FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2024964650> ?p ?o ?g. }

• W2024964650 endingPage "174" @default.
• W2024964650 startingPage "165" @default.
• W2024964650 abstract "5-HT4 receptors positively coupled to adenylyl cyclase and possessing unique pharmacological properties were first described in mouse colliculi neurons using functional studies. The recent introduction of a radiolabeled 5-HT4 receptor antagonist, [3H]GR 113808 [1-[2-(methylsulphonylamino)ethyl]4-piperidinyl]methyl-1-methyl-in dole-3 carboxylate] having high specificity and affinity allowed the pharmacological comparison between the specific binding sites identified with this compound and the functional 5-HT4 receptors in the same preparation, the colliculi neurons. We show here that [3H]GR 113808 binding is saturable in this preparation and reveals a homogeneous population of sites with a pKd value of 9.5 +/- 0.2 and a Bmax of 75 +/- 23 fmol/mg protein. Seventeen agonists and six antagonists with molecules structurally related either to indoles, benzamides or benzimidazolones and previously known as 5-HT4 receptor ligands, were tested for their ability to compete with [3H]GR 113808 binding sites and to stimulate or inhibit 5-HT-stimulated adenylyl cyclase activity. Highly significant correlations were obtained between the affinities of either agonists or antagonists for [3H]GR 113808 binding sites and their potencies for functional 5-HT4 receptors (r = 0.87 and 0.99, respectively). In addition, we also found good correlations between the Kd of several 5-HT4 receptor ligands determined in cell membranes of mouse colliculi neurons and their Kd determined in previous studies in guinea-pig striatum (0.95) and in human caudate (0.97). [3H]GR 113808 binding studies demonstrated that the 50% decrease in 5-HT-stimulated cAMP accumulation which followed a 5 min exposure period with 5-HT (10 microM) was not accompanied by any significant decrease in the number of binding sites. Longer exposure periods with 5-HT resulted in a decrease in [3H]GR 113808 binding sites which started to be significant after 30 min." @default.
• W2024964650 created "2016-06-24" @default.
• W2024964650 creator A5008089947 @default.
• W2024964650 creator A5045863654 @default.
• W2024964650 creator A5071581900 @default.
• W2024964650 creator A5078340517 @default.
• W2024964650 date "1996-03-01" @default.
• W2024964650 modified "2023-10-08" @default.
• W2024964650 title "Pharmacological comparison between [3H]GR 113808 binding sites and functional 5-HT4 receptors in neurons" @default.
• W2024964650 cites W1963541966 @default.
• W2024964650 cites W1965635846 @default.
• W2024964650 cites W1965961744 @default.
• W2024964650 cites W1969274489 @default.
• W2024964650 cites W1969377544 @default.
• W2024964650 cites W1975661708 @default.
• W2024964650 cites W1980368200 @default.
• W2024964650 cites W1983649348 @default.
• W2024964650 cites W1984028006 @default.
• W2024964650 cites W1987500506 @default.
• W2024964650 cites W1989826835 @default.
• W2024964650 cites W2016161989 @default.
• W2024964650 cites W2017836262 @default.
• W2024964650 cites W2035977493 @default.
• W2024964650 cites W2037505307 @default.
• W2024964650 cites W2039634087 @default.
• W2024964650 cites W2043813981 @default.
• W2024964650 cites W2044861397 @default.
• W2024964650 cites W2047499026 @default.
• W2024964650 cites W2053074524 @default.
• W2024964650 cites W2057106837 @default.
• W2024964650 cites W2060207881 @default.
• W2024964650 cites W2063493172 @default.
• W2024964650 cites W2071112327 @default.
• W2024964650 cites W2072458796 @default.
• W2024964650 cites W2074631079 @default.
• W2024964650 cites W2078248414 @default.
• W2024964650 cites W2079854766 @default.
• W2024964650 cites W2081378538 @default.
• W2024964650 cites W2085547042 @default.
• W2024964650 cites W2091014133 @default.
• W2024964650 cites W2114164301 @default.
• W2024964650 cites W2116949924 @default.
• W2024964650 cites W2318453725 @default.
• W2024964650 cites W4293247451 @default.
• W2024964650 cites W67730575 @default.
• W2024964650 doi "https://doi.org/10.1016/0014-2999(95)00786-5" @default.
• W2024964650 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/8867105" @default.
• W2024964650 hasPublicationYear "1996" @default.
• W2024964650 type Work @default.
• W2024964650 sameAs 2024964650 @default.
• W2024964650 citedByCount "39" @default.
• W2024964650 countsByYear W20249646502013 @default.
• W2024964650 countsByYear W20249646502014 @default.
• W2024964650 countsByYear W20249646502015 @default.
• W2024964650 countsByYear W20249646502016 @default.
• W2024964650 countsByYear W20249646502017 @default.
• W2024964650 countsByYear W20249646502018 @default.
• W2024964650 crossrefType "journal-article" @default.
• W2024964650 hasAuthorship W2024964650A5008089947 @default.
• W2024964650 hasAuthorship W2024964650A5045863654 @default.
• W2024964650 hasAuthorship W2024964650A5071581900 @default.
• W2024964650 hasAuthorship W2024964650A5078340517 @default.
• W2024964650 hasConcept C107824862 @default.
• W2024964650 hasConcept C12554922 @default.
• W2024964650 hasConcept C126322002 @default.
• W2024964650 hasConcept C134018914 @default.
• W2024964650 hasConcept C144024400 @default.
• W2024964650 hasConcept C149923435 @default.
• W2024964650 hasConcept C170493617 @default.
• W2024964650 hasConcept C185592680 @default.
• W2024964650 hasConcept C192096249 @default.
• W2024964650 hasConcept C2778938600 @default.
• W2024964650 hasConcept C2779178603 @default.
• W2024964650 hasConcept C2908647359 @default.
• W2024964650 hasConcept C55493867 @default.
• W2024964650 hasConcept C67847695 @default.
• W2024964650 hasConcept C71924100 @default.
• W2024964650 hasConcept C86803240 @default.
• W2024964650 hasConceptScore W2024964650C107824862 @default.
• W2024964650 hasConceptScore W2024964650C12554922 @default.
• W2024964650 hasConceptScore W2024964650C126322002 @default.
• W2024964650 hasConceptScore W2024964650C134018914 @default.
• W2024964650 hasConceptScore W2024964650C144024400 @default.
• W2024964650 hasConceptScore W2024964650C149923435 @default.
• W2024964650 hasConceptScore W2024964650C170493617 @default.
• W2024964650 hasConceptScore W2024964650C185592680 @default.
• W2024964650 hasConceptScore W2024964650C192096249 @default.
• W2024964650 hasConceptScore W2024964650C2778938600 @default.
• W2024964650 hasConceptScore W2024964650C2779178603 @default.
• W2024964650 hasConceptScore W2024964650C2908647359 @default.
• W2024964650 hasConceptScore W2024964650C55493867 @default.
• W2024964650 hasConceptScore W2024964650C67847695 @default.
• W2024964650 hasConceptScore W2024964650C71924100 @default.
• W2024964650 hasConceptScore W2024964650C86803240 @default.
• W2024964650 hasIssue "2" @default.
• W2024964650 hasLocation W20249646501 @default.
• W2024964650 hasLocation W20249646502 @default.
• W2024964650 hasOpenAccess W2024964650 @default.

• next