Matches in SemOpenAlex for { <https://semopenalex.org/work/W1743554895> ?p ?o ?g. }
Showing items 1 to 66 of
66
with 100 items per page.
- W1743554895 endingPage "9" @default.
- W1743554895 startingPage "604" @default.
- W1743554895 abstract "The binding properties of the 5-hydroxytryptamine2 (5-HT2) receptor have been the subject of much interest and debate in recent years. The hallucinogenic amphetamine derivative 4-bromo-2,5-dimethoxyphenylisopropylamine (DOB) has been shown to bind to a small number of binding sites with properties very similar to [3H]ketanserin-labeled 5-HT2 receptors, but with much higher agonist affinities. Some researchers have interpreted this as evidence for the existence of a new subtype of 5-HT2 receptor (termed 5-HT2A), whereas others have interpreted these data as indicative of agonist high affinity and agonist low affinity states for the 5-HT2 receptor. In this investigation, a cDNA clone encoding the serotonin 5-HT2 receptor was transiently transfected into monkey kidney Cos-7 cells and stably transfected into mouse fibroblast L-M(TK-) cells. In both systems, expression of this single serotonin receptor cDNA led to the appearance of both [3H]DOB and [3H]ketanserin binding sites with properties that matched their binding characteristics in mammalian brain homogenates. Addition of guanosine 5'-(beta, gamma-imido) triphosphate [Gpp(NH)p] to this system caused a rightward shift and steepening of agonist competition curves for [3H] ketanserin binding, converting a two-site binding curve to a single low affinity binding state. Gpp(NH)p addition also caused a 50% decrease in the number of high affinity [3H]DOB binding sites, with no change in the dissociation constant of the remaining high affinity states. These data on a single human 5-HT2 receptor cDNA expressed in two different transfection host cells indicate that [3H]DOB and [3H]ketanserin binding reside on the same gene product, apparently interacting with agonist and antagonist conformations of a single human 5-HT2 receptor protein. These observations are consistent with the classical view of interconvertible agonist affinity states of GTP-binding protein-coupled receptors and strongly support the two state over the two receptor model for DOB binding to the 5-HT2 receptor." @default.
- W1743554895 created "2016-06-24" @default.
- W1743554895 creator A5010208798 @default.
- W1743554895 creator A5022257880 @default.
- W1743554895 creator A5077351723 @default.
- W1743554895 creator A5079860234 @default.
- W1743554895 creator A5081076088 @default.
- W1743554895 date "1990-11-01" @default.
- W1743554895 modified "2023-09-23" @default.
- W1743554895 title "[3H]-DOB(4-bromo-2,5-dimethoxyphenylisopropylamine) and [3H] ketanserin label two affinity states of the cloned human 5-hydroxytryptamine2 receptor." @default.
- W1743554895 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2233697" @default.
- W1743554895 hasPublicationYear "1990" @default.
- W1743554895 type Work @default.
- W1743554895 sameAs 1743554895 @default.
- W1743554895 citedByCount "14" @default.
- W1743554895 countsByYear W17435548952016 @default.
- W1743554895 countsByYear W17435548952022 @default.
- W1743554895 crossrefType "journal-article" @default.
- W1743554895 hasAuthorship W1743554895A5010208798 @default.
- W1743554895 hasAuthorship W1743554895A5022257880 @default.
- W1743554895 hasAuthorship W1743554895A5077351723 @default.
- W1743554895 hasAuthorship W1743554895A5079860234 @default.
- W1743554895 hasAuthorship W1743554895A5081076088 @default.
- W1743554895 hasConcept C107824862 @default.
- W1743554895 hasConcept C153911025 @default.
- W1743554895 hasConcept C170493617 @default.
- W1743554895 hasConcept C185592680 @default.
- W1743554895 hasConcept C200220013 @default.
- W1743554895 hasConcept C2775864247 @default.
- W1743554895 hasConcept C2777785214 @default.
- W1743554895 hasConcept C2778938600 @default.
- W1743554895 hasConcept C53910766 @default.
- W1743554895 hasConcept C55493867 @default.
- W1743554895 hasConcept C86803240 @default.
- W1743554895 hasConceptScore W1743554895C107824862 @default.
- W1743554895 hasConceptScore W1743554895C153911025 @default.
- W1743554895 hasConceptScore W1743554895C170493617 @default.
- W1743554895 hasConceptScore W1743554895C185592680 @default.
- W1743554895 hasConceptScore W1743554895C200220013 @default.
- W1743554895 hasConceptScore W1743554895C2775864247 @default.
- W1743554895 hasConceptScore W1743554895C2777785214 @default.
- W1743554895 hasConceptScore W1743554895C2778938600 @default.
- W1743554895 hasConceptScore W1743554895C53910766 @default.
- W1743554895 hasConceptScore W1743554895C55493867 @default.
- W1743554895 hasConceptScore W1743554895C86803240 @default.
- W1743554895 hasIssue "5" @default.
- W1743554895 hasLocation W17435548951 @default.
- W1743554895 hasOpenAccess W1743554895 @default.
- W1743554895 hasPrimaryLocation W17435548951 @default.
- W1743554895 hasRelatedWork W1505522657 @default.
- W1743554895 hasRelatedWork W2003847756 @default.
- W1743554895 hasRelatedWork W2007471305 @default.
- W1743554895 hasRelatedWork W2049104108 @default.
- W1743554895 hasRelatedWork W2070551380 @default.
- W1743554895 hasRelatedWork W2075657964 @default.
- W1743554895 hasRelatedWork W2111826689 @default.
- W1743554895 hasRelatedWork W2395716976 @default.
- W1743554895 hasRelatedWork W2403634309 @default.
- W1743554895 hasRelatedWork W2494980698 @default.
- W1743554895 hasVolume "38" @default.
- W1743554895 isParatext "false" @default.
- W1743554895 isRetracted "false" @default.
- W1743554895 magId "1743554895" @default.
- W1743554895 workType "article" @default.