat (77 %) and dog (78 %). In mice and rats, the bioavailability of galantamine administered via the food was lower than of galantamine administered by gavage. Elimination half-life of galantamine was relatively large in rat and dog and smaller in mouse and rabbit. After i.v. administration, galantamine plasma levels declined fairly rapidly in the various animal species tested with an elimination half-life of 1−5 h in the rat and 4−7 h in the dog. The volume of distribution was 4−5 l/kg in rats and dogs. Plasma clearance was highest in male rats, 1.9 l/kg/h, about twice the value of female rats and of dogs. Sex differences in pharmacokinetics of galantamine were shown to exist in rats and mice. Male rats generally had lower plasma values of galantamine and lower exposure rates; in mice, the effect was opposite. In dogs, no sex differences in the pharmacokinetics of galantamine could be detected. In mice and rats, the bioavailability of galantamine administered via the food was lower than of galantamine administered by gavage[2].
Animal Research Animal Models Male Sprague Dawley rats
Dosages 0, 0.1, 1.0, or 5.0 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00299676 Completed
Alzheimer Disease|Dementia|Galantamine
Janssen-Cilag Pty Ltd
 May 2005 --

Chemical Information & Solubility

Molecular Weight 287.35 Formula

C17H21NO3
CAS No. 357-70-0 SDF --
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (139.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 20 mg/mL

Ethanol : Insoluble


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