Interaction of Human Butyrylcholinesterase Variants with Bambuterol and Terbutaline

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Stereoselective inhibition of human butyrylcholinesterase by the enantiomers of bambuterol and their intermediates.

This work describes the sequential hydrolysis of bambuterol enantiomers and their monocarbamate metabolites (MONO) catalyzed by human butyrylcholinesterase (BChE) as well as the enzyme inhibition resulting from this process. Particular emphasis is given to the contribution given by MONO to the enzyme inhibition because it was not fully characterized in previous works. Bambuterol and MONO enanti...

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Novel Human Butyrylcholinesterase Variants: Toward Organophosphonate Detoxication

Human butyrylcholinesterase (hBChE) is currently being developed as a detoxication enzyme for stoichiometric binding and/or catalytic hydrolysis of organophosphates. Herein, we describe the use of a molecular evolution method to develop novel hBChE variants with increased resistance to stereochemically defined nerve agent model compounds of soman, sarin, and cyclosarin. Novel hBChE variants (Y3...

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Comparison between a new once-daily, bronchodilating drug, bambuterol, and terbutaline sustained-release, twice daily.

Bambuterol is a prodrug, from which terbutaline is slowly generated. The objectives of the study were to evaluate whether bambuterol, given once daily, can control symptoms in asthmatic patients and to compare the bronchodilating effect and the side effects with those of terbutaline sustained-release (SR) tablets given twice daily. Twenty-five out-patients with bronchial asthma were treated dur...

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Butyrylcholinesterase Genetic Variants: Association with Cocaine Dependence and Related Phenotypes

OBJECTIVE The search for genetic vulnerability factors in cocaine dependence has focused on the role that neuroplasticity plays in addiction. However, like many other drugs, the ability of an individual to metabolize cocaine can also influence susceptibility to dependence. Butyrylcholinesterase (BChE) metabolizes cocaine, and genetic variants of the BChE gene (BCHE) alter its catalytic activity...

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ژورنال

عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry

سال: 2004

ISSN: 1475-6366,1475-6374

DOI: 10.1080/14756360410001667300