Results are reported as the percentage of radioligand binding without addition of an agonist. (avma.org)
Herein we describe the synthesis and pharmacological characterization of the first GPR88 radioligand, [3H]RTI-33, derived from a synthetic agonist RTI-13951-33. (rti.org)
In comparison to fenretinide, A1120 did not act as a RARα agonist, while exhibiting superior in vitro potency in RBP4 binding and RBP4-TTR interaction assays. (arvojournals.org)
Vitro1
The present study utilized radioligand binding and immunoblotting techniques to compare in vitro DAT density and ligand affinity across a series of cell lines stably transfected with constructs containing the DAT1 coding region flanked downstream by one of four DAT1 3'UTR variants. (biomedcentral.com)
Specific3
3H]RTI-33 has a specific activity of 83.4 Ci/mmol and showed one-site, saturable binding (KD of 85 nM) in membranes prepared from stable PPLS-HA-hGPR88-CHO cells. (rti.org)
PBB5 showed specific binding to recombinant K18 tau fibrils by fluorescence assay, to post-mortem Alzheimer's disease brain tissue homogenate by competitive binding against [ 11 C]PBB3 and to tau deposits (AT-8 positive) in post-mortem corticobasal degeneration and progressive supranuclear palsy brains. (springer.com)
96% and specific activity of 308.3 TBq/mmol at the optimized conditions (pH of 3.5-4, ligand amount of 2.4 nmol, temperature of 90-95°C and reaction time of 10 min). (sinap.ac.cn)
Concentrations2
Determination of DPM is important for making conversions to calculate molar concentrations of radioligands, and it is also important if a comparison between different instruments is required. (nih.gov)
The specific activity of [3H]-CP55.940 (158 Ci mmol?1) was diluted with unlabelled CP55.940 to obtain final assay concentrations from 0.032 to 10 nM. (moca-09.org)
Receptor4
Functional luciferase reporter gene assays were performed to assess receptor activation in HeLa cells. (nih.gov)
The radioligand binding assay for the AII receptor is regarded as the primary method for the evaluation of AT $_1$ receptor antagonists for their activity. (koreascience.kr)
In this paper, we characterized the liver AT $_1$ receptor and describe the efficient method of the radioligand binding assay using rat liver as a source of AT $_1$ receptor. (koreascience.kr)
Most of the non-peptide tachykinin receptor antagonists described to date directly or indirectly arose out of large compound collection screening using a robust radioligand binding assay as the primary screen. (justia.com)
Biological2
Radioligand binding assays are a "work horse" in biological laboratories and have been adapted for HTS and lead optimization support in drug discovery. (nih.gov)
Biological assays with mammalian cells showed only a slight drop in cell viability (13%) at the highest concentration (1000 µM), while SNP exhibited an LC50 of 228 µM. (bvsalud.org)
Liver1
To further study the pancreatic effect and glucose utilization, plasma insulin concentration, insulin secreted from isolated rat islets and liver glycogen were assayed. (biomedcentral.com)
Describe1
The purpose of this chapter is to 1) describe common calculations used in radioligand binding assays and 2) outline steps for setting up and using microplate scintillation counters (Microbeta Trilux and TopCount). (nih.gov)
Assess1
Translocator protein (TSPO) targeting positron emission tomography (PET) imaging radioligands have potential utility in epilepsy to assess the efficacy of novel therapeutics for targeting neuroinflammation. (frontiersin.org)
Cells1
Moreover, IK-175 led to a decrease in suppressive IL17A - , IL-22 + expressing T cells in a Th17 differentiation assay. (aacrjournals.org)