scholarly journals Interspecies In Vitro Evaluation of Stereoselective Protein Binding for 3,4-Methylenedioxymethamphetamine

2017 ◽  
Vol 2017 ◽  
pp. 1-7
Author(s):  
Wan Raihana Wan Aasim ◽  
Soo Choon Tan ◽  
Siew Hua Gan
Keyword(s):  
Protein Binding ◽  
Human Plasma ◽  
In Vitro Studies ◽  
Mouse Serum ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Rat Serum ◽  
In Vitro Evaluation ◽  
Rats And Mice

Abuse of 3,4-methylenedioxymethamphetamine (MDMA) is becoming more common worldwide. To date, there is no information available on stereoselectivity of MDMA protein binding in humans, rats, and mice. Since stereoselectivity plays an important role in MDMA’s pharmacokinetics and pharmacodynamics, in this study we investigated its stereoselectivity in protein binding. The stereoselective protein binding ofrac-MDMA was investigated using two different concentrations (20 and 200 ng/mL) in human plasma and mouse and rat sera using an ultrafiltration technique. No significant stereoselectivity in protein binding was observed in both human plasma and rat serum; however, a significant stereoselective binding (p<0.05) was observed in mouse serum. Since the protein binding of MDMA in mouse serum is considerably lower than in humans and rats, caution should be exercised when using mice for in vitro studies involving MDMA.

scholarly journals In vitro and in vivo evaluation of hypothermia on pharmacokinetics and pharmacodynamics of nimodipine in rabbits

2017 ◽  
Vol 46 (1) ◽  
pp. 335-347 ◽  
Author(s):  
Yu-xing Fei ◽  
Tian-hong Zhang ◽  
Jing Zhao ◽  
He Ren ◽  
Ya-nan Du ◽  
...  
Keyword(s):  
Blood Flow ◽  
Cerebral Blood Flow ◽  
Protein Binding ◽  
Plasma Concentrations ◽  
Liver Microsomes ◽  
Intrinsic Clearance ◽  
Pharmacokinetics And Pharmacodynamics ◽  
In Vivo Evaluation

Objective To investigate the effect of hypothermia on the pharmacokinetics and pharmacodynamics of nimodipine in rabbits using in vivo and in vitro methods. Methods Five healthy New Zealand rabbits received a single dose of nimodipine (0.5 mg/kg) intravenously under normothermic and hypothermic conditions. Doppler ultrasound was used to monitor cerebral blood flow, vascular resistance, and heart rate. In vitro evaluations of protein binding, hepatocyte uptake and intrinsic clearance of liver microsomes at different temperatures were also conducted. Results Plasma concentrations of nimodipine were significantly higher in hypothermia than in normothermia. Nimodipine improved cerebral blood flow under both conditions, but had a longer effective duration during the hypothermic period. Low temperature decreased the intrinsic clearance of liver microsomes, with no change in protein binding or hepatocyte uptake of nimodipine. Conclusion Nimodipine is eliminated at a slower rate during hypothermia than during normothermia, mainly due to the decreased activity of cytochrome P450 enzymes. This results in elevated system exposure with little enhancement in pharmacological effect.

THE EFFECTS OF CALCIUM ON PROTEIN-BINDING AND METABOLISM OF ARGININE VASOPRESSIN IN RATS

1965 ◽  
Vol 32 (2) ◽  
pp. 141-151 ◽  
Author(s):  
M. W. SMITH ◽  
N. A. THORN
Keyword(s):  
Protein Binding ◽  
Calcium Chloride ◽  
Blood Volume ◽  
Arginine Vasopressin ◽  
Binding Sites ◽  
Blood Concentration ◽  
Blood Circulation ◽  
Volume Of Distribution ◽  
Rat Serum

SUMMARY Hypercalcaemia produced in rats by the intravenous injection of calcium chloride, slowed the rate of disappearance of injected vasopressin from the blood circulation. 24% of the vasopressin injected appeared in the urine of hypercalcaemic rats compared with 7 % in control animals. Vasopressin injected intravenously into control rats was distributed in a volume equal to the blood volume but when rats had been made hypercalcaemic, the theoretical volume of distribution was three to four times greater. Antidiuresis produced by injection of large doses of vasopressin into hydrated rats was little affected by changes in the blood concentration of calcium. Calcium chloride injected intravenously into hydrated rats resulted in a temporary antidiuresis. Experiments in vitro with Sephadex G-25 showed that both ox neurophysin and rat serum protein bind vasopressin and that calcium interferes with the binding. It is suggested that calcium can compete directly with vasopressin for acidic binding sites on proteins; that this can cause the release of vasopressin and alter the transport and possibly the rate of inactivation, of vasopressin.

Effects of etofibrate on platelet function: In vitro studies in human plasma

1980 ◽  
Vol 19 (3) ◽  
pp. 409-416 ◽  
Author(s):  
M.P. Ortega ◽  
C. Sunkel ◽  
M. Armijo ◽  
J.G. Priego
Keyword(s):  
Human Plasma ◽  
Platelet Function ◽  
In Vitro Studies

Tailoring acyclovir prodrugs with enhanced antiviral activity: rational design, synthesis, human plasma stability and in vitro evaluation

Amino Acids ◽  
2018 ◽  
Vol 50 (8) ◽  
pp. 1131-1143
Author(s):  
Radoslav L. Chayrov ◽  
Evgenios K. Stylos ◽  
Maria V. Chatziathanasiadou ◽  
Kiril N. Chuchkov ◽  
Aleksandra I. Tencheva ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Human Plasma ◽  
Rational Design ◽  
Plasma Stability ◽  
Design Synthesis ◽  
In Vitro Evaluation

Factors affecting the stability of tPA and PAI-1 during storage and handling of human plasma for in vitro studies

1990 ◽  
Vol 1 (5) ◽  
pp. 393-400 ◽  
Author(s):  
F. Hamon ◽  
C. Masson-Lunven ◽  
B. Boutiere ◽  
C. Boyer-Neumann ◽  
M. J. Larri??u ◽  
...  
Keyword(s):  
Human Plasma ◽  
In Vitro Studies ◽  
Factors Affecting ◽  
The Stability ◽  
Pai 1

Copper, nickel and zinc complexes of 3-acetyl coumarin thiosemicarbazone: Synthesis, characterization and in vitro evaluation of cytotoxicity and DNA/protein binding properties

Polyhedron ◽  
2017 ◽  
Vol 135 ◽  
pp. 26-35 ◽  
Author(s):  
K.N. Anees Rahman ◽  
Jebiti Haribabu ◽  
Chandrasekar Balachandran ◽  
Nattamai S.P. Bhuvanesh ◽  
Ramasamy Karvembu ◽  
...  
Keyword(s):  
Protein Binding ◽  
Zinc Complexes ◽  
Binding Properties ◽  
In Vitro Evaluation ◽  
Copper Nickel
Sign in / Sign up

Export Citation Format

Share Document