Title : Brain levels and acetylcholinesterase inhibition with galantamine and donepezil in rats, mice, and rabbits.

Pub. Date : 2005 Feb 8

PMID : 15694923






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1 Brain levels and acetylcholinesterase inhibition with galantamine and donepezil in rats, mice, and rabbits. Galantamine acetylcholinesterase Rattus norvegicus
2 Galantamine is a rather weak acetylcholinesterase (AChE) inhibitor, currently approved for the symptomatic treatment of Alzheimer"s disease, with possible additional allosteric potentiating effects at the nicotinic ACh receptor (nAChR). Galantamine acetylcholinesterase Rattus norvegicus
3 Galantamine is a rather weak acetylcholinesterase (AChE) inhibitor, currently approved for the symptomatic treatment of Alzheimer"s disease, with possible additional allosteric potentiating effects at the nicotinic ACh receptor (nAChR). Galantamine acetylcholinesterase Rattus norvegicus
4 Earlier data from in vitro biochemical tests suggest that donepezil is 40- to 500-fold more potent than galantamine in inhibiting AChE. Galantamine acetylcholinesterase Rattus norvegicus
5 In this study, both brain levels and Ki values for AChE inhibition for donepezil and galantamine in rat, mouse, and rabbit after subcutaneous application were determined. Galantamine acetylcholinesterase Rattus norvegicus
6 Ki values of brain AChE inhibition for galantamine and donepezil, respectively, are 7.1 and 2.3 microg/g in rats, 8.3 and 0.65 microg/g for mice, and 19.1 and 1.3 microg/g in rabbits. Galantamine acetylcholinesterase Rattus norvegicus
7 The data also suggest that for a similar degree of brain AChE inhibition, 3-15 times higher galantamine than donepezil doses are needed. Galantamine acetylcholinesterase Rattus norvegicus