Document Detail


Stability, blood partition, and protein binding of NQ12, a new naphthoquinone derivative.
MedLine Citation:
PMID:  10634309     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The stability of a new phospholipase A2 inhibitor, NQ12, in various pH solutions, human plasma, urine, and gastric juices, and rat liver homogenate, the blood partition of NQ12 between plasma and blood cells of rat blood, and the factors influencing the binding of NQ12 to 4% human serum albumin (HSA) using an equilibrium dialysis technique were evaluated. NQ12 was unstable in various pH solutions, human plasma and urine, and rat liver homogenate when incubated in a water-bath shaker kept at 37 degrees C and at a rate of 50 oscillations per min. However, NQ12 was stable for up to 3-hr incubation in human gastric juice. The plasma-to-blood cell concentration ratios of NQ12 were independent of NQ12 rat blood concentrations when the whole blood was incubated for up to 2-hr; the mean (+/- standard deviation) values were 0.112 +/- 0.0650 and 0.172 +/- 0.105 at initial blood NQ12 concentrations of 10 and 20 microg/ml, respectively. The binding of NQ12 to 4% HSA was considerable (higher than 99%) at NQ12 concentrations ranging from 10 to 100 microg/ml in 4% HSA. The unbound fraction of NQ12 was dependent on NQ12 concentrations, pHs of buffer, and HSA concentrations, but was independent of the concentrations of sulfisoxazole or salicylic acid, incubation temperature, buffers containing various concentrations of chloride ion, and concentrations of heparin and alpha-1-acid glycoprotein.
Authors:
S H Kim; H J Kim; C K Ryu; M G Lee
Related Documents :
6184259 - Cysteamine and prostaglandin f2 beta stimulate rat gastric mucin release.
7972329 - Comparison of two orogastric feeding markers for measuring gastrointestinal motor funct...
7282829 - Indomethacin--placental transfer, cytotoxicity, and teratology in the rat.
964479 - Histamine-stimulated gastric secretion in rats with chronic renal insufficiency.
9517829 - Habituation of oral responding in adult rats.
15232769 - Venous outflow system in rabbit gastric mucosa.
11831379 - Experimental evidence for a non-renin mediated pathway during tame-esterase induced con...
2155689 - Myocardial and metabolic abnormalities in streptozotocin-diabetic wistar and wistar-kyo...
3887969 - Correlation of purkinje neuron depression and hypnotic effects of ethanol in inbred str...
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Research communications in molecular pathology and pharmacology     Volume:  104     ISSN:  1078-0297     ISO Abbreviation:  Res. Commun. Mol. Pathol. Pharmacol.     Publication Date:  1999  
Date Detail:
Created Date:  2000-02-11     Completed Date:  2000-02-11     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  9437512     Medline TA:  Res Commun Mol Pathol Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  165-72     Citation Subset:  IM    
Affiliation:
College of Pharmacy, Seoul National University, South Korea.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
Animals
Chromatography, High Pressure Liquid
Drug Stability
Gastric Juice
Humans
Hydrogen-Ion Concentration
Liver / metabolism
Naphthalenes / blood,  metabolism*,  pharmacokinetics*,  urine
Phospholipases A / antagonists & inhibitors*
Phospholipases A2
Rats
Rats, Sprague-Dawley
Serum Albumin / metabolism
Chemical
Reg. No./Substance:
0/2-chloro-3-((4-ethyl-phenyl)-amino)-1,4-naphthalendione; 0/Naphthalenes; 0/Serum Albumin; EC 3.1.1.-/Phospholipases A; EC 3.1.1.4/Phospholipases A2

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


Previous Document:  Effect of p53 tumor suppressor on nucleotide excision repair in human colon carcinoma cells treated ...
Next Document:  Temperature sensitive effects of alpha-adrenergic stimulation in mouse ventricular myocardia.