Matches in SemOpenAlex for { <https://semopenalex.org/work/W2016102777> ?p ?o ?g. }
Showing items 1 to 95 of
95
with 100 items per page.
- W2016102777 endingPage "2733" @default.
- W2016102777 startingPage "2725" @default.
- W2016102777 abstract "The synthesis and vascular 5-HT1B-like receptor activity of a novel series of 2-oxadiazolyl-5-substituted tryptamine derivatives 2 is described. Modifications to the 2-oxadiazolyl group R1, the heterocycle R2 and the length of the linking chain (n) have been explored. Several compounds were identified which exhibited moderate 5-HT1B-like receptor affinity. In particular, 2-(3-ethyl-1,2,4-oxadiazol-5-yl)-3-[2-(dimethylamino)ethyl]-5-[(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)methyl]-1H-indole (20) in which n = 1 had a pKB = 7.23 at the 5-HT1B-like receptor and >60 fold selectivity over α1-adrenoceptor affinity. This contrasts with the higher homologue derivatives such as 10 and 11 where n = 2 which exhibited decreased potency and selectivity for the 5-HT1B-like receptor. The 2-oxadiazolyl-5-substituted-N,N-dimethyltryptamine derivatives were found to be silent (as judged by the inability of angiotensin II to unmask 5-HT1B-like receptor mediated agonist activity in the rabbit femoral artery) and competitive 5-HT1B-like receptor antagonists with half lives of up to 1.5 hours in dog plasma and with good oral bioavailability." @default.
- W2016102777 created "2016-06-24" @default.
- W2016102777 creator A5005424184 @default.
- W2016102777 creator A5007790629 @default.
- W2016102777 creator A5010610348 @default.
- W2016102777 creator A5014283781 @default.
- W2016102777 creator A5021451098 @default.
- W2016102777 creator A5030931270 @default.
- W2016102777 creator A5036402640 @default.
- W2016102777 creator A5047303896 @default.
- W2016102777 creator A5047386879 @default.
- W2016102777 date "1999-01-01" @default.
- W2016102777 modified "2023-09-26" @default.
- W2016102777 title "Synthesis and serotonergic activity of 2-oxadiazolyl-5-substituted-N,N-dimethyltryptamines: novel antagonists for the vascular 5-HT1B-like receptor" @default.
- W2016102777 cites W1126821415 @default.
- W2016102777 cites W1772950163 @default.
- W2016102777 cites W1944403496 @default.
- W2016102777 cites W1983664314 @default.
- W2016102777 cites W1987424526 @default.
- W2016102777 cites W1996049651 @default.
- W2016102777 cites W2002310148 @default.
- W2016102777 cites W2005395166 @default.
- W2016102777 cites W2009150874 @default.
- W2016102777 cites W2010425214 @default.
- W2016102777 cites W2013252397 @default.
- W2016102777 cites W2016513895 @default.
- W2016102777 cites W2023732689 @default.
- W2016102777 cites W2037344126 @default.
- W2016102777 cites W2056761692 @default.
- W2016102777 cites W2057605455 @default.
- W2016102777 cites W2064516222 @default.
- W2016102777 cites W2078778209 @default.
- W2016102777 cites W2090699172 @default.
- W2016102777 cites W2153853866 @default.
- W2016102777 cites W2319834083 @default.
- W2016102777 cites W2341579207 @default.
- W2016102777 cites W2951248524 @default.
- W2016102777 doi "https://doi.org/10.1039/a903325d" @default.
- W2016102777 hasPublicationYear "1999" @default.
- W2016102777 type Work @default.
- W2016102777 sameAs 2016102777 @default.
- W2016102777 citedByCount "16" @default.
- W2016102777 countsByYear W20161027772012 @default.
- W2016102777 countsByYear W20161027772013 @default.
- W2016102777 countsByYear W20161027772014 @default.
- W2016102777 countsByYear W20161027772015 @default.
- W2016102777 countsByYear W20161027772016 @default.
- W2016102777 countsByYear W20161027772017 @default.
- W2016102777 countsByYear W20161027772021 @default.
- W2016102777 crossrefType "journal-article" @default.
- W2016102777 hasAuthorship W2016102777A5005424184 @default.
- W2016102777 hasAuthorship W2016102777A5007790629 @default.
- W2016102777 hasAuthorship W2016102777A5010610348 @default.
- W2016102777 hasAuthorship W2016102777A5014283781 @default.
- W2016102777 hasAuthorship W2016102777A5021451098 @default.
- W2016102777 hasAuthorship W2016102777A5030931270 @default.
- W2016102777 hasAuthorship W2016102777A5036402640 @default.
- W2016102777 hasAuthorship W2016102777A5047303896 @default.
- W2016102777 hasAuthorship W2016102777A5047386879 @default.
- W2016102777 hasConcept C170493617 @default.
- W2016102777 hasConcept C185592680 @default.
- W2016102777 hasConcept C2775864247 @default.
- W2016102777 hasConcept C37000724 @default.
- W2016102777 hasConcept C53910766 @default.
- W2016102777 hasConcept C55493867 @default.
- W2016102777 hasConcept C86803240 @default.
- W2016102777 hasConcept C98274493 @default.
- W2016102777 hasConceptScore W2016102777C170493617 @default.
- W2016102777 hasConceptScore W2016102777C185592680 @default.
- W2016102777 hasConceptScore W2016102777C2775864247 @default.
- W2016102777 hasConceptScore W2016102777C37000724 @default.
- W2016102777 hasConceptScore W2016102777C53910766 @default.
- W2016102777 hasConceptScore W2016102777C55493867 @default.
- W2016102777 hasConceptScore W2016102777C86803240 @default.
- W2016102777 hasConceptScore W2016102777C98274493 @default.
- W2016102777 hasIssue "19" @default.
- W2016102777 hasLocation W20161027771 @default.
- W2016102777 hasOpenAccess W2016102777 @default.
- W2016102777 hasPrimaryLocation W20161027771 @default.
- W2016102777 hasRelatedWork W1983045415 @default.
- W2016102777 hasRelatedWork W2019365375 @default.
- W2016102777 hasRelatedWork W2043827012 @default.
- W2016102777 hasRelatedWork W2058657762 @default.
- W2016102777 hasRelatedWork W2075568459 @default.
- W2016102777 hasRelatedWork W2077760444 @default.
- W2016102777 hasRelatedWork W2161963368 @default.
- W2016102777 hasRelatedWork W2410935429 @default.
- W2016102777 hasRelatedWork W4206347286 @default.
- W2016102777 hasRelatedWork W4310572306 @default.
- W2016102777 isParatext "false" @default.
- W2016102777 isRetracted "false" @default.
- W2016102777 magId "2016102777" @default.
- W2016102777 workType "article" @default.