FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2033913075> ?p ?o ?g. }

• W2033913075 endingPage "258" @default.
• W2033913075 startingPage "252" @default.
• W2033913075 abstract "YKP1358 is a novel serotonin (5-HT(2A)) and dopamine (D(2)) antagonist that, in preclinical studies, fits the general profile of an atypical antipsychotic. We conducted a D(2) receptor occupancy study with YKP1358 in healthy volunteers using positron emission tomography (PET) to measure the D(2) receptor occupancy of YKP1358 and to characterize its relationship to plasma drug concentrations. A single oral dose, parallel group, dose-escalation (100, 200, and 250 mg) study was performed in 10 healthy male volunteers with the PET radiotracer [(11)C]raclopride. The D(2) receptor occupancy of striatum was measured pre-dose, and at 2, 5, and 10 h after YKP1358 administration. Serial blood samples were taken for measurement of plasma YKP1358 concentrations. D(2) receptor occupancy by YKP1358 increased to 53-83% at 2 h, and then decreased afterwards, ranging from 40-64% at 5 h to 20-51% at 10 h. The YKP1358 dose-plasma concentration relationship exhibited extensive variability, but there was a good relationship between plasma concentrations and D(2) receptor occupancy that was well predicted by a sigmoid E(max) model using nonlinear mixed effects modeling. To our knowledge, this is the first study in which the relationship between plasma concentration and the biomarker of D(2) receptor occupancy was modeled using nonlinear mixed effects modeling. It is anticipated that these results will be useful in estimating for subsequent studies the initial doses of YKP1358 required to achieve a therapeutically effective range of D(2) receptor occupancy." @default.
• W2033913075 created "2016-06-24" @default.
• W2033913075 creator A5010511274 @default.
• W2033913075 creator A5022675590 @default.
• W2033913075 creator A5027055033 @default.
• W2033913075 creator A5038423084 @default.
• W2033913075 creator A5040240958 @default.
• W2033913075 creator A5049046758 @default.
• W2033913075 creator A5055187961 @default.
• W2033913075 creator A5064370332 @default.
• W2033913075 creator A5078125463 @default.
• W2033913075 creator A5079003243 @default.
• W2033913075 creator A5084357182 @default.
• W2033913075 creator A5090893923 @default.
• W2033913075 creator A5091100837 @default.
• W2033913075 date "2007-02-01" @default.
• W2033913075 modified "2023-09-27" @default.
• W2033913075 title "Modeling of Brain D2 Receptor Occupancy-Plasma Concentration Relationships with a Novel Antipsychotic, YKP1358, Using Serial PET Scans in Healthy Volunteers" @default.
• W2033913075 cites W1966108063 @default.
• W2033913075 cites W1976059310 @default.
• W2033913075 cites W1996065499 @default.
• W2033913075 cites W2032124712 @default.
• W2033913075 cites W2048327972 @default.
• W2033913075 cites W2069849124 @default.
• W2033913075 cites W2073066871 @default.
• W2033913075 cites W2078396129 @default.
• W2033913075 cites W2081308285 @default.
• W2033913075 cites W2082000302 @default.
• W2033913075 cites W2099185967 @default.
• W2033913075 cites W2117671988 @default.
• W2033913075 cites W2126097234 @default.
• W2033913075 cites W2130005921 @default.
• W2033913075 cites W2140734930 @default.
• W2033913075 cites W2152031628 @default.
• W2033913075 cites W2154181119 @default.
• W2033913075 cites W2159813162 @default.
• W2033913075 cites W2161570416 @default.
• W2033913075 cites W2163010981 @default.
• W2033913075 cites W2324227497 @default.
• W2033913075 doi "https://doi.org/10.1038/sj.clpt.6100049" @default.
• W2033913075 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17259948" @default.
• W2033913075 hasPublicationYear "2007" @default.
• W2033913075 type Work @default.
• W2033913075 sameAs 2033913075 @default.
• W2033913075 citedByCount "32" @default.
• W2033913075 countsByYear W20339130752012 @default.
• W2033913075 countsByYear W20339130752013 @default.
• W2033913075 countsByYear W20339130752014 @default.
• W2033913075 countsByYear W20339130752015 @default.
• W2033913075 countsByYear W20339130752017 @default.
• W2033913075 countsByYear W20339130752019 @default.
• W2033913075 countsByYear W20339130752021 @default.
• W2033913075 countsByYear W20339130752022 @default.
• W2033913075 crossrefType "journal-article" @default.
• W2033913075 hasAuthorship W2033913075A5010511274 @default.
• W2033913075 hasAuthorship W2033913075A5022675590 @default.
• W2033913075 hasAuthorship W2033913075A5027055033 @default.
• W2033913075 hasAuthorship W2033913075A5038423084 @default.
• W2033913075 hasAuthorship W2033913075A5040240958 @default.
• W2033913075 hasAuthorship W2033913075A5049046758 @default.
• W2033913075 hasAuthorship W2033913075A5055187961 @default.
• W2033913075 hasAuthorship W2033913075A5064370332 @default.
• W2033913075 hasAuthorship W2033913075A5078125463 @default.
• W2033913075 hasAuthorship W2033913075A5079003243 @default.
• W2033913075 hasAuthorship W2033913075A5084357182 @default.
• W2033913075 hasAuthorship W2033913075A5090893923 @default.
• W2033913075 hasAuthorship W2033913075A5091100837 @default.
• W2033913075 hasConcept C112705442 @default.
• W2033913075 hasConcept C126322002 @default.
• W2033913075 hasConcept C134018914 @default.
• W2033913075 hasConcept C160331591 @default.
• W2033913075 hasConcept C170493617 @default.
• W2033913075 hasConcept C185592680 @default.
• W2033913075 hasConcept C18903297 @default.
• W2033913075 hasConcept C2775842073 @default.
• W2033913075 hasConcept C2776885963 @default.
• W2033913075 hasConcept C2778122271 @default.
• W2033913075 hasConcept C2781069445 @default.
• W2033913075 hasConcept C2989005 @default.
• W2033913075 hasConcept C44208683 @default.
• W2033913075 hasConcept C71924100 @default.
• W2033913075 hasConcept C86803240 @default.
• W2033913075 hasConcept C98274493 @default.
• W2033913075 hasConceptScore W2033913075C112705442 @default.
• W2033913075 hasConceptScore W2033913075C126322002 @default.
• W2033913075 hasConceptScore W2033913075C134018914 @default.
• W2033913075 hasConceptScore W2033913075C160331591 @default.
• W2033913075 hasConceptScore W2033913075C170493617 @default.
• W2033913075 hasConceptScore W2033913075C185592680 @default.
• W2033913075 hasConceptScore W2033913075C18903297 @default.
• W2033913075 hasConceptScore W2033913075C2775842073 @default.
• W2033913075 hasConceptScore W2033913075C2776885963 @default.
• W2033913075 hasConceptScore W2033913075C2778122271 @default.
• W2033913075 hasConceptScore W2033913075C2781069445 @default.
• W2033913075 hasConceptScore W2033913075C2989005 @default.
• W2033913075 hasConceptScore W2033913075C44208683 @default.
• W2033913075 hasConceptScore W2033913075C71924100 @default.
• W2033913075 hasConceptScore W2033913075C86803240 @default.

• next