当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > N1phenethyl-norcymserine, a selective butyrylcholinesterase inhibitor, increases acetylcholine release in rat cerebral cortex: a comparison with donepezil and rivastigmine.

N1phenethyl-norcymserine, a selective butyrylcholinesterase inhibitor, increases acetylcholine release in rat cerebral cortex: a comparison with donepezil and rivastigmine.

Abstract：

:The effects of (-)-N(1)phenethyl-norcymserine (PEC, 5 mk/kg, i.p.) on acetylcholine release and cholinesterase activity in the rat cerebral cortex were compared with those of donepezil (1 mg/kg, i.p.), a selective acetylcholinesterase inhibitor, and rivastigmine (0.6 mg/kg, i.p.), an inhibitor of acetylcholinesterase and butyrylcholinesterase. Acetylcholine extracellular levels were measured by microdialysis coupled with HPLC; acetylcholinesterase and butyrylcholinesterase activity were measured with colorimetric and radiometric methods. It was found that comparable 2-3 fold increases in cortical extracellular acetylcholine level, calculated as areas under the curve, followed the administration of the three drugs at the doses used. At the peak of acetylcholine increase, a 27% acetylcholinesterase inhibition and no butyrylcholinesterase inhibition was found after donepezil (1 mg/kg, i.p) administration. At the same time point, rivastigmine (0.6 mg/kg, i.p.) inhibited acetylcholinesterase by 40% and butyrylcholinesterase by 25%. After PEC (5 mg/kg, i.p.) administration, there was a 39% butyrylcholinesterase inhibition and no effect on acetylcholinesterase. Since in the present study it was also confirmed that in the brain butyrylcholinesterase activity is only about 10% of acetylcholinesterase activity, it is surprising that its partial inhibition is sufficient to increase extracellular acetylcholine levels. The importance of butyrylcholinesterase as a "co-regulator" of synaptic acetylcholine levels should thus be reconsidered.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Cerbai F,Giovannini MG,Melani C,Enz A,Pepeu G

doi

10.1016/j.ejphar.2007.06.053

subject

Has Abstract

pub_date

2007-10-31 00:00:00

pages

142-50

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(07)00771-6

journal_volume

572

pub_type

杂志文章

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