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Plasma protein binding and blood-free concentrations: which studies are needed to develop a drug?

Expert Opinion on Drug Metabolism & Toxicology, 2011
Introduction: The plasma protein binding of drugs and metabolites is known to influence their pharmacokinetics and, therefore, their effects. Evaluating the extent and the linearity of protein binding is an essential piece of information that has to be ...
M. Pellegatti   +3 more
semanticscholar   +1 more source

Predicting human plasma protein binding of drugs using plasma protein interaction QSAR analysis (PPI‐QSAR)

Biopharmaceutics & drug disposition, 2011
A novel method, named as the plasma protein‐interaction QSAR analysis (PPI‐QSAR) was used to construct the QSAR models for human plasma protein binding.
Haiyan Li   +6 more
semanticscholar   +1 more source

Plasma protein binding in drug discovery and development.

Combinatorial chemistry & high throughput screening, 2010
This review describes methods for quantifying the binding of small molecule drug candidates to plasma proteins and the application of these methods in drug discovery and development.
M. L. Howard   +3 more
semanticscholar   +1 more source

Impact of Hyperlipidemia on Plasma Protein Binding and Hepatic Drug Transporter and Metabolic Enzyme Regulation in a Rat Model of Gestational Diabetes

Journal of Pharmacology and Experimental Therapeutics, 2010
It is currently unknown whether gestational diabetes mellitus (GDM), a prevalent obstetrical complication, compounds the changes in drug disposition that occur naturally in pregnancy. Hyperlipidemia occurs in GDM.
G. Anger, M. Piquette-Miller
semanticscholar   +1 more source

Plasma Protein Binding

1992
Drugs used in anesthesia are all bound to a greater or lesser degree to plasma proteins. Plasma protein binding of drugs has a significant effect on their kinetics and dynamics. Variations of normal physiology and diseases affect both the concentrations and affinity of plasma proteins for drugs. This chapter provides a brief discussion of the relevance
openaire   +2 more sources

Binding of levonorgestrel to monkey plasma proteins

Experientia, 1983
3H-levonorgestrel, a protein progestational steroid, showed a high affinity saturable binding to monkey plasma. Competitive protein binding experiments suggested that the levonorgestrel binds to a protein which resembles sex hormone-binding globulin.
A. K. Srivastava, S. K. Roy
openaire   +3 more sources

Analysis of plasma proteins that bind to glycosaminoglycans

Biochimica et Biophysica Acta (BBA) - General Subjects, 2007
Glycosaminoglycan-binding proteins, with specific emphasis on dermatan sulfate, have been investigated in human plasma by affinity chromatography, mass spectrometry and Western blotting. Diluted plasma was applied to affinity columns and bound protein was eluted with 500 mM NaCl.
Akio Saito, Hiroshi Munakata
openaire   +3 more sources

Numerical solution of nonlinear pharmacokinetic equations: effects of plasma protein binding on drug distribution and elimination.

Journal of Pharmacy and Science, 1971
Numerical methods are described for the solution of the differential equations arising from nonlinear binding of drugs to plasma proteins, assuming one- and two-compartment pharmacokinetic models.
J. J. Coffey   +2 more
semanticscholar   +1 more source

Techniques for plasma protein binding of demethylchlorimipramine

Clinical Pharmacology & Therapeutics, 1979
The cerebrospinal fluid (CSF) and plasma levels of demethylchlorimipramine (DMC1) were determined during treatment of depression or obsessive‐compulsive disorders with chlorimipramine. In 18 patients the mean CSF/plasma ratio of DMCI was 2.6% ± 0.7 SD with fourfold variation (1.1% to 4.0%).
Mats Garle   +4 more
openaire   +3 more sources

Do we need to optimize plasma protein and tissue binding in drug discovery?

Current Topics in Medicinal Chemistry, 2011
It is a commonly accepted assumption that only unbound drug molecules are available to interact with their targets. In order to achieve high unbound plasma drug concentration, it seems obvious to design compounds with low plasma protein binding ...
Xingrong Liu, Cuiping Chen, C. Hop
semanticscholar   +1 more source

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