FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2040935821> ?p ?o ?g. }

• W2040935821 endingPage "755" @default.
• W2040935821 startingPage "745" @default.
• W2040935821 abstract "1 We have studied the recovery of receptor binding and of isoprenaline-stimulated cyclic AMP responses after chronic (2–5 days) exposure of tissue-cultured living rat heart cells to several β-adrenoceptor antagonists. Most experiments were performed with [3H]- (±)-carazolol and [3H]-(±)-CGP 12177, as prototypes of high affinity lipophilic and hydrophilic ligands respectively. 2 Chronic antagonist treatment did not alter the total number of receptors nor did it cause intracellular accumulation of the ligands. 3 At the end of the treatment, radiolabeled antagonists were displaced either by ‘infinite’ dilution of the incubation medium or by competitive displacement with the non-labelled ligand (-)-timolol. In dilution assays dissociation of Carazolol from specific sites was biphasic with t1/2 values of 41 ± 14 and 219 ± 15 min. Dissociation of CGP 12177 was monophasic with t1/2 of 102 ± 2 min. 4 Timolol enhanced the dissociation rates of both radioligands and suppressed the slow phase of Carazolol dissociation. 5 Isoprenaline-stimulated cyclic AMP formation did not recover in parallel with the release of the two antagonists from receptor binding sites. To reach about 80% of control values for receptor availability or cyclic AMP response required 3 h and 24 h washout periods, respectively, after Carazolol (0.2 nm) treatment, or 1.5 and 12 h washout periods after CGP 12177 (4 nm) treatment. Such a ‘decoupling’ effect was not observed during recovery from chronic exposure to the antagonists, timolol and propranolol. 6 We conclude that some antagonists cause a novel form of desensitization that is not linked to their partial agonistic potency. Moreover, Carazolol-type drugs seem to induce an additional isomeric form of the β-receptor that is not recognized by other antagonists. These observations could explain the well known discrepancy between long duration of action and rapid removal from the circulation of several antagonists in current therapeutic use." @default.
• W2040935821 created "2016-06-24" @default.
• W2040935821 creator A5011419040 @default.
• W2040935821 creator A5073708805 @default.
• W2040935821 date "1984-07-01" @default.
• W2040935821 modified "2023-09-25" @default.
• W2040935821 title "Recovery of β-adrenoceptors and cyclic AMP response after long term treatment of intact heart cells with β-blockers" @default.
• W2040935821 cites W110449010 @default.
• W2040935821 cites W147403299 @default.
• W2040935821 cites W1484657457 @default.
• W2040935821 cites W1506640557 @default.
• W2040935821 cites W1515847027 @default.
• W2040935821 cites W1528802303 @default.
• W2040935821 cites W1531281247 @default.
• W2040935821 cites W1775749144 @default.
• W2040935821 cites W182982796 @default.
• W2040935821 cites W1973230789 @default.
• W2040935821 cites W1997555787 @default.
• W2040935821 cites W2027047679 @default.
• W2040935821 cites W2027106088 @default.
• W2040935821 cites W2034677770 @default.
• W2040935821 cites W2069252373 @default.
• W2040935821 cites W2140684878 @default.
• W2040935821 cites W2163344393 @default.
• W2040935821 cites W2336106635 @default.
• W2040935821 cites W2409200912 @default.
• W2040935821 cites W2409972110 @default.
• W2040935821 cites W2410323139 @default.
• W2040935821 cites W2411353335 @default.
• W2040935821 cites W2461714286 @default.
• W2040935821 cites W3220325 @default.
• W2040935821 cites W4290011701 @default.
• W2040935821 doi "https://doi.org/10.1111/j.1476-5381.1984.tb10814.x" @default.
• W2040935821 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/1987018" @default.
• W2040935821 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/6146370" @default.
• W2040935821 hasPublicationYear "1984" @default.
• W2040935821 type Work @default.
• W2040935821 sameAs 2040935821 @default.
• W2040935821 citedByCount "8" @default.
• W2040935821 crossrefType "journal-article" @default.
• W2040935821 hasAuthorship W2040935821A5011419040 @default.
• W2040935821 hasAuthorship W2040935821A5073708805 @default.
• W2040935821 hasBestOaLocation W20409358211 @default.
• W2040935821 hasConcept C118487528 @default.
• W2040935821 hasConcept C126322002 @default.
• W2040935821 hasConcept C134018914 @default.
• W2040935821 hasConcept C170493617 @default.
• W2040935821 hasConcept C185592680 @default.
• W2040935821 hasConcept C24998067 @default.
• W2040935821 hasConcept C2776090920 @default.
• W2040935821 hasConcept C2776885963 @default.
• W2040935821 hasConcept C2778073030 @default.
• W2040935821 hasConcept C2778151854 @default.
• W2040935821 hasConcept C2781092963 @default.
• W2040935821 hasConcept C55493867 @default.
• W2040935821 hasConcept C71240020 @default.
• W2040935821 hasConcept C71924100 @default.
• W2040935821 hasConcept C74998103 @default.
• W2040935821 hasConcept C98274493 @default.
• W2040935821 hasConceptScore W2040935821C118487528 @default.
• W2040935821 hasConceptScore W2040935821C126322002 @default.
• W2040935821 hasConceptScore W2040935821C134018914 @default.
• W2040935821 hasConceptScore W2040935821C170493617 @default.
• W2040935821 hasConceptScore W2040935821C185592680 @default.
• W2040935821 hasConceptScore W2040935821C24998067 @default.
• W2040935821 hasConceptScore W2040935821C2776090920 @default.
• W2040935821 hasConceptScore W2040935821C2776885963 @default.
• W2040935821 hasConceptScore W2040935821C2778073030 @default.
• W2040935821 hasConceptScore W2040935821C2778151854 @default.
• W2040935821 hasConceptScore W2040935821C2781092963 @default.
• W2040935821 hasConceptScore W2040935821C55493867 @default.
• W2040935821 hasConceptScore W2040935821C71240020 @default.
• W2040935821 hasConceptScore W2040935821C71924100 @default.
• W2040935821 hasConceptScore W2040935821C74998103 @default.
• W2040935821 hasConceptScore W2040935821C98274493 @default.
• W2040935821 hasIssue "3" @default.
• W2040935821 hasLocation W20409358211 @default.
• W2040935821 hasLocation W20409358212 @default.
• W2040935821 hasLocation W20409358213 @default.
• W2040935821 hasLocation W20409358214 @default.
• W2040935821 hasOpenAccess W2040935821 @default.
• W2040935821 hasPrimaryLocation W20409358211 @default.
• W2040935821 hasRelatedWork W1543796853 @default.
• W2040935821 hasRelatedWork W1546720678 @default.
• W2040935821 hasRelatedWork W1971613811 @default.
• W2040935821 hasRelatedWork W1989113118 @default.
• W2040935821 hasRelatedWork W2011693868 @default.
• W2040935821 hasRelatedWork W2045570703 @default.
• W2040935821 hasRelatedWork W2055520311 @default.
• W2040935821 hasRelatedWork W2157556149 @default.
• W2040935821 hasRelatedWork W2162471541 @default.
• W2040935821 hasRelatedWork W2416080723 @default.
• W2040935821 hasVolume "82" @default.
• W2040935821 isParatext "false" @default.
• W2040935821 isRetracted "false" @default.
• W2040935821 magId "2040935821" @default.
• W2040935821 workType "article" @default.