Expanding the Clinical Cytometry Toolbox—Receptor Occupancy by Mass Cytometry
Sign Up to like & getrecommendations! Published in 2019 at "Cytometry Part A"
DOI: 10.1002/cyto.a.23784
Abstract: DETERMINATION of the optimal therapeutic dose is a key challenge in drug development. Receptor occupancy assays (RO assays) measure the binding of biotherapeutics to their cellular targets and are one of the tools used to… read more here.
Keywords: occupancy; mass cytometry; receptor occupancy; cell ... See more keywords
Pharmacological MRI responses of raclopride in rats: The relationship with D2 receptor occupancy and cataleptic behavior
Sign Up to like & getrecommendations! Published in 2020 at "Synapse"
DOI: 10.1002/syn.22180
Abstract: Pharmacological magnetic resonance imaging (phMRI) allows the visualization of brain pharmacological effects of drugs using functional MRI (fMRI). phMRI can help us facilitate central nervous system (CNS) drug development. However, there have been few studies… read more here.
Keywords: receptor; receptor occupancy; responses raclopride; cataleptic behavior ... See more keywords
Binding of the D3-preferring antipsychotic candidate F17464 to dopamine D3 and D2 receptors: a PET study in healthy subjects with [11C]-(+)-PHNO
Sign Up to like & getrecommendations! Published in 2019 at "Psychopharmacology"
DOI: 10.1007/s00213-019-05387-w
Abstract: F17464, a dopamine D3 receptor antagonist with relatively high D3 selectivity (70 fold vs D2 in vitro), exhibits an antipsychotic profile in preclinical studies, and therapeutic efficacy was demonstrated in a randomized placebo-controlled clinical trial… read more here.
Keywords: receptor occupancy; study healthy; 11c phno; f17464 dopamine ... See more keywords
NK1 receptor antagonists for depression: Why a validated concept was abandoned.
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DOI: 10.1016/j.jad.2017.07.042
Abstract: BACKGROUND NK1 receptor antagonists were abandoned despite antidepressant efficacy in five randomized clinical trials. The loss of confidence may be attributed to the failure of a Phase III clinical program with the NK1 receptor antagonist… read more here.
Keywords: depression; receptor occupancy; nk1 receptor; receptor antagonists ... See more keywords
A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy
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DOI: 10.1038/s41598-017-00104-z
Abstract: CC Chemokine Receptor 2 (CCR2) and its endogenous ligand CCL2 are involved in a number of diseases, including atherosclerosis. Several CCR2 antagonists have been developed as potential therapeutic agents, however their in vivo clinical efficacy… read more here.
Keywords: high receptor; ccr2; receptor occupancy; novel ccr2 ... See more keywords
Effects of the sigma-1 receptor agonist blarcamesine in a murine model of fragile X syndrome: neurobehavioral phenotypes and receptor occupancy
Sign Up to like & getrecommendations! Published in 2021 at "Scientific Reports"
DOI: 10.1038/s41598-021-94079-7
Abstract: Fragile X syndrome (FXS), a disorder of synaptic development and function, is the most prevalent genetic form of intellectual disability and autism spectrum disorder. FXS mouse models display clinically-relevant phenotypes, such as increased anxiety and… read more here.
Keywords: fxs; fragile syndrome; receptor occupancy; receptor ... See more keywords
Predicting the dopamine D2 receptor occupancy of ropinirole in rats using positron emission tomography and pharmacokinetic–pharmacodynamic modeling
Sign Up to like & getrecommendations! Published in 2019 at "Xenobiotica"
DOI: 10.1080/00498254.2018.1428383
Abstract: Abstract 1. The purpose of this study was to measure dopamine D2/3 receptor occupancy (RO) as a marker of the clinical efficacy of ropinirole in rats via positron emission tomography (PET) using 18F-fallypride as the… read more here.
Keywords: ropinirole; receptor occupancy; pharmacokinetic pharmacodynamic; dopamine receptor ... See more keywords
Flow cytometry and receptor occupancy in immune-oncology therapy.
Sign Up to like & getrecommendations! Published in 2021 at "Expert opinion on biological therapy"
DOI: 10.1080/14712598.2021.1944098
Abstract: INTRODUCTION Immunotherapies are focused on strategies that alter immune responses, using antibodies that binds to receptors on different immune cell subsets and either activate or suppress their functions depending on the immune response being targeted.… read more here.
Keywords: receptor occupancy; pharmacology; flow cytometry; occupancy ... See more keywords
Receptor occupancy assessment and interpretation in terms of quantitative systems pharmacology: nivolumab case study
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DOI: 10.1080/19420862.2022.2156317
Abstract: ABSTRACT Receptor occupancy assays applied in clinical studies provide insights into pharmacokinetic-pharmacodynamic relationships for therapeutic antibodies. When measured by different assays, however, receptor occupancy results can be controversial, as was observed for nivolumab, a monoclonal… read more here.
Keywords: systems pharmacology; pharmacology; quantitative systems; receptor occupancy ... See more keywords
Dopamine D2 Receptor Occupancy Estimated From Plasma Concentrations of Four Different Antipsychotics and the Subjective Experience of Physical and Mental Well-Being in Schizophrenia: Results From the Randomized NeSSy Trial.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Clinical Psychopharmacology"
DOI: 10.1097/jcp.0000000000001131
Abstract: BACKGROUND Impaired subjective well-being in schizophrenia patients treated with antipsychotics has often been linked inter alia to the antidopaminergic effects of medication. Thus, it is important to capture the association between striatal dopamine D2 receptor… read more here.
Keywords: subjective well; occupancy; receptor occupancy; mental well ... See more keywords
MAP Bayesian modelling combining striatal dopamine receptor occupancy and plasma concentrations to optimize antipsychotic dose regimens in individual patients
Sign Up to like & getrecommendations! Published in 2022 at "British Journal of Clinical Pharmacology"
DOI: 10.1111/bcp.15260
Abstract: Develop a robust and user‐friendly software tool for the prediction of dopamine D2 receptor occupancy (RO) in patients with schizophrenia treated with either olanzapine or risperidone, in order to facilitate clinician exploration of the impact… read more here.
Keywords: receptor occupancy; plasma; dopamine receptor;