Matches in SemOpenAlex for { <https://semopenalex.org/work/W2109600293> ?p ?o ?g. }
- W2109600293 abstract "Neuropeptide Y2 (NPY2) receptors are implicated in diverse brain disorders, but no suitable PET radiotracers are currently available for studying NPY2 receptors in the living brain. We developed a novel positron-emitting radioligand based on the NPY2 receptor antagonist JNJ-31020028 (N-(4-(4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl)-3-fluorophenyl)-2-pyridin-3-ylbenzamide) and used the radiotracer for PET brain imaging in pigs.In vitro receptor autoradiography studies were performed to establish the anatomic distribution of NPY2 receptors in the pig brain. In vivo, baseline 90-min PET recordings of N-(11)C-methyl-JNJ-31020028 were conducted in anesthetized Yorkshire x Landrace pigs, concurrent with arterial blood sampling. Postchallenge scans were conducted after injection of unlabeled JNJ-31020028 as a pharmacologic intervention. Cyclosporine A was used to enhance levels of the PET radiotracer in the brain. The PET images were manually coregistered to a MR imaging atlas of the pig brain. Maps of the N-(11)C-methyl-JNJ-31020028 volume of distribution in the brain were prepared, and regional binding potentials of NPY2 receptors toward the radioligand were calculated using the simplified reference tissue method.In autoradiography studies, N-(11)C-methyl-JNJ-31020028 receptor binding sites were observed primarily in the hippocampus and were inhibited by unlabeled JNJ-31020028. In PET studies, N-(11)C-methyl-JNJ-31020028 was metabolized slowly in the bloodstream, with 25% of the (11)C-labeled parent compound remaining 30 min after injection. PET imaging showed baseline binding potentials of 0.64 ± 0.07 in the thalamus, 0.55 ± 0.02 in the caudate, and 0.49 ± 0.03 in the hippocampus. Graphical reference region analyses demonstrated that N-(11)C-methyl-JNJ-31020028 binding was reversible; infusion of unlabeled JNJ-31020028 markedly displaced the PET radioligand from binding sites in the hippocampus, thalamus, caudate nucleus, and cerebellum but not in the corpus callosum, which served as reference region for nonspecific binding.N-(11)C-methyl-JNJ-31020028 has several suitable properties for PET neuroimaging of NPY2 receptors. First, it is metabolized slowly in the bloodstream of pigs. Second, using cyclosporine, the target-to-background ratio of N-(11)C-methyl-JNJ-31020028 is sufficient for estimating pharmacokinetic parameters. Third, N-(11)C-methyl-JNJ-31020028 binds reversibly and competitively to cerebral sites known to contain relatively high numbers of NPY2 receptors, such as the hippocampus, thalamus, caudate nucleus, and cerebellum. Fourth, white matter such as corpus callosum, known to contain negligible numbers of NPY2 receptors, can serve as a reference region for estimating binding potentials in brain regions. To our knowledge, there is no other radioligand with these favorable properties and with this specificity for NPY2 receptors, which makes N-(11)C-methyl-JNJ-31020028 the first candidate radioligand for PET investigations of NPY2 receptors in the living brain." @default.
- W2109600293 created "2016-06-24" @default.
- W2109600293 creator A5009230887 @default.
- W2109600293 creator A5020392008 @default.
- W2109600293 creator A5030681439 @default.
- W2109600293 creator A5038074049 @default.
- W2109600293 creator A5039403483 @default.
- W2109600293 creator A5040511930 @default.
- W2109600293 creator A5062023062 @default.
- W2109600293 creator A5078197116 @default.
- W2109600293 creator A5080138773 @default.
- W2109600293 date "2014-03-10" @default.
- W2109600293 modified "2023-09-28" @default.
- W2109600293 title "PET Brain Imaging of Neuropeptide Y2 Receptors Using N-11C-Methyl-JNJ-31020028 in Pigs" @default.
- W2109600293 cites W1561005445 @default.
- W2109600293 cites W1976923417 @default.
- W2109600293 cites W1978013584 @default.
- W2109600293 cites W1991924547 @default.
- W2109600293 cites W1993990935 @default.
- W2109600293 cites W2009106508 @default.
- W2109600293 cites W2011444761 @default.
- W2109600293 cites W2034416686 @default.
- W2109600293 cites W2034975615 @default.
- W2109600293 cites W2035593869 @default.
- W2109600293 cites W2037708800 @default.
- W2109600293 cites W2037748200 @default.
- W2109600293 cites W2041624270 @default.
- W2109600293 cites W2052329451 @default.
- W2109600293 cites W2057672354 @default.
- W2109600293 cites W2068177011 @default.
- W2109600293 cites W2072565832 @default.
- W2109600293 cites W2072644024 @default.
- W2109600293 cites W2090573979 @default.
- W2109600293 cites W2109379016 @default.
- W2109600293 cites W2117671988 @default.
- W2109600293 cites W2127449611 @default.
- W2109600293 cites W2130053145 @default.
- W2109600293 cites W2169526301 @default.
- W2109600293 doi "https://doi.org/10.2967/jnumed.113.125351" @default.
- W2109600293 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24614224" @default.
- W2109600293 hasPublicationYear "2014" @default.
- W2109600293 type Work @default.
- W2109600293 sameAs 2109600293 @default.
- W2109600293 citedByCount "10" @default.
- W2109600293 countsByYear W21096002932015 @default.
- W2109600293 countsByYear W21096002932016 @default.
- W2109600293 countsByYear W21096002932018 @default.
- W2109600293 countsByYear W21096002932019 @default.
- W2109600293 countsByYear W21096002932020 @default.
- W2109600293 countsByYear W21096002932022 @default.
- W2109600293 crossrefType "journal-article" @default.
- W2109600293 hasAuthorship W2109600293A5009230887 @default.
- W2109600293 hasAuthorship W2109600293A5020392008 @default.
- W2109600293 hasAuthorship W2109600293A5030681439 @default.
- W2109600293 hasAuthorship W2109600293A5038074049 @default.
- W2109600293 hasAuthorship W2109600293A5039403483 @default.
- W2109600293 hasAuthorship W2109600293A5040511930 @default.
- W2109600293 hasAuthorship W2109600293A5062023062 @default.
- W2109600293 hasAuthorship W2109600293A5078197116 @default.
- W2109600293 hasAuthorship W2109600293A5080138773 @default.
- W2109600293 hasBestOaLocation W21096002931 @default.
- W2109600293 hasConcept C118303440 @default.
- W2109600293 hasConcept C118552586 @default.
- W2109600293 hasConcept C126322002 @default.
- W2109600293 hasConcept C150903083 @default.
- W2109600293 hasConcept C170493617 @default.
- W2109600293 hasConcept C185592680 @default.
- W2109600293 hasConcept C202751555 @default.
- W2109600293 hasConcept C207001950 @default.
- W2109600293 hasConcept C26291073 @default.
- W2109600293 hasConcept C2775842073 @default.
- W2109600293 hasConcept C2777670902 @default.
- W2109600293 hasConcept C2989005 @default.
- W2109600293 hasConcept C55493867 @default.
- W2109600293 hasConcept C60592354 @default.
- W2109600293 hasConcept C67847695 @default.
- W2109600293 hasConcept C71924100 @default.
- W2109600293 hasConcept C86803240 @default.
- W2109600293 hasConceptScore W2109600293C118303440 @default.
- W2109600293 hasConceptScore W2109600293C118552586 @default.
- W2109600293 hasConceptScore W2109600293C126322002 @default.
- W2109600293 hasConceptScore W2109600293C150903083 @default.
- W2109600293 hasConceptScore W2109600293C170493617 @default.
- W2109600293 hasConceptScore W2109600293C185592680 @default.
- W2109600293 hasConceptScore W2109600293C202751555 @default.
- W2109600293 hasConceptScore W2109600293C207001950 @default.
- W2109600293 hasConceptScore W2109600293C26291073 @default.
- W2109600293 hasConceptScore W2109600293C2775842073 @default.
- W2109600293 hasConceptScore W2109600293C2777670902 @default.
- W2109600293 hasConceptScore W2109600293C2989005 @default.
- W2109600293 hasConceptScore W2109600293C55493867 @default.
- W2109600293 hasConceptScore W2109600293C60592354 @default.
- W2109600293 hasConceptScore W2109600293C67847695 @default.
- W2109600293 hasConceptScore W2109600293C71924100 @default.
- W2109600293 hasConceptScore W2109600293C86803240 @default.
- W2109600293 hasLocation W21096002931 @default.
- W2109600293 hasLocation W21096002932 @default.
- W2109600293 hasOpenAccess W2109600293 @default.
- W2109600293 hasPrimaryLocation W21096002931 @default.
- W2109600293 hasRelatedWork W1994539986 @default.