Results 211 to 220 of about 423,855 (249)
Oxygen equilibration dynamics in assisted reproductive technology embryo culture media. [PDF]
J Assist Reprod GenetKulkarni S +4 more
europepmc +1 more source
Update and reuse: Structure-guided nanobody evolution against SARS-CoV-2 escape. [PDF]
PLoS PathogBu F +13 more
europepmc +1 more source
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Influence of ampicillin elimination half-life on in-vitro bactericidal effect
Journal of Antimicrobial Chemotherapy, 1985Escherichia coli ATCC 12407 was exposed in an in-vitro kinetic model to multiple dose ampicillin regimens differing in simulated drug elimination half-life but with equal dosage intervals and similar dose levels. Bacterial sensitivity was monitored during drug exposure. Greater bactericidal effect was observed with long half-life regimens.
C A, White, R D, Toothaker
exaly +3 more sources
Molecular Pharmaceutics, 2019
A large variety of drugs bind effectively to melanin, and this binding influences their ocular pharmacokinetic and distribution profiles. We aimed to establish a correlation between in vitro melanin binding and in vivo ocular pharmacokinetics (PK). The extent of melanin binding in vitro was determined for a set of model drugs; binding kinetics and ...
Arto Urtti, Ruben Alvarez Sanchez
exaly +3 more sources
A large variety of drugs bind effectively to melanin, and this binding influences their ocular pharmacokinetic and distribution profiles. We aimed to establish a correlation between in vitro melanin binding and in vivo ocular pharmacokinetics (PK). The extent of melanin binding in vitro was determined for a set of model drugs; binding kinetics and ...
Arto Urtti, Ruben Alvarez Sanchez
exaly +3 more sources
ChemMedChem
A reliable prediction of the in vivo plasma half‐life of drug candidates, from easily accessible in vitro assays, is not yet possible. It is surmised that the existing models, which consider protein binding and metabolic clearance, will be improved if they also include the propensity of molecules to bind to cell membranes.
Carla Pou, Miralbell +4 more
exaly +3 more sources
A reliable prediction of the in vivo plasma half‐life of drug candidates, from easily accessible in vitro assays, is not yet possible. It is surmised that the existing models, which consider protein binding and metabolic clearance, will be improved if they also include the propensity of molecules to bind to cell membranes.
Carla Pou, Miralbell +4 more
exaly +3 more sources
Journal of Pharmaceutical Sciences, 2010
Optimizing pharmacokinetic properties to improve oral exposure is a common theme in modern drug discovery. In the present work, in vitro Caco-2 permeability and microsomal half-life screens were utilized in an effort to guide the structure-activity relationship in order to improve the pharmacokinetic properties of novel HIV-1 attachment inhibitors. The
Tao Wang, , Zheng Yang
exaly +3 more sources
Optimizing pharmacokinetic properties to improve oral exposure is a common theme in modern drug discovery. In the present work, in vitro Caco-2 permeability and microsomal half-life screens were utilized in an effort to guide the structure-activity relationship in order to improve the pharmacokinetic properties of novel HIV-1 attachment inhibitors. The
Tao Wang, , Zheng Yang
exaly +3 more sources
Drug Metabolism and Disposition, 1999
Twenty-nine drugs of disparate structures and physicochemical properties were used in an examination of the capability of human liver microsomal lability data ("in vitro T(1/2)" approach) to be useful in the prediction of human clearance. Additionally, the potential importance of nonspecific binding to microsomes in the in vitro incubation milieu for ...
R Scott Obach
exaly +3 more sources
Twenty-nine drugs of disparate structures and physicochemical properties were used in an examination of the capability of human liver microsomal lability data ("in vitro T(1/2)" approach) to be useful in the prediction of human clearance. Additionally, the potential importance of nonspecific binding to microsomes in the in vitro incubation milieu for ...
R Scott Obach
exaly +3 more sources
Determination of the apparent half-life of erythrocytes with radioactive 51Cr In vitro
Clinica Chimica Acta, 1961Abstract The uptake of sodium chromate-51Cr by normal erythrocytes was estimated in relation to the number of red cells per μl. It is shown that the 51Cr uptake in a haemolytic syndrome—not associated with an antigen-antibody syndrome—is always increased compared to the 51Cr uptake in the same number of normal erythrocytes per μl. This quotient—the Q-
E, van KAMPEN, W, HEERSPINK
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SHORT IN VITRO HALF‐LIFE OF THYMOPOIETIN 32–36 PENTAPEPTIDE IN HUMAN PLASMA
International Journal of Peptide and Protein Research, 1979Thymopoietin32–36(TP5) is a synthetic pentapeptide that has the biological activity of its parent molecule, the 49 amino acid thymic hormone thymopoietin. Tritiated thymopoietin32–36(3H‐TP5) was prepared by reductive tritiation of dibromotyrosyl‐TP5. The stability of3H‐TP5 in human plasma was studied by analyzing samples by thin‐layer chromatography at
J P, Tischio +4 more
openaire +2 more sources
Microchemical Journal, 2020
Abstract Metabolic stability plays a crucial role in assessing the safety of potential drug candidates. Assays to designate in vitro half-life are well established and are focused on phase I metabolism using human liver microsomes. However, such an assay can easily be modified to include phase II metabolism.
Szymon Ulenberg +6 more
openaire +2 more sources
Abstract Metabolic stability plays a crucial role in assessing the safety of potential drug candidates. Assays to designate in vitro half-life are well established and are focused on phase I metabolism using human liver microsomes. However, such an assay can easily be modified to include phase II metabolism.
Szymon Ulenberg +6 more
openaire +2 more sources