Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase.
Biperiden is a drug used in Parkinson disease treatment and it serves also as an antiseizures compound in organophosphates poisoning. It acts as antagonist of muscarinic receptor activated by acetylcholine while the enzyme acetylcholinesterase (AChE) cleaves acetylcholine in synaptic junction into c...
| Publicado en: | BioMed Research International Vol. 2017; pp. 1 - 6 |
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| Autores principales: | , , |
| Formato: | equations & formulas research tables/charts Journal Article |
| Publicado: |
Wiley-Blackwell
7/13/2017
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=124092487&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 124092487 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 23146133 FT2T jtl: BioMed Research International issn: 23146133 maglogo: N pubinfo: dt: 7/13/2017 vid: 2017 pid: 480 pub: Wiley-Blackwell place: Malden, Massachusetts artinfo: ui: 124092487 124092487 124092487 10.1155/2017/2532764 124092487 ppf: 1 ppct: 5 formats: fmt: @attributes: type: P tig: atl: Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase. aug: au: Kostelnik, Adam Cegan, Alexander Pohanka, Miroslav affil: Faculty of Chemical Technology, University of Pardubice, Studentska 95, 53210 Pardubice, Czech Republic sug: subj: Antiparkinson Agents Therapeutic Use Acetylcholinesterase Physiology Human Seizures Prevention and Control Enzymes Drug Interactions Computer Systems Cholinergic Antagonists Administration and Dosage Data Analysis Software Funding Source ab: Biperiden is a drug used in Parkinson disease treatment and it serves also as an antiseizures compound in organophosphates poisoning. It acts as antagonist of muscarinic receptor activated by acetylcholine while the enzyme acetylcholinesterase (AChE) cleaves acetylcholine in synaptic junction into choline and acetic acid. This enzyme is inhibited by various compounds; however there has not been proposed evidence about interaction with biperiden molecule. We investigated this interaction using standard Ellman’s assay and experimental findings were critically completed with an in silico prediction by SwissDock docking software. Uncompetitive mechanism of action was revealed from Dixon plot and inhibition constant (Ki) was calculated to be 1.11 mmol/l. The lowest predicted binding energy was −7.84 kcal/mol corresponding to H-bond between biperiden molecule and Tyr 341 residuum in protein structure of AChE. This interaction seems to be further stabilized by π-π interaction with Tyr 72, Trp 286, and Tyr 341. In conclusion, biperiden appears as a very weak inhibitor but it can serve as a lead structure in a pharmacological research. pubtype: Academic Journal doctype: equations & formulas research tables/charts Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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