FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2113143471> ?p ?o ?g. }

• W2113143471 endingPage "154" @default.
• W2113143471 startingPage "138" @default.
• W2113143471 abstract "The new phosphodiesterase 10A inhibitor (PDE10AI) JNJ-42314415 [3-[6-(2-methoxyethyl)pyridin-3-yl]-2-methyl-8-morpholin-4-ylimidazo[1,2-a]pyrazine] was compared with three reference PDE10AIs and eight dopamine 2 (D₂) receptor blockers. Despite displaying relatively low PDE10A activity in vitro, JNJ-42314415 was found to be a relatively potent and specific PDE10AI in vivo. The compound was devoid of effects on prolactin release and of receptor interactions associated with other commonly observed adverse effects of available antipsychotics. Similar to D₂ receptor blockers, the tested PDE10AIs antagonized stimulant-induced behavior and inhibited conditioned avoidance behavior; these effects were observed at doses close to the ED₅₀ for striatal PDE10A occupancy. Relative to the ED₅₀ for inhibition of apomorphine-induced stereotypy, PDE10AIs blocked conditioned avoidance behavior and behaviors induced by nondopaminergic stimulants (phencyclidine, scopolamine) more efficiently than did D₂ receptor blockers; however, they blocked behaviors induced by dopaminergic stimulants (apomorphine, <i>d</i>-amphetamine) less efficiently. PDE10AIs also induced less pronounced catalepsy than D₂ receptor blockers. The effects of PDE10A inhibition against dopaminergic stimulants and on catalepsy were potentiated by the D₁ antagonist SCH-23390 (8-chloro-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1<i>H</i>-3-benzazepin-7-ol), suggesting that enhancement of D₁ receptor-mediated neurotransmission contributes to the behavioral profile of PDE10AIs. By reducing dopamine D₂ and concomitantly potentiating dopamine D₁ receptor-mediated neurotransmission, PDE10AIs may show antipsychotic activity with an improved side-effect profile relative to D₂ receptor blockers. However, the clinical implications of this dual mechanism must be further explored." @default.
• W2113143471 created "2016-06-24" @default.
• W2113143471 creator A5003819577 @default.
• W2113143471 creator A5011863919 @default.
• W2113143471 creator A5023940497 @default.
• W2113143471 creator A5029049116 @default.
• W2113143471 creator A5039828157 @default.
• W2113143471 creator A5059028911 @default.
• W2113143471 creator A5067361882 @default.
• W2113143471 creator A5076010133 @default.
• W2113143471 creator A5082370713 @default.
• W2113143471 date "2014-01-13" @default.
• W2113143471 modified "2023-10-14" @default.
• W2113143471 title "Pharmacology of JNJ-42314415, a Centrally Active Phosphodiesterase 10A (PDE10A) Inhibitor: A Comparison of PDE10A Inhibitors with D₂ Receptor Blockers as Potential Antipsychotic Drugs" @default.
• W2113143471 cites W1916083706 @default.
• W2113143471 cites W1965030220 @default.
• W2113143471 cites W1966745290 @default.
• W2113143471 cites W1969089145 @default.
• W2113143471 cites W1969601547 @default.
• W2113143471 cites W1972278987 @default.
• W2113143471 cites W1975769625 @default.
• W2113143471 cites W1978546687 @default.
• W2113143471 cites W1978583856 @default.
• W2113143471 cites W1989167892 @default.
• W2113143471 cites W1999961963 @default.
• W2113143471 cites W2010764223 @default.
• W2113143471 cites W2014349109 @default.
• W2113143471 cites W2016380985 @default.
• W2113143471 cites W2021504413 @default.
• W2113143471 cites W2023405690 @default.
• W2113143471 cites W2033479196 @default.
• W2113143471 cites W2048024033 @default.
• W2113143471 cites W2055863987 @default.
• W2113143471 cites W2067788315 @default.
• W2113143471 cites W2068057735 @default.
• W2113143471 cites W2071403847 @default.
• W2113143471 cites W2082938271 @default.
• W2113143471 cites W2088763860 @default.
• W2113143471 cites W2092208995 @default.
• W2113143471 cites W2093855835 @default.
• W2113143471 cites W2096987707 @default.
• W2113143471 cites W2122503957 @default.
• W2113143471 cites W2124526332 @default.
• W2113143471 cites W2130392097 @default.
• W2113143471 cites W2143850783 @default.
• W2113143471 cites W2154017841 @default.
• W2113143471 cites W4254775916 @default.
• W2113143471 doi "https://doi.org/10.1124/jpet.113.211904" @default.
• W2113143471 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/24421319" @default.
• W2113143471 hasPublicationYear "2014" @default.
• W2113143471 type Work @default.
• W2113143471 sameAs 2113143471 @default.
• W2113143471 citedByCount "29" @default.
• W2113143471 countsByYear W21131434712014 @default.
• W2113143471 countsByYear W21131434712015 @default.
• W2113143471 countsByYear W21131434712016 @default.
• W2113143471 countsByYear W21131434712017 @default.
• W2113143471 countsByYear W21131434712018 @default.
• W2113143471 countsByYear W21131434712019 @default.
• W2113143471 countsByYear W21131434712020 @default.
• W2113143471 countsByYear W21131434712021 @default.
• W2113143471 countsByYear W21131434712022 @default.
• W2113143471 crossrefType "journal-article" @default.
• W2113143471 hasAuthorship W2113143471A5003819577 @default.
• W2113143471 hasAuthorship W2113143471A5011863919 @default.
• W2113143471 hasAuthorship W2113143471A5023940497 @default.
• W2113143471 hasAuthorship W2113143471A5029049116 @default.
• W2113143471 hasAuthorship W2113143471A5039828157 @default.
• W2113143471 hasAuthorship W2113143471A5059028911 @default.
• W2113143471 hasAuthorship W2113143471A5067361882 @default.
• W2113143471 hasAuthorship W2113143471A5076010133 @default.
• W2113143471 hasAuthorship W2113143471A5082370713 @default.
• W2113143471 hasConcept C120069818 @default.
• W2113143471 hasConcept C126322002 @default.
• W2113143471 hasConcept C137183658 @default.
• W2113143471 hasConcept C170493617 @default.
• W2113143471 hasConcept C181199279 @default.
• W2113143471 hasConcept C185592680 @default.
• W2113143471 hasConcept C2777525119 @default.
• W2113143471 hasConcept C2778851735 @default.
• W2113143471 hasConcept C2779917531 @default.
• W2113143471 hasConcept C2780476085 @default.
• W2113143471 hasConcept C2780948584 @default.
• W2113143471 hasConcept C513476851 @default.
• W2113143471 hasConcept C55493867 @default.
• W2113143471 hasConcept C62826618 @default.
• W2113143471 hasConcept C67018056 @default.
• W2113143471 hasConcept C71924100 @default.
• W2113143471 hasConcept C79418042 @default.
• W2113143471 hasConcept C98274493 @default.
• W2113143471 hasConceptScore W2113143471C120069818 @default.
• W2113143471 hasConceptScore W2113143471C126322002 @default.
• W2113143471 hasConceptScore W2113143471C137183658 @default.
• W2113143471 hasConceptScore W2113143471C170493617 @default.
• W2113143471 hasConceptScore W2113143471C181199279 @default.
• W2113143471 hasConceptScore W2113143471C185592680 @default.
• W2113143471 hasConceptScore W2113143471C2777525119 @default.
• W2113143471 hasConceptScore W2113143471C2778851735 @default.

• next