Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists†

1997 ◽  
Vol 40 (25) ◽  
pp. 4053-4068 ◽  
Author(s):  
Michael Rowley ◽  
Janusz J. Kulagowski ◽  
Alan P. Watt ◽  
Denise Rathbone ◽  
Graeme I. Stevenson ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Nmda Receptor Antagonists ◽  
Receptor Antagonists ◽  
Brain Penetration

scholarly journals NMDA receptor antagonists ketamine and Ro25-6981 inhibit evoked release of glutamate in vivo in the subiculum

2014 ◽  
Vol 4 (6) ◽  
pp. e395-e395 ◽  
Author(s):  
T L Stan ◽  
A Alvarsson ◽  
N Branzell ◽  
V C Sousa ◽  
P Svenningsson
Keyword(s):  
Nmda Receptor ◽  
Nmda Receptor Antagonists ◽  
Receptor Antagonists

scholarly journals Gallium-68-Labelled Indocyanine Green as a Potential Liver Reserve Imaging Agent

2019 ◽  
Vol 2019 ◽  
pp. 1-8
Author(s):  
Yuxiao Xia ◽  
Li Zhang ◽  
Yanhong Zhao ◽  
Xiangdong Liu ◽  
Liang Cai ◽  
...  
Keyword(s):  
Indocyanine Green ◽  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Water Solubility ◽  
Time Points ◽  
Binding Rate ◽  
Very High

Objective. This work evaluated the potential of 68Ga-labelledNOTA-ICG (1,4,7-triazacyclononane-1,4,7-triacetic acid indocyanine green) for liver reserve imaging. Methods. To determine the optimal conditions for generating 68Ga-NOTA-ICG, various reaction parameters were implemented. Quality control analysis was performed using different chromatography techniques. The in vitro and in vivo stability was also measured at specific time points. The radioactivity ratio between n-octanol and water was determined to evaluate the water solubility of 68Ga-NOTA-ICG. The plasma-protein binding rate of the labelled compound was determined by the methanol method. The biodistribution and imaging findings were evaluated in normal animals at different time points after injection. A preliminary imaging evaluation was performed using an animal model of hepatic ischaemia-reperfusion injury, which was confirmed by pathology. Results. 68Ga-NOTA-ICG was prepared with very high radiochemical purity (>98%) by reacting at 90°C for 10 min at pH = 3.5∼4.0, with excellent stability in vivo and in vitro (>95% 3 h postpreparation). The in vitro plasma-protein binding rate of 68Ga-NOTA-ICG was 13.01 ± 0.7%, and it showed strong water solubility log P=−2.01±0.04. We found that in addition to excretion through the biliary tract and intestines, 68Ga-NOTA-ICG can be excreted through the urinary tract. The image quality of 68Ga-NOTA-ICG was very high; imaging agent retained in the area of liver injury could clearly be observed. Conclusion. This is the first report on a 68Ga-labelled NOTA-ICG fragment for liver reserve function studies. This complex has promise as a candidate agent for liver reserve imaging.

scholarly journals Probenecid: Its Chromatographic Determination, Plasma Protein Binding, and in vivo Pharmacokinetics in Dogs

2006 ◽  
Vol 68 (4) ◽  
pp. 361-365 ◽  
Author(s):  
Takehiko KAKIZAKI ◽  
Yukiko YOKOYAMA ◽  
Masahiro NATSUHORI ◽  
Azusa KARASAWA ◽  
Satoshi KUBO ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Chromatographic Determination ◽  
In Vivo Pharmacokinetics

scholarly journals In Vivo Microdialysis for Pharmacokinetic Investigations: A Plasma Protein Binding Study of Valproate in Rabbits.

1994 ◽  
Vol 17 (12) ◽  
pp. 1630-1634 ◽  
Author(s):  
Mikiro NAKASHIMA ◽  
Naoko TAKEUCHI ◽  
Motoko HAMADA ◽  
Kenji MATSUYAMA ◽  
Masataka ICHIKAWA ◽  
...  
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
In Vivo Microdialysis ◽  
Binding Study

Effects of NMDA receptor antagonists on visceromotor reflexes and on intestinal motility, in vivo

2007 ◽  
Vol 19 (7) ◽  
pp. 617-624 ◽  
Author(s):  
a. d. shafton ◽  
g. bogeski ◽  
p. d. kitchener ◽  
g. j. sanger ◽  
j. b. furness ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Intestinal Motility ◽  
Nmda Receptor Antagonists ◽  
Receptor Antagonists

In vitro and in vivo irreversible plasma protein binding of beclobric acid enantiomers

Chirality ◽  
1993 ◽  
Vol 5 (3) ◽  
pp. 120-125 ◽  
Author(s):  
Sascha Mayer ◽  
Ernst Mutschler ◽  
Hildegard Spahn-Langguth ◽  
Leslie Z. Benet
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein

scholarly journals Plasma protein binding of phenytoin in the aged: in vivo studies.

1982 ◽  
Vol 13 (3) ◽  
pp. 423-425 ◽  
Author(s):  
M Patterson ◽  
R Heazelwood ◽  
B Smithurst ◽  
MJ Eadie
Keyword(s):  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
In Vivo Studies

Correlation of in vitro and in vivo plasma protein binding using ultracentrifugation and UPLC-tandem mass spectrometry

The Analyst ◽  
2013 ◽  
Vol 138 (20) ◽  
pp. 6106 ◽  
Author(s):  
Cheruvu Hanumanth Srikanth ◽  
Tridib Chaira ◽  
Sunitha Sampathi ◽  
Sreekumar V. B. ◽  
Ramesh B. Bambal
Keyword(s):  
Mass Spectrometry ◽  
Tandem Mass Spectrometry ◽  
Protein Binding ◽  
Plasma Protein Binding ◽  
Plasma Protein ◽  
Tandem Mass
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