Please use this identifier to cite or link to this item: http://hdl.handle.net/11455/70692
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dc.contributor.authorChiou, S.Y.en_US
dc.contributor.authorLai, G.W.en_US
dc.contributor.authorTsai, Y.H.en_US
dc.contributor.authorLin, L.Y.en_US
dc.contributor.authorLin, G.en_US
dc.date2005zh_TW
dc.date.accessioned2014-06-11T06:00:10Z-
dc.date.available2014-06-11T06:00:10Z-
dc.identifier.issn1054-2523zh_TW
dc.identifier.urihttp://hdl.handle.net/11455/70692-
dc.description.abstractFive common cardiovascular drugs, lovastatin, simvastatin, amlodipine besylate, nifedipine, and hydralazine hydrochloride, and two common benzodiazepines, diazepam and chlordiazepoxide hydrochloride, are all reversible mixed-type inhibitors of acetylcholinesterase and butyrylcholinesterase. The pK(i) values for acetylcholinesterase and butyrylcholinesterase inhibitions by these drugs are linearly correlated with the molecular weights, with slopes of 0.005 and 0.0021, respectively. Therefore, van der Waals' interactions between acetylcholinesterase and these drugs are stronger than those between butyrylcholinesterase probably due to a small active site gorge and a significant peripheral anionic site for acetylcholinesterase. The fact that the pKi values for both butyrylcholinesterase and acetylcholinesterase inhibitions are linearly correlated with each other suggests that both enzyme inhibitions proceed via a common mechanism. Furthermore, acetylcholinesterase and butyrylcholinesterase inhibitors such as tacrine, donepezil, rivastigmine, and galantamine are currently used to manage Alzheimer's disease. Since amlodipine besylate is a very potent inhibitor of both cholinesterases, amlodipine besylate may, like donepezil, be useful in Alzheimer's disease treatment.en_US
dc.language.isoen_USzh_TW
dc.relationMedicinal Chemistry Researchen_US
dc.relation.ispartofseriesMedicinal Chemistry Research, Volume 14, Issue 5, Page(s) 297-308.en_US
dc.relation.urihttp://dx.doi.org/10.1007/s00044-005-0140-0en_US
dc.subjecttorpedo-californicaen_US
dc.subjectbindingen_US
dc.titleQSAR for acetylcholinesterase and butyrylcholinesterase inhibition by cardiovascular drugs and benzodiazepinesen_US
dc.typeJournal Articlezh_TW
dc.identifier.doi10.1007/s00044-005-0140-0zh_TW
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.languageiso639-1en_US-
item.grantfulltextnone-
item.cerifentitytypePublications-
item.openairetypeJournal Article-
item.fulltextno fulltext-
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