Results 21 to 30 of about 2,283,209 (217)

Artificial tissue binding models : development and comparative evaluation of high - throughput lipophilicity assays and their use for PET tracer optimization [PDF]

, 2015
The purpose of this thesis was to increase the efficiency of the Positron Emission Tomography (PET) tracer development process. Since many neuroimaging agents fail due to undesirably high non-specific binding (NSB) to brain tissue, we aimed at estimating
Assmus, Frauke
core   +1 more source

Design and validation of recombinant protein standards for quantitative Western blot analysis of cannabinoid CB1 receptor density in cell membranes: an alternative to radioligand binding methods

Microbial Cell Factories, 2022
Background Replacement of radioligand binding assays with antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR) levels requires the use of purified protein standards containing the antigen.
Miquel Saumell-Esnaola, Ainhoa Elejaga-Jimeno, Leyre Echeazarra, Leire Borrega-Román, Sergio Barrondo, Maider López de Jesús, Imanol González-Burguera, Alberto Gómez-Caballero, María Aranzazu Goicolea, Joan Sallés, Gontzal García del Caño   +10 more
doaj   +1 more source

Synthesis, Biological Evaluation, and Docking Studies of Antagonistic Hydroxylated Arecaidine Esters Targeting mAChRs

Molecules, 2022
The muscarinic acetylcholine receptor family is a highly sought-after target in drug and molecular imaging discovery efforts aimed at neurological disorders.
Jonas Kilian, Marlon Millard, Marius Ozenil, Dominik Krause, Khadija Ghaderi, Wolfgang Holzer, Ernst Urban, Helmut Spreitzer, Wolfgang Wadsak, Marcus Hacker, Thierry Langer, Verena Pichler   +11 more
doaj   +1 more source

Characterization of muscarinic receptor binding by the novel radioligand, [3H]imidafenacin, in the bladder and other tissues of rats

Journal of Pharmacological Sciences, 2016
The present study aimed to directly characterize specific binding sites of tritium ([3H])-labeled imidafenacin, a new radioligand for labeling muscarinic receptors, in the bladder and other peripheral or central nervous tissues of rats.
Shiori Kuraoka, Yoshihiko Ito, Hirokazu Wakuda, Kazumasa Shinozuka, Satomi Onoue, Shizuo Yamada   +5 more
doaj   +1 more source

Oxytocin receptor binding sites in the periphery of the neonatal mouse. [PDF]

PLoS ONE, 2017
Oxytocin (OXT) is a pleiotropic regulator of physiology and behavior. An emerging body of evidence demonstrates a role for OXT in the transition to postnatal life of the infant. To identify potential sites of OXT action via the OXT receptor (OXTR) in the
Maria A Greenwood, Elizabeth A D Hammock
doaj   +1 more source

Newly Synthesized Fluorinated Cinnamylpiperazines Possessing Low In Vitro MAO-B Binding

Molecules, 2020
Herein, we report on the synthesis and pharmacological evaluation of ten novel fluorinated cinnamylpiperazines as potential monoamine oxidase B (MAO-B) ligands. The designed derivatives consist of either cinnamyl or 2-fluorocinnamyl moieties connected to
Ivana I. Jevtić, Thu Hang Lai, Jelena Z. Penjišević, Sladjana Dukić-Stefanović, Deana B. Andrić, Peter Brust, Sladjana V. Kostić-Rajačić, Rodrigo Teodoro   +7 more
doaj   +1 more source

SPECT/CT Imaging, Biodistribution and Radiation Dosimetry of a 177Lu-DOTA-Integrin αvβ6 Cystine Knot Peptide in a Pancreatic Cancer Xenograft Model

Frontiers in Oncology, 2021
IntroductionPancreatic ductal adenocarcinoma (PDAC) is one of the most aggressive malignant neoplasms, as many cases go undetected until they reach an advanced stage. Integrin αvβ6 is a cell surface receptor overexpressed in PDAC.
Sachindra Sachindra, Teresa Hellberg, Samantha Exner, Sonal Prasad, Sonal Prasad, Nicola Beindorff, Stephan Rogalla, Richard Kimura, Sanjiv Sam Gambhir, Bertram Wiedenmann, Carsten Grötzinger, Carsten Grötzinger, Carsten Grötzinger, Carsten Grötzinger   +13 more
doaj   +1 more source

Optical Control of the Glucocorticoid Receptor Activity With a Photoswitchable Agonist

Angewandte Chemie, EarlyView.
A photoswitchable glucocorticoid receptor agonist enables optical control of receptor activity, achieving picomolar potency and partial agonism that preferentially maintains anti‐inflammatory signaling over canonical transcriptional activation. ABSTRACT Glucocorticoids (GCs) are widely prescribed anti‐inflammatory agents whose clinical utility is ...
Zoe Sessions, Chloé Van Leene, Dorien Clarisse, George Keen, Agnė Šveistytė, Dinahlee Saturnino Guarino, Robert H. Mach, Karolien De Bosscher, Dirk Trauner   +8 more
wiley   +2 more sources

Development of a Radioligand Binding Assay for Detection of Gastrin/CCKB Receptors in the Human Gastrointestinal Tract [PDF]

, 1996
The initial strategy of the thesis (Chapter 3) examined the presence and characterisation of gastrin/CCKB receptors in the rat pancreatic cell line, AR42J. This cell line was chosen due to its continuous expression of high affinity gastrin/CCKB receptors
Mackenzie, Janet Fraser
core   +6 more sources

Engineered Mutation of Some Important Amino Acids in Angiotensin II Type 1 (AT1) Receptor Increases the Binding Affinity of AT1-Receptor Antagonists

Journal of Pharmacological Sciences, 2010
The present study was designed to examine the binding affinity and functional potency of selective angiotensin II type 1 (AT1)-receptor antagonists towards specific mutants of AT1 receptor using site-directed mutagenesis.
Mohiuddin Ahmed Bhuiyan, Murad Hossain, Masaji Ishiguro, Takashi Nakamura, Takafumi Nagatomo   +4 more
doaj   +1 more source