Novel 18F-labeled κ-opioid receptor antagonist as PET radiotracer: synthesis and in vivo evaluation of 18F-LY2459989 in nonhuman primates
The κ-opioid receptor (KOR) has been implicated in depression, addictions, and other
central nervous system disorders and, thus, is an important target for drug development. We …
central nervous system disorders and, thus, is an important target for drug development. We …
An improved antagonist radiotracer for the κ-opioid receptor: synthesis and characterization of 11C-LY2459989
The κ-opioid receptors (KORs) are implicated in several neuropsychiatric diseases and
addictive disorders. PET with radioligands provides a means to image the KOR in vivo and …
addictive disorders. PET with radioligands provides a means to image the KOR in vivo and …
Synthesis and evaluation of 11C-LY2795050 as a κ-opioid receptor antagonist radiotracer for PET imaging
Kappa-opioid receptors (KOR) are believed to be involved in the pathophysiology of
depression, anxiety disorders, drug abuse, and alcoholism. To date, only 1 tracer, the KOR …
depression, anxiety disorders, drug abuse, and alcoholism. To date, only 1 tracer, the KOR …
Development and in vivo evaluation of a κ-opioid receptor agonist as a PET radiotracer with superior imaging characteristics
Studies have shown κ-opioid receptor (KOR) abnormalities in addictive disorders, other
central nervous system diseases, and Alzheimer's disease. We have developed the first set …
central nervous system diseases, and Alzheimer's disease. We have developed the first set …
Determination of in vivo Bmax and Kd for 11C-GR103545, an agonist PET tracer for κ-opioid receptors: a study in nonhuman primates
The κ-opioid receptors (KOR) are involved in mood disorders and addictive conditions. In
vivo imaging studies of this receptor in humans have not been reported because of the lack …
vivo imaging studies of this receptor in humans have not been reported because of the lack …
Kinetic Modeling and Test–Retest Reproducibility of 11C-EKAP and 11C-FEKAP, Novel Agonist Radiotracers for PET Imaging of the κ-Opioid Receptor in Humans
The κ-opioid receptor (KOR) is implicated in various neuropsychiatric disorders. We
previously evaluated an agonist tracer, 11C-GR103545, for PET imaging of KOR in humans …
previously evaluated an agonist tracer, 11C-GR103545, for PET imaging of KOR in humans …
11C-GR103545, a Radiotracer for Imagingκ-Opioid Receptors In Vivo with PET: Synthesis and Evaluation in Baboons
PS Talbot, R Narendran, ER Butelman… - Journal of Nuclear …, 2005 - Soc Nuclear Med
Brain κ-opioid receptors (ORs) may be involved in several pathologic conditions, such as
addiction, psychosis, and seizures.(±)-4-Methoxycarbonyl-2-[(1-pyrrolidinylmethyl]-1-[(3, 4 …
addiction, psychosis, and seizures.(±)-4-Methoxycarbonyl-2-[(1-pyrrolidinylmethyl]-1-[(3, 4 …
Novel kappa opioid receptor agonist as improved PET radiotracer: Development and in vivo evaluation
The kappa opioid receptor (KOR) is involved in depression, alcoholism, and drug abuse.
The current agonist radiotracer 11C-GR103545 is not ideal for imaging KOR due to its slow …
The current agonist radiotracer 11C-GR103545 is not ideal for imaging KOR due to its slow …
Determination of the in vivo selectivity of a new κ-opioid receptor antagonist PET tracer 11C-LY2795050 in the rhesus monkey
11C-LY2795050 is a novel κ-selective antagonist PET tracer. The in vitro binding affinities (K
i) of LY2795050 at the κ-opioid (KOR) and μ-opioid (MOR) receptors are 0.72 and 25.8 nM …
i) of LY2795050 at the κ-opioid (KOR) and μ-opioid (MOR) receptors are 0.72 and 25.8 nM …
Test–retest reproducibility of binding parameters in humans with 11C-LY2795050, an antagonist PET radiotracer for the κ opioid receptor
11C-LY2795050 is a new antagonist PET radioligand for the κ opioid receptor (KOR). In this
study, we assessed the reproducibility of the binding parameters of 11C-LY2795050 in …
study, we assessed the reproducibility of the binding parameters of 11C-LY2795050 in …
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