Matches in SemOpenAlex for { <https://semopenalex.org/work/W2092200401> ?p ?o ?g. }
- W2092200401 endingPage "297" @default.
- W2092200401 startingPage "291" @default.
- W2092200401 abstract "Antagonists, but not agonists, of the 5-HT3 receptor are useful therapeutic agents, and it is possible that partial agonists may also be potentially useful in the clinic. Here we show that 5-fluorotryptamine (5-FT) is a partial agonist at both 5-HT3A and 5-HT3AB receptors with an Rmax (Imax/Imax 5-HT) of 0.64 and 0.45 respectively. It is about 10 fold less potent than 5-HT: EC50=16 and 27 microM, and Ki for displacement of [3H]granisetron binding=0.8 and 1.8 microM for 5-HT3A and 5-HT3AB receptors respectively. We have also explored the potencies and efficacies of tryptamine and a range of 5-substituted tryptamine derivatives. At 5-HT3A receptors tryptamine is a weak (Rmax=0.15), low affinity (EC50=113 microM; Ki=4.8 microM) partial agonist, while 5-chlorotryptamine has a similar affinity to 5-FT (EC50=8.1 microM; Ki=2.7 microM) but is a very weak partial agonist (Rmax=0. 0037). These, and data from 5-methyltryptamine and 5-methoxytryptamine, reveal the importance of size and electronegativity at this location for efficient channel opening." @default.
- W2092200401 created "2016-06-24" @default.
- W2092200401 creator A5002660163 @default.
- W2092200401 creator A5035505196 @default.
- W2092200401 creator A5047202581 @default.
- W2092200401 creator A5048302486 @default.
- W2092200401 creator A5062317368 @default.
- W2092200401 creator A5084645832 @default.
- W2092200401 date "2008-02-01" @default.
- W2092200401 modified "2023-10-18" @default.
- W2092200401 title "5-Fluorotryptamine is a partial agonist at 5-HT3 receptors, and reveals that size and electronegativity at the 5 position of tryptamine are critical for efficient receptor function" @default.
- W2092200401 cites W1923513268 @default.
- W2092200401 cites W1980408303 @default.
- W2092200401 cites W1984302804 @default.
- W2092200401 cites W2001479739 @default.
- W2092200401 cites W2002923181 @default.
- W2092200401 cites W2005487766 @default.
- W2092200401 cites W2007667271 @default.
- W2092200401 cites W2010163969 @default.
- W2092200401 cites W2027758764 @default.
- W2092200401 cites W2043703377 @default.
- W2092200401 cites W2047321326 @default.
- W2092200401 cites W2053557358 @default.
- W2092200401 cites W2062909773 @default.
- W2092200401 cites W2075276440 @default.
- W2092200401 cites W2076860019 @default.
- W2092200401 cites W2096091943 @default.
- W2092200401 cites W2101625991 @default.
- W2092200401 cites W2122587704 @default.
- W2092200401 cites W2127837438 @default.
- W2092200401 cites W2138722801 @default.
- W2092200401 cites W2158824176 @default.
- W2092200401 doi "https://doi.org/10.1016/j.ejphar.2007.11.014" @default.
- W2092200401 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2649378" @default.
- W2092200401 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18082160" @default.
- W2092200401 hasPublicationYear "2008" @default.
- W2092200401 type Work @default.
- W2092200401 sameAs 2092200401 @default.
- W2092200401 citedByCount "19" @default.
- W2092200401 countsByYear W20922004012012 @default.
- W2092200401 countsByYear W20922004012013 @default.
- W2092200401 countsByYear W20922004012014 @default.
- W2092200401 countsByYear W20922004012016 @default.
- W2092200401 countsByYear W20922004012017 @default.
- W2092200401 countsByYear W20922004012018 @default.
- W2092200401 countsByYear W20922004012019 @default.
- W2092200401 countsByYear W20922004012021 @default.
- W2092200401 crossrefType "journal-article" @default.
- W2092200401 hasAuthorship W2092200401A5002660163 @default.
- W2092200401 hasAuthorship W2092200401A5035505196 @default.
- W2092200401 hasAuthorship W2092200401A5047202581 @default.
- W2092200401 hasAuthorship W2092200401A5048302486 @default.
- W2092200401 hasAuthorship W2092200401A5062317368 @default.
- W2092200401 hasAuthorship W2092200401A5084645832 @default.
- W2092200401 hasBestOaLocation W20922004011 @default.
- W2092200401 hasConcept C170493617 @default.
- W2092200401 hasConcept C185592680 @default.
- W2092200401 hasConcept C2775864247 @default.
- W2092200401 hasConcept C2777135210 @default.
- W2092200401 hasConcept C2778938600 @default.
- W2092200401 hasConcept C38533456 @default.
- W2092200401 hasConcept C53910766 @default.
- W2092200401 hasConcept C55493867 @default.
- W2092200401 hasConcept C58732023 @default.
- W2092200401 hasConcept C71240020 @default.
- W2092200401 hasConcept C86803240 @default.
- W2092200401 hasConcept C98274493 @default.
- W2092200401 hasConceptScore W2092200401C170493617 @default.
- W2092200401 hasConceptScore W2092200401C185592680 @default.
- W2092200401 hasConceptScore W2092200401C2775864247 @default.
- W2092200401 hasConceptScore W2092200401C2777135210 @default.
- W2092200401 hasConceptScore W2092200401C2778938600 @default.
- W2092200401 hasConceptScore W2092200401C38533456 @default.
- W2092200401 hasConceptScore W2092200401C53910766 @default.
- W2092200401 hasConceptScore W2092200401C55493867 @default.
- W2092200401 hasConceptScore W2092200401C58732023 @default.
- W2092200401 hasConceptScore W2092200401C71240020 @default.
- W2092200401 hasConceptScore W2092200401C86803240 @default.
- W2092200401 hasConceptScore W2092200401C98274493 @default.
- W2092200401 hasIssue "3" @default.
- W2092200401 hasLocation W20922004011 @default.
- W2092200401 hasLocation W20922004012 @default.
- W2092200401 hasLocation W20922004013 @default.
- W2092200401 hasLocation W20922004014 @default.
- W2092200401 hasLocation W20922004015 @default.
- W2092200401 hasOpenAccess W2092200401 @default.
- W2092200401 hasPrimaryLocation W20922004011 @default.
- W2092200401 hasRelatedWork W1986216739 @default.
- W2092200401 hasRelatedWork W2012837477 @default.
- W2092200401 hasRelatedWork W2019365375 @default.
- W2092200401 hasRelatedWork W2041032137 @default.
- W2092200401 hasRelatedWork W2092200401 @default.
- W2092200401 hasRelatedWork W2263018755 @default.
- W2092200401 hasRelatedWork W2891037884 @default.
- W2092200401 hasRelatedWork W2950486117 @default.
- W2092200401 hasRelatedWork W2991822442 @default.
- W2092200401 hasRelatedWork W3146158776 @default.
- W2092200401 hasVolume "580" @default.