Linked Life Data

6620295

Source:http://linkedlifedata.com/resource/pubmed/id/6620295

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
10
pubmed:dateCreated
1983-11-23
pubmed:abstractText
A series of 3-O-alkylmorphine analogues was synthesized to determine if there was a good correlation between the rate of metabolism, type I binding affinity, and lipid solubility. The data indicate that the Km for the N-demethylation declines with increasing chain length from C1 to C9, while for increasing chain length the Vmax for the N-demethylation increases to a maximum of 15.20 nmol min-1 (mg of protein)-1 for the butyl analogue (C4) and then slowly declines with analogues with chain lengths greater than butyl (C4). The decyl (C10) and dodecyl (C12) analogues showed no activity. There was a good correlation between the lipophilicity and Km values, except for codeine and the C10 and C12 analogues. The type I binding dissociation constants (Ks) also decreased with increasing alkyl chain length with an excellent correlation between the Ks and log P. The ODmax did not change with increasing the chain length of the analogues. Our data suggest that in male rat hepatic microsomes the catalytic site for N-demethylation and the site for type I binding in this series of compounds are similar but distinct.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
26
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1343-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:year
1983
pubmed:articleTitle
Role of substrate lipophilicity on the N-demethylation and type I binding of 3-O-alkylmorphine analogues.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, U.S. Gov't, Non-P.H.S.