FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1275434546> ?p ?o ?g. }

• W1275434546 endingPage "262" @default.
• W1275434546 startingPage "253" @default.
• W1275434546 abstract "Phosphodiesterase 10A (PDE10A) plays a key role in the regulation of brain striatal signaling. A PET tracer for PDE10A may serve as a tool to evaluate PDE10A expression in vivo in central nervous system disorders with striatal pathology. Here, we further characterized the binding properties of a previously reported radioligand we developed for PDE10A, [(11)C]TZ1964B, in rodents and nonhuman primates (NHPs). The tritiated counterpart [(3)H]TZ1964B was used for in vitro binding characterizations in rat striatum homogenates and in vitro autoradiographic studies in rat brain slices. The carbon-11 labeled [(11)C]TZ1964B was utilized in the ex vivo autoradiography studies for the brain of rats and microPET imaging studies for the brain of NHPs. MicroPET scans of [(11)C]TZ1964B in NHPs were conducted at baseline, as well as with using a selective PDE10A inhibitor MP-10 for either pretreatment or displacement. The in vivo regional target occupancy (Occ) was obtained by pretreating with different doses of MP-10 (0.05-2.00 mg/kg). Both in vitro binding assays and in vitro autoradiographic studies revealed a nanomolar binding affinity of [(3)H]TZ1964B to the rat striatum. The striatal binding of [(3)H]TZ1964B and [(11)C]TZ1964B was either displaced or blocked by MP-10 in rats and NHPs. Autoradiography and microPET imaging confirmed that the specific binding of the radioligand was found in the striatum but not in the cerebellum. Blocking studies also confirmed the suitability of the cerebellum as an appropriate reference region. The binding potentials (BPND) of [(11)C]TZ1964B in the NHP striatum that were calculated using either the Logan reference model (LoganREF, 3.96 ± 0.17) or the simplified reference tissue model (SRTM, 4.64 ± 0.47), with the cerebellum as the reference region, was high and had good reproducibility. The occupancy studies indicated a MP-10 dose of 0.31 ± 0.09 mg/kg (LoganREF)/0.45 ± 0.17mg/kg (SRTM) occupies 50% striatal PDE10A binding sites. Studies in rats and NHPs demonstrated radiolabeled TZ1964B has a high binding affinity and good specificity for PDE10A, as well as favorable in vivo pharmacokinetic properties and binding profiles. Our data suggests that [(11)C]TZ1964B is a promising radioligand for in vivo imaging PDE10A in the brain of living subject." @default.
• W1275434546 created "2016-06-24" @default.
• W1275434546 creator A5004835193 @default.
• W1275434546 creator A5008417526 @default.
• W1275434546 creator A5029519704 @default.
• W1275434546 creator A5031804038 @default.
• W1275434546 creator A5036528352 @default.
• W1275434546 creator A5050656056 @default.
• W1275434546 creator A5061153948 @default.
• W1275434546 creator A5070606018 @default.
• W1275434546 creator A5082789515 @default.
• W1275434546 creator A5089327014 @default.
• W1275434546 date "2015-11-01" @default.
• W1275434546 modified "2023-10-14" @default.
• W1275434546 title "Preclinical evaluation of a promising C-11 labeled PET tracer for imaging phosphodiesterase 10A in the brain of living subject" @default.
• W1275434546 cites W1507818862 @default.
• W1275434546 cites W1733847523 @default.
• W1275434546 cites W1968619342 @default.
• W1275434546 cites W1975769625 @default.
• W1275434546 cites W1989283753 @default.
• W1275434546 cites W2009327907 @default.
• W1275434546 cites W2009687348 @default.
• W1275434546 cites W2012732096 @default.
• W1275434546 cites W2021504413 @default.
• W1275434546 cites W2023640367 @default.
• W1275434546 cites W2025935143 @default.
• W1275434546 cites W2038018468 @default.
• W1275434546 cites W2038476239 @default.
• W1275434546 cites W2038555389 @default.
• W1275434546 cites W2047108643 @default.
• W1275434546 cites W2051809205 @default.
• W1275434546 cites W2054420039 @default.
• W1275434546 cites W2054929374 @default.
• W1275434546 cites W2059110429 @default.
• W1275434546 cites W2063017390 @default.
• W1275434546 cites W2064890293 @default.
• W1275434546 cites W2073188580 @default.
• W1275434546 cites W2074639778 @default.
• W1275434546 cites W2078471544 @default.
• W1275434546 cites W2096833562 @default.
• W1275434546 cites W2107832652 @default.
• W1275434546 cites W2112278807 @default.
• W1275434546 cites W2117671988 @default.
• W1275434546 cites W2124327561 @default.
• W1275434546 cites W2136424883 @default.
• W1275434546 cites W2144036031 @default.
• W1275434546 cites W2165028799 @default.
• W1275434546 cites W2280279811 @default.
• W1275434546 doi "https://doi.org/10.1016/j.neuroimage.2015.07.049" @default.
• W1275434546 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4604036" @default.
• W1275434546 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26216275" @default.
• W1275434546 hasPublicationYear "2015" @default.
• W1275434546 type Work @default.
• W1275434546 sameAs 1275434546 @default.
• W1275434546 citedByCount "17" @default.
• W1275434546 countsByYear W12754345462016 @default.
• W1275434546 countsByYear W12754345462017 @default.
• W1275434546 countsByYear W12754345462018 @default.
• W1275434546 countsByYear W12754345462019 @default.
• W1275434546 countsByYear W12754345462021 @default.
• W1275434546 countsByYear W12754345462022 @default.
• W1275434546 crossrefType "journal-article" @default.
• W1275434546 hasAuthorship W1275434546A5004835193 @default.
• W1275434546 hasAuthorship W1275434546A5008417526 @default.
• W1275434546 hasAuthorship W1275434546A5029519704 @default.
• W1275434546 hasAuthorship W1275434546A5031804038 @default.
• W1275434546 hasAuthorship W1275434546A5036528352 @default.
• W1275434546 hasAuthorship W1275434546A5050656056 @default.
• W1275434546 hasAuthorship W1275434546A5061153948 @default.
• W1275434546 hasAuthorship W1275434546A5070606018 @default.
• W1275434546 hasAuthorship W1275434546A5082789515 @default.
• W1275434546 hasAuthorship W1275434546A5089327014 @default.
• W1275434546 hasBestOaLocation W12754345462 @default.
• W1275434546 hasConcept C126322002 @default.
• W1275434546 hasConcept C150903083 @default.
• W1275434546 hasConcept C169760540 @default.
• W1275434546 hasConcept C170493617 @default.
• W1275434546 hasConcept C181199279 @default.
• W1275434546 hasConcept C185592680 @default.
• W1275434546 hasConcept C202751555 @default.
• W1275434546 hasConcept C207001950 @default.
• W1275434546 hasConcept C26291073 @default.
• W1275434546 hasConcept C2779652256 @default.
• W1275434546 hasConcept C2780062018 @default.
• W1275434546 hasConcept C513476851 @default.
• W1275434546 hasConcept C55493867 @default.
• W1275434546 hasConcept C60592354 @default.
• W1275434546 hasConcept C62826618 @default.
• W1275434546 hasConcept C67847695 @default.
• W1275434546 hasConcept C71924100 @default.
• W1275434546 hasConcept C79418042 @default.
• W1275434546 hasConcept C86803240 @default.
• W1275434546 hasConcept C98274493 @default.
• W1275434546 hasConceptScore W1275434546C126322002 @default.
• W1275434546 hasConceptScore W1275434546C150903083 @default.
• W1275434546 hasConceptScore W1275434546C169760540 @default.
• W1275434546 hasConceptScore W1275434546C170493617 @default.
• W1275434546 hasConceptScore W1275434546C181199279 @default.

• next