Matches in SemOpenAlex for { <https://semopenalex.org/work/W2046404328> ?p ?o ?g. }
Showing items 1 to 100 of
100
with 100 items per page.
- W2046404328 abstract "1. The irreversible opioid receptor antagonist beta-chlornaltrexamine (beta-CNA) has been shown previously to have agonist activity in the guinea-pig ileum preparation. However, the receptor type or types mediating this effect have not been established. 2. In this study, the agonism of beta-CNA was investigated by use of the competitive antagonist 16-methylcyprenorphine (RX8008M). Non-cumulative concentration-effect curves for beta-CNA were displaced in a non-parallel fashion indicating that the agonism was mediated by both mu- and kappa-receptors. 3. In principle, expression of agonism by an irreversible receptor antagonist could compromise its use in estimating agonist dissociation constants (pKAs) due to desensitization operating in addition to receptor inactivation. For kappa-receptors, this possibility was checked by use of ethylketocyclazocine (EKC) to mimic the agonist effects of beta-CNA and test whether subsequent EKC concentration-effect curves were displaced. For mu-receptors it was necessary to perform more involved experiments in which [D-Ala2, MePhe4, Gly-ol5]enkephalin (DAGOL) was used as a standard agonist and its pKA was estimated under different conditions of beta-CNA incubation. 4. These analyses indicated that neither the mu- nor the kappa-receptor-mediated agonism of beta-CNA was associated with appreciable receptor desensitization. In turn it was concluded that the usefulness of beta-CNA as a pharmacological tool for the estimation of mu- and kappa-opioid receptor agonist dissociation constants is not compromised by the agonist effects that the compound demonstrates at these receptors." @default.
- W2046404328 created "2016-06-24" @default.
- W2046404328 creator A5016092938 @default.
- W2046404328 creator A5076330866 @default.
- W2046404328 date "1988-09-01" @default.
- W2046404328 modified "2023-09-23" @default.
- W2046404328 title "Estimation of opioid receptor agonist dissociation constants with β-chlornaltrexamine, an irreversible ligand which also displays agonism" @default.
- W2046404328 cites W1878046841 @default.
- W2046404328 cites W1964131185 @default.
- W2046404328 cites W1965132832 @default.
- W2046404328 cites W1974884991 @default.
- W2046404328 cites W1994909080 @default.
- W2046404328 cites W2018788131 @default.
- W2046404328 cites W2040825227 @default.
- W2046404328 cites W2046435944 @default.
- W2046404328 cites W2066482395 @default.
- W2046404328 cites W2073522296 @default.
- W2046404328 cites W2075189759 @default.
- W2046404328 cites W2075811628 @default.
- W2046404328 cites W2083476200 @default.
- W2046404328 cites W2269438443 @default.
- W2046404328 doi "https://doi.org/10.1111/j.1476-5381.1988.tb16569.x" @default.
- W2046404328 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1854139" @default.
- W2046404328 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2851350" @default.
- W2046404328 hasPublicationYear "1988" @default.
- W2046404328 type Work @default.
- W2046404328 sameAs 2046404328 @default.
- W2046404328 citedByCount "4" @default.
- W2046404328 crossrefType "journal-article" @default.
- W2046404328 hasAuthorship W2046404328A5016092938 @default.
- W2046404328 hasAuthorship W2046404328A5076330866 @default.
- W2046404328 hasBestOaLocation W20464043282 @default.
- W2046404328 hasConcept C126322002 @default.
- W2046404328 hasConcept C134018914 @default.
- W2046404328 hasConcept C14397066 @default.
- W2046404328 hasConcept C14527384 @default.
- W2046404328 hasConcept C170493617 @default.
- W2046404328 hasConcept C17744445 @default.
- W2046404328 hasConcept C184389661 @default.
- W2046404328 hasConcept C185592680 @default.
- W2046404328 hasConcept C199539241 @default.
- W2046404328 hasConcept C2776885963 @default.
- W2046404328 hasConcept C2777803847 @default.
- W2046404328 hasConcept C2778122271 @default.
- W2046404328 hasConcept C2778938600 @default.
- W2046404328 hasConcept C2779779143 @default.
- W2046404328 hasConcept C2779886867 @default.
- W2046404328 hasConcept C2781063702 @default.
- W2046404328 hasConcept C43587935 @default.
- W2046404328 hasConcept C55493867 @default.
- W2046404328 hasConcept C58732023 @default.
- W2046404328 hasConcept C71924100 @default.
- W2046404328 hasConcept C86803240 @default.
- W2046404328 hasConcept C86811712 @default.
- W2046404328 hasConcept C94625758 @default.
- W2046404328 hasConcept C98274493 @default.
- W2046404328 hasConceptScore W2046404328C126322002 @default.
- W2046404328 hasConceptScore W2046404328C134018914 @default.
- W2046404328 hasConceptScore W2046404328C14397066 @default.
- W2046404328 hasConceptScore W2046404328C14527384 @default.
- W2046404328 hasConceptScore W2046404328C170493617 @default.
- W2046404328 hasConceptScore W2046404328C17744445 @default.
- W2046404328 hasConceptScore W2046404328C184389661 @default.
- W2046404328 hasConceptScore W2046404328C185592680 @default.
- W2046404328 hasConceptScore W2046404328C199539241 @default.
- W2046404328 hasConceptScore W2046404328C2776885963 @default.
- W2046404328 hasConceptScore W2046404328C2777803847 @default.
- W2046404328 hasConceptScore W2046404328C2778122271 @default.
- W2046404328 hasConceptScore W2046404328C2778938600 @default.
- W2046404328 hasConceptScore W2046404328C2779779143 @default.
- W2046404328 hasConceptScore W2046404328C2779886867 @default.
- W2046404328 hasConceptScore W2046404328C2781063702 @default.
- W2046404328 hasConceptScore W2046404328C43587935 @default.
- W2046404328 hasConceptScore W2046404328C55493867 @default.
- W2046404328 hasConceptScore W2046404328C58732023 @default.
- W2046404328 hasConceptScore W2046404328C71924100 @default.
- W2046404328 hasConceptScore W2046404328C86803240 @default.
- W2046404328 hasConceptScore W2046404328C86811712 @default.
- W2046404328 hasConceptScore W2046404328C94625758 @default.
- W2046404328 hasConceptScore W2046404328C98274493 @default.
- W2046404328 hasLocation W20464043281 @default.
- W2046404328 hasLocation W20464043282 @default.
- W2046404328 hasLocation W20464043283 @default.
- W2046404328 hasLocation W20464043284 @default.
- W2046404328 hasOpenAccess W2046404328 @default.
- W2046404328 hasPrimaryLocation W20464043281 @default.
- W2046404328 hasRelatedWork W1975466551 @default.
- W2046404328 hasRelatedWork W2020502640 @default.
- W2046404328 hasRelatedWork W2046404328 @default.
- W2046404328 hasRelatedWork W2066678665 @default.
- W2046404328 hasRelatedWork W2077709555 @default.
- W2046404328 hasRelatedWork W2088539696 @default.
- W2046404328 hasRelatedWork W2110133277 @default.
- W2046404328 hasRelatedWork W2146835843 @default.
- W2046404328 hasRelatedWork W2220256369 @default.
- W2046404328 hasRelatedWork W2344216978 @default.
- W2046404328 isParatext "false" @default.
- W2046404328 isRetracted "false" @default.
- W2046404328 magId "2046404328" @default.
- W2046404328 workType "article" @default.