Galanthamine

Catalog No.S3866 Batch:S386602

Technical Data

Formula	C₁₇H₂₁NO₃
Molecular Weight	287.35	CAS No.	357-70-0
Solubility (25°C)*	In vitro	DMSO	40 mg/mL (139.2 mM)
		Water	20 mg/mL (69.6 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:^{^[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.
Animal Study:^{^[1]}	Animal Models Male Sprague Dawley rats Dosages 0, 0.1, 1.0, or 5.0 mg/kg Administration i.p.

Cell Assay:^{^[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.

Animal Study:^{^[1]}

Animal Models
Male Sprague Dawley rats
Dosages
0, 0.1, 1.0, or 5.0 mg/kg
Administration
i.p.

References

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SHIPPING AND STORAGE
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