FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2034897299> ?p ?o ?g. }

• W2034897299 endingPage "15" @default.
• W2034897299 startingPage "9" @default.
• W2034897299 abstract "Agonist binding to G protein-coupled receptors induces the formation of a receptor-G protein complex and subsequent guanosine 5'-diphosphate/guanosine 5'-triphosphate (GDP/GTP) exchange. Some receptors, however, form receptor-G protein complexes and promote GDP/GTP exchange even when not occupied by agonists. Such receptors preferentially activate pertussis toxin-sensitive G proteins (i.e., G(i)/G(o)), and the interactions of receptors and G proteins are affected by monovalent cations (most notably Na(+)), both in the occupied and unoccupied state. We investigated the effects of Na(+) on the intrinsic activity of 5-hydroxytryptamine(1A) (5-HT(1A)) receptor ligands, measured as maximal effect (E(MAX)), using guanosine 5'-0-(3-[35S]thio)-triphosphate ([35S]GTPgammaS) binding to membranes prepared from human epithelioid carcinoma (HeLa) cells, expressing 500 fmol/mg protein of cloned human 5-HT(1A) receptor (HA7 cells). A decrease of the NaCl concentration decreased the maximal effect of serotonin, increased basal [35S]GTPgammaS binding, and increased the negative intrinsic activity of spiperone and N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]-N-(2-pyridinyl)cyclohexaneca rboxamide (WAY 100635). This ability of WAY 100635 to decrease basal [35S]GTPgammaS binding was antagonized by (s)-N-tert-butyl-3-(4-(2-methoxyphenyl)piperazine-1-yl)-2-phenylpropa namide ((s)-WAY 100135) (pA(2)=7.77). Further, WAY 100635 was able to antagonize carboxamidotryptamine (5-CT)-stimulated [35S]GTPgammaS binding with a pA(2) of 9.9, in standard NaCl conditions, and of 9.7, in the absence of NaCl. Changes in membrane concentration did not affect the ability of WAY 100635 to decrease [35S]GTPgammaS binding. WAY 100635 did not affect basal [35S]GTPgammaS binding to membranes from untransfected HeLa cells. Pertussis toxin (200 ng/ml) prevented WAY 100635 and spiperone to decrease [35S]GTPgammaS binding, showing that their effects were mediated by G proteins of the G(i)/G(o) family. In conclusion, the constitutive and stimulated activity of human 5-HT(1A) receptors expressed in HA7 cells is sodium-dependent, which allowed to confirm the 5-HT(1A) inverse agonist properties of spiperone, and to show that WAY 100635 is an inverse agonist at 5-HT(1A) receptors that inhibits basal [35S]GTPgammaS binding to a lesser extent than spiperone. [35S]GTPgammaS binding to membranes from HA7 cells under low NaCl conditions appears to be especially suitable to evidence and pharmacologically analyze the inverse agonist properties of 5-HT(1A) receptor ligands." @default.
• W2034897299 created "2016-06-24" @default.
• W2034897299 creator A5080164174 @default.
• W2034897299 creator A5091250799 @default.
• W2034897299 date "2000-07-01" @default.
• W2034897299 modified "2023-10-11" @default.
• W2034897299 title "The putative «silent» 5-HT1A receptor antagonist, WAY 100635, has inverse agonist properties at cloned human 5-HT1A receptors" @default.
• W2034897299 cites W1521629728 @default.
• W2034897299 cites W1963690073 @default.
• W2034897299 cites W1986980508 @default.
• W2034897299 cites W1992281684 @default.
• W2034897299 cites W2008180356 @default.
• W2034897299 cites W2013968961 @default.
• W2034897299 cites W2018755088 @default.
• W2034897299 cites W2025888192 @default.
• W2034897299 cites W2044190119 @default.
• W2034897299 cites W2052861175 @default.
• W2034897299 cites W2076460438 @default.
• W2034897299 cites W2094569992 @default.
• W2034897299 cites W2119335473 @default.
• W2034897299 doi "https://doi.org/10.1016/s0014-2999(00)00410-6" @default.
• W2034897299 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10915831" @default.
• W2034897299 hasPublicationYear "2000" @default.
• W2034897299 type Work @default.
• W2034897299 sameAs 2034897299 @default.
• W2034897299 citedByCount "38" @default.
• W2034897299 countsByYear W20348972992012 @default.
• W2034897299 countsByYear W20348972992013 @default.
• W2034897299 countsByYear W20348972992014 @default.
• W2034897299 countsByYear W20348972992017 @default.
• W2034897299 countsByYear W20348972992019 @default.
• W2034897299 countsByYear W20348972992020 @default.
• W2034897299 crossrefType "journal-article" @default.
• W2034897299 hasAuthorship W2034897299A5080164174 @default.
• W2034897299 hasAuthorship W2034897299A5091250799 @default.
• W2034897299 hasConcept C118716 @default.
• W2034897299 hasConcept C126322002 @default.
• W2034897299 hasConcept C134018914 @default.
• W2034897299 hasConcept C170493617 @default.
• W2034897299 hasConcept C181199279 @default.
• W2034897299 hasConcept C185592680 @default.
• W2034897299 hasConcept C2775864247 @default.
• W2034897299 hasConcept C2776638253 @default.
• W2034897299 hasConcept C2777995097 @default.
• W2034897299 hasConcept C2778684643 @default.
• W2034897299 hasConcept C2778938600 @default.
• W2034897299 hasConcept C2779817904 @default.
• W2034897299 hasConcept C2781073084 @default.
• W2034897299 hasConcept C2781093953 @default.
• W2034897299 hasConcept C38533456 @default.
• W2034897299 hasConcept C49773422 @default.
• W2034897299 hasConcept C53910766 @default.
• W2034897299 hasConcept C55493867 @default.
• W2034897299 hasConcept C71924100 @default.
• W2034897299 hasConcept C80631254 @default.
• W2034897299 hasConcept C86803240 @default.
• W2034897299 hasConcept C89951826 @default.
• W2034897299 hasConceptScore W2034897299C118716 @default.
• W2034897299 hasConceptScore W2034897299C126322002 @default.
• W2034897299 hasConceptScore W2034897299C134018914 @default.
• W2034897299 hasConceptScore W2034897299C170493617 @default.
• W2034897299 hasConceptScore W2034897299C181199279 @default.
• W2034897299 hasConceptScore W2034897299C185592680 @default.
• W2034897299 hasConceptScore W2034897299C2775864247 @default.
• W2034897299 hasConceptScore W2034897299C2776638253 @default.
• W2034897299 hasConceptScore W2034897299C2777995097 @default.
• W2034897299 hasConceptScore W2034897299C2778684643 @default.
• W2034897299 hasConceptScore W2034897299C2778938600 @default.
• W2034897299 hasConceptScore W2034897299C2779817904 @default.
• W2034897299 hasConceptScore W2034897299C2781073084 @default.
• W2034897299 hasConceptScore W2034897299C2781093953 @default.
• W2034897299 hasConceptScore W2034897299C38533456 @default.
• W2034897299 hasConceptScore W2034897299C49773422 @default.
• W2034897299 hasConceptScore W2034897299C53910766 @default.
• W2034897299 hasConceptScore W2034897299C55493867 @default.
• W2034897299 hasConceptScore W2034897299C71924100 @default.
• W2034897299 hasConceptScore W2034897299C80631254 @default.
• W2034897299 hasConceptScore W2034897299C86803240 @default.
• W2034897299 hasConceptScore W2034897299C89951826 @default.
• W2034897299 hasIssue "1" @default.
• W2034897299 hasLocation W20348972991 @default.
• W2034897299 hasLocation W20348972992 @default.
• W2034897299 hasOpenAccess W2034897299 @default.
• W2034897299 hasPrimaryLocation W20348972991 @default.
• W2034897299 hasRelatedWork W1522302812 @default.
• W2034897299 hasRelatedWork W1977705849 @default.
• W2034897299 hasRelatedWork W1994182693 @default.
• W2034897299 hasRelatedWork W2007883351 @default.
• W2034897299 hasRelatedWork W2019921154 @default.
• W2034897299 hasRelatedWork W2053188024 @default.
• W2034897299 hasRelatedWork W2086044924 @default.
• W2034897299 hasRelatedWork W2093548650 @default.
• W2034897299 hasRelatedWork W2170857974 @default.
• W2034897299 hasRelatedWork W2430699237 @default.
• W2034897299 hasVolume "401" @default.
• W2034897299 isParatext "false" @default.
• W2034897299 isRetracted "false" @default.
• W2034897299 magId "2034897299" @default.

• next