Matches in SemOpenAlex for { <https://semopenalex.org/work/W2284228974> ?p ?o ?g. }
Showing items 1 to 87 of
87
with 100 items per page.
- W2284228974 endingPage "9" @default.
- W2284228974 startingPage "1022" @default.
- W2284228974 abstract "A-77636 is a dopamine (DA) D1 receptor-selective agonist that was previously shown to elicit beneficial responses in animal models of Parkinson's disease (PD) (Kebabian et al.: Eur. J. Pharmacol. 229: 203, 1992). However, A-77636 is of limited potential for PD therapy because it induces rapid tolerance in vivo. To understand the basis of rapid onset of tolerance to the compound, we conducted studies to compare the in vitro properties of A-77636 and A-81686; the latter is a structurally related D1 agonist that did not induce significant tolerance in vivo under similar experimental conditions. With SK-N-MC, a neuroblastoma cell line, as an in vitro model for the D1 receptor, significant differences in D1 receptor function were noted after pretreatment with the two compounds. Specifically, 1-hr pretreatment with A-77636 resulted in significant residual cAMP production, even after the drug solution was removed and the cells were washed. The residual cAMP activity was selectively inhibited by SCH 23390, a selective D1 antagonist. The residual cAMP activity declined with pretreatment time, and after 4-hr pretreatment, little residual cAMP production was observed. Cotreatment of SK-N-MC cells with SCH 23390 and A-77636 did not prevent residual cAMP production by A-77636. In contrast, A-81686 did not elicit residual cAMP production is SK-N-MC cells. Although A-77636 treated cells were devoid of agonist response 4 hr after drug removal, A-81686-treated cells exhibited significant cAMP response after drug removal. Preincubation of rat striatal membranes with A-77636 resulted in a large decrease in D1 receptor binding, despite repeated washings, whereas A-81686 pretreatment caused only a small reduction in D1 receptor binding. On the basis of the present data, we conclude that A-77636 dissociates slowly from the D1 receptor. The continued activation of the D1 receptor by A-77636 leads to inability of the receptor to recover its responsivity, which may explain its long duration of action and its ability to induce rapid behavioral tolerance in vivo." @default.
- W2284228974 created "2016-06-24" @default.
- W2284228974 creator A5020642706 @default.
- W2284228974 creator A5021286943 @default.
- W2284228974 creator A5029035402 @default.
- W2284228974 creator A5030863061 @default.
- W2284228974 creator A5031362541 @default.
- W2284228974 creator A5052113856 @default.
- W2284228974 creator A5055776003 @default.
- W2284228974 creator A5085735820 @default.
- W2284228974 creator A5086075511 @default.
- W2284228974 date "1996-03-01" @default.
- W2284228974 modified "2023-09-26" @default.
- W2284228974 title "Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636." @default.
- W2284228974 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8786531" @default.
- W2284228974 hasPublicationYear "1996" @default.
- W2284228974 type Work @default.
- W2284228974 sameAs 2284228974 @default.
- W2284228974 citedByCount "17" @default.
- W2284228974 countsByYear W22842289742013 @default.
- W2284228974 countsByYear W22842289742017 @default.
- W2284228974 countsByYear W22842289742021 @default.
- W2284228974 countsByYear W22842289742022 @default.
- W2284228974 countsByYear W22842289742023 @default.
- W2284228974 crossrefType "journal-article" @default.
- W2284228974 hasAuthorship W2284228974A5020642706 @default.
- W2284228974 hasAuthorship W2284228974A5021286943 @default.
- W2284228974 hasAuthorship W2284228974A5029035402 @default.
- W2284228974 hasAuthorship W2284228974A5030863061 @default.
- W2284228974 hasAuthorship W2284228974A5031362541 @default.
- W2284228974 hasAuthorship W2284228974A5052113856 @default.
- W2284228974 hasAuthorship W2284228974A5055776003 @default.
- W2284228974 hasAuthorship W2284228974A5085735820 @default.
- W2284228974 hasAuthorship W2284228974A5086075511 @default.
- W2284228974 hasConcept C120069818 @default.
- W2284228974 hasConcept C120750228 @default.
- W2284228974 hasConcept C126322002 @default.
- W2284228974 hasConcept C134018914 @default.
- W2284228974 hasConcept C150903083 @default.
- W2284228974 hasConcept C170493617 @default.
- W2284228974 hasConcept C185592680 @default.
- W2284228974 hasConcept C207001950 @default.
- W2284228974 hasConcept C2778258207 @default.
- W2284228974 hasConcept C2778938600 @default.
- W2284228974 hasConcept C2779779143 @default.
- W2284228974 hasConcept C2779917531 @default.
- W2284228974 hasConcept C513476851 @default.
- W2284228974 hasConcept C71924100 @default.
- W2284228974 hasConcept C86803240 @default.
- W2284228974 hasConcept C98274493 @default.
- W2284228974 hasConceptScore W2284228974C120069818 @default.
- W2284228974 hasConceptScore W2284228974C120750228 @default.
- W2284228974 hasConceptScore W2284228974C126322002 @default.
- W2284228974 hasConceptScore W2284228974C134018914 @default.
- W2284228974 hasConceptScore W2284228974C150903083 @default.
- W2284228974 hasConceptScore W2284228974C170493617 @default.
- W2284228974 hasConceptScore W2284228974C185592680 @default.
- W2284228974 hasConceptScore W2284228974C207001950 @default.
- W2284228974 hasConceptScore W2284228974C2778258207 @default.
- W2284228974 hasConceptScore W2284228974C2778938600 @default.
- W2284228974 hasConceptScore W2284228974C2779779143 @default.
- W2284228974 hasConceptScore W2284228974C2779917531 @default.
- W2284228974 hasConceptScore W2284228974C513476851 @default.
- W2284228974 hasConceptScore W2284228974C71924100 @default.
- W2284228974 hasConceptScore W2284228974C86803240 @default.
- W2284228974 hasConceptScore W2284228974C98274493 @default.
- W2284228974 hasIssue "3" @default.
- W2284228974 hasLocation W22842289741 @default.
- W2284228974 hasOpenAccess W2284228974 @default.
- W2284228974 hasPrimaryLocation W22842289741 @default.
- W2284228974 hasRelatedWork W1965592767 @default.
- W2284228974 hasRelatedWork W1976621129 @default.
- W2284228974 hasRelatedWork W1977323374 @default.
- W2284228974 hasRelatedWork W1999003861 @default.
- W2284228974 hasRelatedWork W2000408031 @default.
- W2284228974 hasRelatedWork W2019937176 @default.
- W2284228974 hasRelatedWork W2020816237 @default.
- W2284228974 hasRelatedWork W2027408532 @default.
- W2284228974 hasRelatedWork W2056639291 @default.
- W2284228974 hasRelatedWork W2093189958 @default.
- W2284228974 hasVolume "276" @default.
- W2284228974 isParatext "false" @default.
- W2284228974 isRetracted "false" @default.
- W2284228974 magId "2284228974" @default.
- W2284228974 workType "article" @default.