Galanthamine

Catalog No.S3866 Synonyms: Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine

For research use only.

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

CAS No. 357-70-0

Selleck's Galanthamine has been cited by 1 Publication

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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

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].

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].

Protocol (from reference)

Cell Research:[1]
  • 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.
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: Male Sprague Dawley rats
  • Dosages: 0, 0.1, 1.0, or 5.0 mg/kg
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(348.0 mM)
Water 57 mg/mL
(198.36 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 287.35
Formula

C17H21NO3

CAS No. 357-70-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCC23C=CC(CC2OC4=C(C=CC(=C34)C1)OC)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00299676 Completed Drug: Galantamine (Reminyl) Alzheimer Disease|Dementia|Galantamine Janssen-Cilag Pty Ltd May 2005 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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