Matches in SemOpenAlex for { <https://semopenalex.org/work/W1976735236> ?p ?o ?g. }
- W1976735236 endingPage "442" @default.
- W1976735236 startingPage "433" @default.
- W1976735236 abstract "While it is well established that opiate receptors up-regulate following chronic antagonist treatment in vivo, possible down-regulation following chronic agonist treatment remains controversial. In this study, rats received a continuous seven-day infusion of bremazocine. an opioid drug suggested to be a potent agonist at κ receptors and an antagonist at μ and δ receptors. Opiate receptor binding was assessed in both cryostat sections and homogenates of rat brain, under conditions selective for μ, δ and κ sites. Data from both sections and homogenates showed an increase in the capacity of μ binding sites following chronic bremazocine treatment, suggesting that up-regulation of μ receptors had occurred, and that residual ligand from the in vivo treatment had largely been removed. A significant decrease in κ binding was observed in sections, and experiments using homogenates demonstrated a dramatic loss of high-affinity κ binding, with an increase in low-affinity binding. There was no apparent alteration in binding to δ receptors. No significant changes were observed following acute injection of bremazocine. Quantitative light-microscopic autoradiography confirmed the results of the binding experiments, and showed that the magnitude of these effects varied between different brain regions. No decrease in κ binding was seen following chronic administration of the partial κ agonist nalorphine, indicating that high agonist intrinsic activity is necessary for down-regulation to occur. In addition, chronic co-administration ol bremazocine with the partial agonist/antagonist diprclorphine did not cause a significant decrease in κ binding, implying that diprenorphine can antagonize the down-regulatory effect. These results provide evidence that bremazocine possesses different degrees of intrinsic activity at μ, δ and κ receptors. They demonstrate that, at least in the case of κ sites, opiate receptors do show down-regulation following chronic agonist treatment in vivo." @default.
- W1976735236 created "2016-06-24" @default.
- W1976735236 creator A5012916525 @default.
- W1976735236 creator A5019734071 @default.
- W1976735236 date "1989-01-01" @default.
- W1976735236 modified "2023-10-14" @default.
- W1976735236 title "Control of opiate receptor numberin vivo: Simultaneous κ-receptor down-regulation and μ-receptor up-regulation following chronic agonist/antagonist treatment" @default.
- W1976735236 cites W1487442802 @default.
- W1976735236 cites W1582702727 @default.
- W1976735236 cites W1605904469 @default.
- W1976735236 cites W1966556269 @default.
- W1976735236 cites W1970844675 @default.
- W1976735236 cites W1971415798 @default.
- W1976735236 cites W1975216040 @default.
- W1976735236 cites W1978455948 @default.
- W1976735236 cites W1979385488 @default.
- W1976735236 cites W1985205546 @default.
- W1976735236 cites W1986130864 @default.
- W1976735236 cites W1986587759 @default.
- W1976735236 cites W1994224597 @default.
- W1976735236 cites W2008588702 @default.
- W1976735236 cites W2019552715 @default.
- W1976735236 cites W2027730590 @default.
- W1976735236 cites W2035711615 @default.
- W1976735236 cites W2038642833 @default.
- W1976735236 cites W2040390193 @default.
- W1976735236 cites W2044987726 @default.
- W1976735236 cites W2047858340 @default.
- W1976735236 cites W2048548721 @default.
- W1976735236 cites W2052957794 @default.
- W1976735236 cites W2054069282 @default.
- W1976735236 cites W2055194175 @default.
- W1976735236 cites W2057390595 @default.
- W1976735236 cites W2058558193 @default.
- W1976735236 cites W2063483021 @default.
- W1976735236 cites W2071087516 @default.
- W1976735236 cites W2074837694 @default.
- W1976735236 cites W2075322499 @default.
- W1976735236 cites W2080003856 @default.
- W1976735236 cites W2084442692 @default.
- W1976735236 cites W2088365056 @default.
- W1976735236 cites W2154942511 @default.
- W1976735236 cites W3220325 @default.
- W1976735236 cites W957480215 @default.
- W1976735236 doi "https://doi.org/10.1016/0306-4522(89)90070-5" @default.
- W1976735236 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2542839" @default.
- W1976735236 hasPublicationYear "1989" @default.
- W1976735236 type Work @default.
- W1976735236 sameAs 1976735236 @default.
- W1976735236 citedByCount "49" @default.
- W1976735236 countsByYear W19767352362017 @default.
- W1976735236 crossrefType "journal-article" @default.
- W1976735236 hasAuthorship W1976735236A5012916525 @default.
- W1976735236 hasAuthorship W1976735236A5019734071 @default.
- W1976735236 hasConcept C126322002 @default.
- W1976735236 hasConcept C134018914 @default.
- W1976735236 hasConcept C150903083 @default.
- W1976735236 hasConcept C170493617 @default.
- W1976735236 hasConcept C185592680 @default.
- W1976735236 hasConcept C207001950 @default.
- W1976735236 hasConcept C2776657501 @default.
- W1976735236 hasConcept C2776885963 @default.
- W1976735236 hasConcept C2778539182 @default.
- W1976735236 hasConcept C2778750930 @default.
- W1976735236 hasConcept C2778938600 @default.
- W1976735236 hasConcept C2779012664 @default.
- W1976735236 hasConcept C2779886867 @default.
- W1976735236 hasConcept C55493867 @default.
- W1976735236 hasConcept C71924100 @default.
- W1976735236 hasConcept C86803240 @default.
- W1976735236 hasConcept C98274493 @default.
- W1976735236 hasConceptScore W1976735236C126322002 @default.
- W1976735236 hasConceptScore W1976735236C134018914 @default.
- W1976735236 hasConceptScore W1976735236C150903083 @default.
- W1976735236 hasConceptScore W1976735236C170493617 @default.
- W1976735236 hasConceptScore W1976735236C185592680 @default.
- W1976735236 hasConceptScore W1976735236C207001950 @default.
- W1976735236 hasConceptScore W1976735236C2776657501 @default.
- W1976735236 hasConceptScore W1976735236C2776885963 @default.
- W1976735236 hasConceptScore W1976735236C2778539182 @default.
- W1976735236 hasConceptScore W1976735236C2778750930 @default.
- W1976735236 hasConceptScore W1976735236C2778938600 @default.
- W1976735236 hasConceptScore W1976735236C2779012664 @default.
- W1976735236 hasConceptScore W1976735236C2779886867 @default.
- W1976735236 hasConceptScore W1976735236C55493867 @default.
- W1976735236 hasConceptScore W1976735236C71924100 @default.
- W1976735236 hasConceptScore W1976735236C86803240 @default.
- W1976735236 hasConceptScore W1976735236C98274493 @default.
- W1976735236 hasIssue "2" @default.
- W1976735236 hasLocation W19767352361 @default.
- W1976735236 hasLocation W19767352362 @default.
- W1976735236 hasOpenAccess W1976735236 @default.
- W1976735236 hasPrimaryLocation W19767352361 @default.
- W1976735236 hasRelatedWork W1975774803 @default.
- W1976735236 hasRelatedWork W1976735236 @default.
- W1976735236 hasRelatedWork W1999249877 @default.
- W1976735236 hasRelatedWork W2007476630 @default.
- W1976735236 hasRelatedWork W2043808177 @default.