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NOP-1A

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https://www.readbyqxmd.com/read/27353045/occupancy-of-nociceptin-orphanin-fq-peptide-receptors-by-the-antagonist-ly2940094-in-rats-and-healthy-human-subjects
#1
Eyas Raddad, Amy Chappell, Jeffery Meyer, Alan Wilson, Charles E Ruegg, Johannes Tauscher, Michael A Statnick, Vanessa Barth, Xin Zhang, Steven J Verfaille
Therapeutic benefits from nociceptin opioid peptide receptor (NOP) antagonism were proposed for obesity, eating disorders, and depression. LY2940094 ([2-[4-[(2-chloro-4,4-difluoro-spiro[5H-thieno[2,3-c]pyran-7,4'-piperidine]-1'-yl)methyl]-3-methyl-pyrazol-1-yl]-3-pyridyl]methanol) is a novel, orally bioavailable, potent, and selective NOP antagonist. We studied NOP receptor occupancy (RO) after single oral LY2940094 doses in rat hypothalamus and human brain by use of liquid chromatography with tandem mass spectrometry (LC-MS/MS) (LSN2810397) and positron emission tomography (PET) ([(11)C]NOP-1A) tracers, respectively...
September 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/25873424/improved-models-for-plasma-radiometabolite-correction-and-their-impact-on-kinetic-quantification-in-pet-studies
#2
Matteo Tonietto, Mattia Veronese, Gaia Rizzo, Paolo Zanotti-Fregonara, Talakad G Lohith, Masahiro Fujita, Sami S Zoghbi, Alessandra Bertoldo
The quantification of dynamic positron emission tomography studies performed with arterial sampling usually requires correcting the input function for the presence of radiometabolites by using a model of the plasma parent fraction (PPf). Here, we show how to include the duration of radioligand injection in the PPf model formulations to achieve a more physiologic description of the plasma measurements. This formulation (here called convoluted model) was tested on simulated data and on three datasets with different parent kinetics: [(11)C]NOP-1A, [(11)C]MePPEP, and [(11)C](R)-rolipram...
September 2015: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/24225488/retest-imaging-of-11c-nop-1a-binding-to-nociceptin-orphanin-fq-peptide-nop-receptors-in-the-brain-of-healthy-humans
#3
Talakad G Lohith, Sami S Zoghbi, Cheryl L Morse, Maria D Ferraris Araneta, Vanessa N Barth, Nancy A Goebl, Johannes T Tauscher, Victor W Pike, Robert B Innis, Masahiro Fujita
[(11)C]NOP-1A is a novel high-affinity PET ligand for imaging nociceptin/orphanin FQ peptide (NOP) receptors. Here, we report reproducibility and reliability measures of binding parameter estimates for [(11)C]NOP-1A binding in the brain of healthy humans. After intravenous injection of [(11)C]NOP-1A, PET scans were conducted twice on eleven healthy volunteers on the same (10/11 subjects) or different (1/11 subjects) days. Subjects underwent serial sampling of radial arterial blood to measure parent radioligand concentrations...
February 15, 2014: NeuroImage
https://www.readbyqxmd.com/read/22312136/brain-and-whole-body-imaging-of-nociceptin-orphanin-fq-peptide-receptor-in-humans-using-the-pet-ligand-11c-nop-1a
#4
Talakad G Lohith, Sami S Zoghbi, Cheryl L Morse, Maria F Araneta, Vanessa N Barth, Nancy A Goebl, Johannes T Tauscher, Victor W Pike, Robert B Innis, Masahiro Fujita
UNLABELLED: Nociceptin/orphanin FQ peptide (NOP) receptor is a new class of opioid receptor that may play a pathophysiologic role in anxiety and drug abuse and is a potential therapeutic target in these disorders. We previously developed a high-affinity PET ligand, (11)C-NOP-1A, which yielded promising results in monkey brain. Here, we assessed the ability of (11)C-NOP-1A to quantify NOP receptors in human brain and estimated its radiation safety profile. METHODS: After intravenous injection of (11)C-NOP-1A, 7 healthy subjects underwent brain PET for 2 h and serial sampling of radial arterial blood to measure parent radioligand concentrations...
March 2012: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/21880575/brain-and-whole-body-imaging-in-rhesus-monkeys-of-11c-nop-1a-a-promising-pet-radioligand-for-nociceptin-orphanin-fq-peptide-receptors
#5
Yasuyuki Kimura, Masahiro Fujita, Jinsoo Hong, Talakad G Lohith, Robert L Gladding, Sami S Zoghbi, Johannes A Tauscher, Nancy Goebl, Karen S Rash, Zhaogen Chen, Concepcion Pedregal, Vanessa N Barth, Victor W Pike, Robert B Innis
UNLABELLED: Our laboratory developed (S)-3-(2'-fluoro-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran]-1-yl)-2-(2-fluorobenzyl)-N-methylpropanamide ((11)C-NOP-1A), a new radioligand for the nociceptin/orphanin FQ peptide (NOP) receptor, with high affinity (K(i), 0.15 nM) and appropriate lipophilicity (measured logD, 3.4) for PET brain imaging. Here, we assessed the utility of (11)C-NOP-1A for quantifying NOP receptors in the monkey brain and estimated the radiation safety profile of this radioligand based on its biodistribution in monkeys...
October 2011: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
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