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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1-3
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pubmed:dateCreated |
2008-9-8
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pubmed:abstractText |
Butyrylcholinesterase (BChE, EC 3.1.1.8) is important in human cocaine metabolism despite its limited ability to hydrolyze this drug. Efforts to improve the catalytic efficiency of this enzyme have led to a quadruple mutant cocaine hydrolase, "CocH", that in animal models of addiction appears promising for treatment of overdose and relapse. We incorporated the CocH mutations into a BChE-albumin fusion protein, "Albu-CocH", and evaluated the pharmacokinetics of the enzyme after i.v. injection in rats. As assessed from the time course of cocaine hydrolyzing activity in plasma, Albu-CocH redistributed into extracellular fluid (16% of estimated total body water) with a t(1/2) of 0.66h and it underwent elimination with a t(1/2) of 8h. These results indicate that the enzyme has ample stability for short-term applications and may be suitable for longer-term treatment as well. Present data also confirm the markedly enhanced power of Albu-CocH for cocaine hydrolysis and they support the view that Albu-CocH might prove valuable in treating phenomena associated with cocaine abuse.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-10421438,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-10681384,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-10698749,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-11104759,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-12130672,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-12369817,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-12388634,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-12413452,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-12639296,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-16253215,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-16275916,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-16968810,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-17114567,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-17188226,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-237428,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-3364151,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-639429,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-7487957,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18514640-9443938
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0009-2797
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
175
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
83-7
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pubmed:dateRevised |
2011-5-13
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pubmed:meshHeading |
pubmed-meshheading:18514640-Albumins,
pubmed-meshheading:18514640-Animals,
pubmed-meshheading:18514640-Biocatalysis,
pubmed-meshheading:18514640-Butyrylcholinesterase,
pubmed-meshheading:18514640-Cocaine,
pubmed-meshheading:18514640-Cocaine-Related Disorders,
pubmed-meshheading:18514640-Female,
pubmed-meshheading:18514640-Male,
pubmed-meshheading:18514640-Rats,
pubmed-meshheading:18514640-Rats, Wistar
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pubmed:year |
2008
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pubmed:articleTitle |
An albumin-butyrylcholinesterase for cocaine toxicity and addiction: catalytic and pharmacokinetic properties.
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pubmed:affiliation |
Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, 200 First Street SW, Rochester, MN 55905, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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