Linked Life Data

3134033

Source:http://linkedlifedata.com/resource/pubmed/id/3134033

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
13
pubmed:dateCreated
1988-8-11
pubmed:abstractText
Analogues of the analgetic drug pethidine were synthesized. Two N-aralkylen derivatives displayed a superior inhibitory effect on the activity of NADH:ubiquinone reductase in beef heart mitochondrial membranes. Dose-response curves revealed that the potency of these compounds is very comparable to that of the standard probe rotenone. The inhibitors were characterized by (a) their action on the reductase activity in various (eukaryotic and prokaryotic) organisms, (b) their influence on the enzyme kinetics, (c) their effects on the NADH dependent reduction of different electron acceptors, (d) their interference with the activities of other mitochondrial oxido-reductases. With regard to many of these aspects a close analogy between pethidine derivatives and rotenone was observed. A computer simulation of the steric structures of these molecules indicates that both classes of the chemically rather unrelated inhibitors may imitate very similar conformations. The potential advantages of the pethidine derivatives for the investigation of structure - function relationships within complex I of the respiratory chain is discussed.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0006-2952
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
37
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2551-8
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Pethidine analogues, a novel class of potent inhibitors of mitochondrial NADH: ubiquinone reductase.
pubmed:affiliation
Institut für Physiologische Chemie, Universität München, Federal Republic of Germany.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't