Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
|
pubmed:dateCreated |
1995-2-16
|
pubmed:abstractText |
Oxadiazolones and oxadiazolethiones are potent, reversible competitive inhibitors of MAO B in rat brain mitochondria. We have compared the Ki values of six of these inhibitors towards MAO B from rat, human and beef liver mitochondria, using benzylamine as substrate. Unexpectedly, their inhibitory potency varies by 3 to 4 orders of magnitude between rat and beef liver MAO B, whereas the inhibition of the rat and human liver enzymes is quite similar. Examples are 5-(4-benzyl-oxyphenyl)-3-(2-cyano-ethyl)-1,3,4-oxadiazole-2(3H)-th ione, with Ki at 30 degrees of 0.5 nM for rat, 0.8 nM for human, and 1,830 nM for beef liver mitochondria and 5-(4-benzyloxyphenyl)-3-(2-hydroxyethyl)-1,3,4-oxadiazol-2(3 H)-one with Ki values of 1.2, 1.1 and 1,320 nM for MAO B from these three sources. Since solubilized and membrane-bound enzymes had similar sensitivities to the inhibitors, the differences seen must arise from differences in the amino acid sequences of the three enzymes.
|
pubmed:grant | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
0006-291X
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
17
|
pubmed:volume |
206
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
556-62
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:7826372-Animals,
pubmed-meshheading:7826372-Cattle,
pubmed-meshheading:7826372-Humans,
pubmed-meshheading:7826372-Kinetics,
pubmed-meshheading:7826372-Male,
pubmed-meshheading:7826372-Middle Aged,
pubmed-meshheading:7826372-Mitochondria, Liver,
pubmed-meshheading:7826372-Monoamine Oxidase,
pubmed-meshheading:7826372-Monoamine Oxidase Inhibitors,
pubmed-meshheading:7826372-Rats,
pubmed-meshheading:7826372-Rats, Sprague-Dawley,
pubmed-meshheading:7826372-Species Specificity,
pubmed-meshheading:7826372-Structure-Activity Relationship
|
pubmed:year |
1995
|
pubmed:articleTitle |
Dramatic species differences in the susceptibility of monoamine oxidase B to a group of powerful inhibitors.
|
pubmed:affiliation |
Department of Biochemistry and Biophysics, University of California at San Francisco 94143.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
|