Results 301 to 310 of about 2,396,679 (391)

Preclinical Pharmacokinetic Evaluation of Mithramycin and Mithramycin SA Tryptophan-Conjugated Analog. [PDF]

Pharmaceutics
Niloy KK, Horn J, Bhuiyan NH, Shaaban KA, Bhosale SS, Prisinzano TE, Thorson JS, Rohr J, Leggas M.   +8 more
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Revisiting the role of Annexins in membrane trafficking. [PDF]

Cell Mol Life Sci
Grewal T, Gerke V, Nylandsted J, Rentero C, Enrich C.   +4 more
europepmc   +1 more source

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Plasma Protein Binding of Challenging Compounds

Journal of Pharmaceutical Sciences, 2015
Accurately determining fraction unbound (fu ) with currently available methods has been challenging for certain compounds. Inaccurate fu values can lead to the misinterpretation of important attributes of a drug candidate. Our analysis of over 2000 Pfizer drug discovery compounds showed no systematic bias in low or high fu precision using the ...
Li Di, Mark Niosi, Jian Lin, Shannon Cawley, Phillip D. Yates, Cheng Chang, Carrie Funk, Keith Riccardi   +7 more
openaire   +4 more sources

An update on the importance of plasma protein binding in drug discovery and development

Expert Opinion on Drug Discovery, 2021
Introduction: Plasma protein binding (PPB) remains a controversial topic in drug discovery and development. Fraction unbound (fu) is a critical parameter that needs to be measured accurately, because it has significant impacts on the predictions of drug ...
L. Di
semanticscholar   +1 more source

Optimizing a High-Throughput Solid-Phase Microextraction System to Determine the Plasma Protein Binding of Drugs in Human Plasma.

Analytical Chemistry, 2021
Plasma protein binding refers to the binding of a drug to plasma proteins after entering the body. The measurement of plasma protein binding is essential during drug development and in clinical practice, as it provides a more detailed understanding of ...
K. Roy, Emir Nazdrajić, O. Shimelis, M. J. Ross, Yong Chen, Hugh M Cramer, J. Pawliszyn   +6 more
semanticscholar   +1 more source

Plasma protein binding of ceftriaxone

Xenobiotica, 1987
1. The plasma protein binding characteristics of ceftriaxone, a new cephalosporin antibiotic, were determined in human, baboon, rabbit, dog and rat plasma. 2. The protein binding of ceftriaxone was similar and concentration-dependent in human, baboon, rabbit and rat plasma, being highly bound (90-95%) at low concentrations (less than 100 micrograms/ml)
W G Crouthamel, I. Bekersky, A C Popick
openaire   +3 more sources

Plasma protein binding of carbamazepine

Clinical Pharmacology & Therapeutics, 1975
The binding of carbamazepine to the pro teins of human plasma has been studied using ultrafiltration techniques. In vitro studies at 37° C showed the relation between concentration of unbound drug and total drug to be linear thraugh the range of total concentration of 5 to 50 µg/ml.
Hooper W.D., Dubetz D.K., Bochner F., Cotter L.M., Smith G.A., Eadie M.J., Tyrer J.H.   +6 more
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Plasma protein binding of norethisterone

Contraception, 1982
Norethisterone (NET) is transported in the blood stream bound to plasma proteins. It is generally believed that only the part of the hormone that is not bound to plasma proteins can exert biological activity. NET binds to albumin and, like other 19-nortestosterone derived progestins, it also binds to sex hormone binding globulin (SHBG).
Viveca Odlind, Arne Victor, Elof D. B. Johansson   +2 more
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Synthesis, Radiolabeling, and Characterization of Plasma Protein-Binding Ligands: Potential Tools for Modulation of the Pharmacokinetic Properties of (Radio)Pharmaceuticals.

Bioconjugate chemistry, 2017
The development of (radio)pharmaceuticals with favorable pharmacokinetic profiles is crucial for allowing the optimization of the imaging or therapeutic potential and the minimization of undesired side effects.
C. Müller, R. Farkas, F. Borgna, R. Schmid, M. Benešová, R. Schibli   +5 more
semanticscholar   +1 more source

The binding of chlorothiazide to plasma proteins

Biochimica et Biophysica Acta (BBA) - Protein Structure, 1971
Abstract Association constants and values for the enthalpy and entropy of binding of chlorothiazide to human serum albumin have been determined by a variety of methods. The influence of chlorothiazide binding on the plasma levels of the hypotensive drug pempidine has been considered.
A. Rosen, A. Breckenridge
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