FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2056547085> ?p ?o ?g. }

• W2056547085 abstract "Three compounds that have been suggested to irreversibly inactivate beta-adrenergic receptors were studied: NHNPNBE [N-(2-hydroxy-3-[1-napthoxy]-propyl)-N-bromoacetylethylenediami ne], BAAM (bromoacetylalprenololmenthane), and Ro 3-7894 [1-(5-chloracetylaminobenzfuran-2-yl)-2-isopropylaminoethanol++ +]. Membranes of rat cerebral cortex were used as a source of predominantly beta 1-adrenergic receptors and membranes of rat cerebellum were used as a source of predominantly beta 2-adrenergic receptors. Beta-Adrenergic receptor binding sites were studied by Scatchard analysis of saturation isotherms of specific [125I]-pindolol ([125I]PIN) binding. NHNPNBE added to the incubation medium competitively inhibited specific [125I]PIN binding in both cerebellum and cerebral cortex with KI values of 1-2 microM in each tissue. After washout of membranes pretreated with NHNPNBE for 30 min at 37 degrees, no loss of specific [125I]PIN binding sites was observed in either cerebellum or cortex except at very high concentrations (30-100 microM). Ro 3-7894 caused a simple competitive inhibition of specific [125I]PIN binding in rat cerebellar membranes with a KI of approximately 14 microM, an effect which was reversed completely by washing. In cerebral cortex, Ro 3-7894 added to the incubation medium apparently decreased the density of [125I]PIN binding sites with an IC50 around 1 microM. This effect was reversed after washing the membranes twice. However, in the presence of Ro 3-7894 some Scatchard plots showed a slight curvature. Further saturation of the [125I]PIN binding sites in cerebral cortex showed that the inhibition by Ro 3-7894 was competitive but with a high- and low-affinity component, consistent with Ro 3-7894 being a beta 1-selective competitive antagonist. Ro 3-7894 was also beta 1-selective in other tissues. BAAM added to the incubation medium competitively inhibited specific [125I]PIN binding in both cerebellum and cortex with KI values of 0.006 to 0.03 microM, but was about 5-fold more potent in cerebellum. After treatment of membranes with higher concentrations of BAAM for 30 min at 37 degrees and washing twice, there was a dose-dependent decrease in the density of specific [125I]PIN binding sites with IC50 values of approximately 0.3 microM in both tissues. Similar effects were observed in rat heart. These data suggest that NHNPNBE is a simple competitive antagonist at both beta 1- and beta 2-adrenergic receptors except at very high concentrations. Ro 3-7894 is a beta 1-selective competitive antagonist with no apparent irreversible effects.(ABSTRACT TRUNCATED AT 400 WORDS)" @default.
• W2056547085 created "2016-06-24" @default.
• W2056547085 creator A5054874056 @default.
• W2056547085 creator A5072107420 @default.
• W2056547085 date "1986-03-01" @default.
• W2056547085 modified "2023-09-23" @default.
• W2056547085 title "Interactions of putatively irreversible antagonists with β1− and β2− adrenergic receptors" @default.
• W2056547085 cites W1487262298 @default.
• W2056547085 cites W1496691536 @default.
• W2056547085 cites W1982637660 @default.
• W2056547085 cites W1983649348 @default.
• W2056547085 cites W1989113118 @default.
• W2056547085 cites W1994782070 @default.
• W2056547085 cites W1996393830 @default.
• W2056547085 cites W1998514229 @default.
• W2056547085 cites W2008203547 @default.
• W2056547085 cites W2013283830 @default.
• W2056547085 cites W2024260091 @default.
• W2056547085 cites W2025112538 @default.
• W2056547085 cites W2031693500 @default.
• W2056547085 cites W2044235485 @default.
• W2056547085 cites W2047950711 @default.
• W2056547085 cites W2057532767 @default.
• W2056547085 cites W2071494953 @default.
• W2056547085 cites W2074631079 @default.
• W2056547085 cites W2081963773 @default.
• W2056547085 cites W2090983062 @default.
• W2056547085 cites W2412959987 @default.
• W2056547085 cites W4293247451 @default.
• W2056547085 doi "https://doi.org/10.1016/0006-2952(86)90255-8" @default.
• W2056547085 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2869757" @default.
• W2056547085 hasPublicationYear "1986" @default.
• W2056547085 type Work @default.
• W2056547085 sameAs 2056547085 @default.
• W2056547085 citedByCount "15" @default.
• W2056547085 crossrefType "journal-article" @default.
• W2056547085 hasAuthorship W2056547085A5054874056 @default.
• W2056547085 hasAuthorship W2056547085A5072107420 @default.
• W2056547085 hasConcept C107824862 @default.
• W2056547085 hasConcept C12554922 @default.
• W2056547085 hasConcept C126322002 @default.
• W2056547085 hasConcept C134018914 @default.
• W2056547085 hasConcept C170493617 @default.
• W2056547085 hasConcept C185592680 @default.
• W2056547085 hasConcept C25642318 @default.
• W2056547085 hasConcept C2778499207 @default.
• W2056547085 hasConcept C2779652256 @default.
• W2056547085 hasConcept C2781041448 @default.
• W2056547085 hasConcept C40465926 @default.
• W2056547085 hasConcept C41625074 @default.
• W2056547085 hasConcept C55493867 @default.
• W2056547085 hasConcept C71924100 @default.
• W2056547085 hasConcept C86803240 @default.
• W2056547085 hasConceptScore W2056547085C107824862 @default.
• W2056547085 hasConceptScore W2056547085C12554922 @default.
• W2056547085 hasConceptScore W2056547085C126322002 @default.
• W2056547085 hasConceptScore W2056547085C134018914 @default.
• W2056547085 hasConceptScore W2056547085C170493617 @default.
• W2056547085 hasConceptScore W2056547085C185592680 @default.
• W2056547085 hasConceptScore W2056547085C25642318 @default.
• W2056547085 hasConceptScore W2056547085C2778499207 @default.
• W2056547085 hasConceptScore W2056547085C2779652256 @default.
• W2056547085 hasConceptScore W2056547085C2781041448 @default.
• W2056547085 hasConceptScore W2056547085C40465926 @default.
• W2056547085 hasConceptScore W2056547085C41625074 @default.
• W2056547085 hasConceptScore W2056547085C55493867 @default.
• W2056547085 hasConceptScore W2056547085C71924100 @default.
• W2056547085 hasConceptScore W2056547085C86803240 @default.
• W2056547085 hasLocation W20565470851 @default.
• W2056547085 hasLocation W20565470852 @default.
• W2056547085 hasOpenAccess W2056547085 @default.
• W2056547085 hasPrimaryLocation W20565470851 @default.
• W2056547085 hasRelatedWork W1976438981 @default.
• W2056547085 hasRelatedWork W2024260091 @default.
• W2056547085 hasRelatedWork W2034583712 @default.
• W2056547085 hasRelatedWork W2052453588 @default.
• W2056547085 hasRelatedWork W2056547085 @default.
• W2056547085 hasRelatedWork W2063619316 @default.
• W2056547085 hasRelatedWork W2131377884 @default.
• W2056547085 hasRelatedWork W2315166476 @default.
• W2056547085 hasRelatedWork W2398764952 @default.
• W2056547085 hasRelatedWork W4289992546 @default.
• W2056547085 isParatext "false" @default.
• W2056547085 isRetracted "false" @default.
• W2056547085 magId "2056547085" @default.
• W2056547085 workType "article" @default.