Results 81 to 90 of about 2,283,209 (217)

Do Brain Extracellular Fluid Concentrations Predict PET‐Inferred Receptor Occupancy in Human CNS? A Mechanistic Model‐Based Analysis of Dopamine D2 Receptor Ligands

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1389-1401, November 2026.
A mechanistic CNS PBPK model framework was applied to eight antipsychotic D2 receptor ligands, comparing brain extracellular fluid (brainECF) and brain cell membrane (brainM) as biophase for predicting human receptor occupancy compared against PET neuroimaging data. BrainM concentrations showed improved agreement with PET‐derived receptor occupancy for
Divakar Budda, J.G. Coen van Hasselt, Elizabeth C.M. de Lange   +2 more
wiley   +1 more source

RADIOLIGAND ASSAY FOR DETERMINING BIOTIN IN BIOLOGICAL FLUIDS

, 1987
A NEW RADIOLIGAND ASSAY FOR DETERMINING BIOTIN IN BIOLOGICAL FLUIDS IS DESCRIBED IN THIS STUDY. THE MAIN ASSAY REAGENTS ARE: A MIXTURE OF NB-(4-OH-3-125I-PHENYL)ETHYL] AND N-[B-(4-OH-3,5-DI- 125I-PHENYL)ETHYL] BIOTINAMIDES (RADIOTRACER),AVIDIN (BINDING ...
Λιβανίου, Ευαγγελία, Livaniou, Evangelia   +1 more
core   +1 more source

Qualifying a eukaryotic cell-free system for fluorescence based GPCR analyses

Scientific Reports, 2017
Membrane proteins are key elements in cell-mediated processes. In particular, G protein-coupled receptors (GPCRs) have attracted increasing interest since they affect cellular signaling.
Anne Zemella, Solveig Grossmann, Rita Sachse, Andrei Sonnabend, Michael Schaefer, Stefan Kubick   +5 more
doaj   +1 more source

Impact of correlated PBPK parameters on intra‐patient global sensitivity analysis in molecular radiotherapy

Medical Physics, Volume 53, Issue 11, November 2026.
Abstract Background Physiologically based pharmacokinetic (PBPK) models integrated into digital twins provide a robust framework for optimizing individualized molecular radiotherapy (MRT). Nevertheless, uncertainties in PBPK‐model‐derived dosimetry can compromise the reliability of dosimetry‐guided treatment planning and individualized therapy ...
Elham Yousefzadeh‐Nowshahr, Deni Hardiansyah, Valentina Vasic, Anna‐Lena Theisen, Johannes Tran‐Gia, Philipp E. Hartrampf, Ambros J. Beer, Michael Lassmann, Gerhard Glatting   +8 more
wiley   +1 more source

Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro

Frontiers in Pharmacology, 2018
It is now well established that GPR139, a G-protein coupled receptor exclusively expressed in the brain and pituitary, is activated by the essential amino acids L-tryptophan (L-Trp) and L-phenylalanine (L-Phe) via Gαq-coupling.
Diane Nepomuceno, Chester Kuei, Curt Dvorak, Timothy Lovenberg, Changlu Liu, Pascal Bonaventure   +5 more
doaj   +1 more source

Receptor kinetics: Binding flux‐based approaches offer complementary insight into how ligand binding evolves with time

British Journal of Pharmacology, Volume 183, Issue 21, Page 6444-6457, November 2026.
Background and Purpose Binding kinetics are essentially based on rate constants. Yet, this view has been challenged by the idea that ‘binding fluxes’ are dynamic and therefore more relevant. Those fluxes refer to the rate at which a target/receptor changes from one state into another through ligand/drug binding or a conformational change.
Georges Vauquelin, Terry Kenakin, Dominique Maes   +2 more
wiley   +1 more source

Overview of the detection methods for equilibrium dissociation constant KD of drug-receptor interaction

Journal of Pharmaceutical Analysis, 2018
Drug-receptor interaction plays an important role in a series of biological effects, such as cell proliferation, immune response, tumor metastasis, and drug delivery. Therefore, the research on drug-receptor interaction is growing rapidly.
Weina Ma, Liu Yang, Langchong He
doaj   +1 more source

Optimum conditions of radioligand receptor binding assay of ligands of benzodiazepine receptors.

Iranian journal of pharmaceutical research : IJPR, 2014
To obtain drugs which are more selective at benzodiazepine (BZD) receptors, design and synthesis of functionally selective ligands for BZD receptors is the current strategy of our pharmaceutical chemistry department. The affinity of newly synthesized ligands is assessed by radioligand receptor binding assays.
Ahmadi, Fatemeh, Dabirian, Sara, Faizi, Mehrdad, Tabatabai, Sayyed Abbas, Beiki, Davood, Shahhosseini, Soraya   +5 more
openaire   +2 more sources

Parkinson's disease under dopamine replacement therapy as a human framework for studying addiction‐relevant mechanisms

Psychiatry and Clinical Neurosciences, Volume 80, Issue 11, Page 877-888, November 2026.
Addiction is a chronic relapsing condition characterized by compulsive reward seeking and impaired behavioral control, associated with major individual and societal burden. Mechanistic investigation in humans remains constrained by ethical limitations, uncontrolled exposure histories, and ecological confounds.
Vanessa Fleury, Elvira Pirondini, Damien Benis, Tiffany Corbet, Gabriel Thorens, Christian Lüscher, Paul Krack   +6 more
wiley   +1 more source

Tuning the Triazolotriazine Scaffold Toward Selective A3 Adenosine Receptor Antagonists: From Molecular Recognition to Neuroprotection

ChemMedChem, Volume 21, Issue 20, 28 October 2026.
Structure‐based optimization of the triazolo‐triazine scaffold afforded highly potent and selective adenosine A3 receptor antagonists. Replacement of the classical 2‐furyl group with phenyl‐based substituents markedly improved A3 receptor affinity and selectivity.
Veronika Kost, Filippo Prencipe, Federica Panozzi, Veronica Salmaso, Sonja Kachler, Karl‐Norbert Klotz, Elisabetta Coppi, Simone Adorinni, Stefano Moro, Anna Maria Pugliese, Stephanie Federico, Giampiero Spalluto, Tatiana Da Ros   +12 more
wiley   +1 more source