Document Detail


pH-dependent accumulation of fentanyl, lofentanil and alfentanil by beating guinea pig atria.
MedLine Citation:
PMID:  2864047     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The influence of the pH of the incubation medium on the cellular accumulation of tritiated fentanyl, lofentanil, and alfentanil was investigated in isolated guinea pig atria. Fentanyl and lofentanil accumulated in atrial tissue up to about 30- and 50-fold, respectively. The amount of drug bound when equilibrium was attained was found to be dependent upon the pH of the medium. By plotting binding equilibria v. pH of the bath, curves were obtained which resembled titration curves. Half-maximal binding was attained at pH values close to the pKa values of fentanyl and lofentanil. Alfentanil was found to accumulate less. The uptake by the tissue was strongly proportional to the extracellular concentration. Atria equilibrated with fentanyl at pH 8.5 released the compound rapidly when exposed to a pH of 7.0, even in the continuous presence of fentanyl in the bath. The consequences of the findings for in vivo conditions are discussed with respect to a possible augmentation of the actions of fentanyl by respiratory acidosis.
Authors:
H Lüllmann; B S Martins; T Peters
Related Documents :
24233617 - Conformational effects on the fluorescence of pyrene-labeled alkyldiacyl glycerols in d...
39257 - Clostridium botulinum can grow and form toxin at ph values lower than 4.6.
748087 - Studies on the pepsinogens of human gastric mucosal extracts.
15752807 - Development of an ultrasonic technique for in situ investigating the properties of depo...
58867 - Regular structures in unit membranes. iii. further observations on the particulate comp...
25336527 - Domain wall transformations and hopping in la0.7sr0.3mno3 nanostructures imaged with hi...
Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  British journal of anaesthesia     Volume:  57     ISSN:  0007-0912     ISO Abbreviation:  Br J Anaesth     Publication Date:  1985 Oct 
Date Detail:
Created Date:  1985-11-19     Completed Date:  1985-11-19     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0372541     Medline TA:  Br J Anaesth     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1012-7     Citation Subset:  IM    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Alfentanil
Analgesics, Opioid / metabolism*
Animals
Fentanyl / analogs & derivatives*,  metabolism*
Guinea Pigs
Heart Atria
Hydrogen-Ion Concentration
Myocardial Contraction
Myocardium / metabolism*
Time Factors
Chemical
Reg. No./Substance:
0/Analgesics, Opioid; 437-38-7/Fentanyl; 60645-00-3/lofentanil; 71195-58-9/Alfentanil

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  Epidemiological value of the gamma-glutamyltransferase test in Salmonella typhimurium.
Next Document:  Efficacy of the extradural administration of lofentanil, buprenorphine or saline in the management o...