Matches in SemOpenAlex for { <https://semopenalex.org/work/W4246295056> ?p ?o ?g. }
Showing items 1 to 90 of
90
with 100 items per page.
- W4246295056 endingPage "441" @default.
- W4246295056 startingPage "431" @default.
- W4246295056 abstract "1Rizatriptan (MK-462, (N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine)) and its structurally related analogue L-741,519 (N-methyl-4-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]piperidine) are novel 5-HT1D-receptor agonists. Rizatriptan has shown efficacy as an anti-migraine agent in clinical trials. Since angiographic studies in patients have shown that sumatriptan (an established 5-HT1D-receptor agonist) can cause coronary artery vasoconstriction, we compared the effects of rizatriptan and L-741,519 with those of 5-HT and sumatriptan on endothelium-denuded segments of human coronary artery in vitro. 2Coronary arteries were obtained from explanted hearts from patients undergoing cardiac transplantation (n=16 viable arteries from 13 males, 3 females, aged 38–68 years) and arterial segments (5–6 mm in length) were mounted in organ baths for isometric tension recording. Each segment was first exposed to 45mm KCl and then to 5-HT (1 nm–100 μm). Concentration–effect curves to rizatriptan and sumatriptan (Study 1, n=6 or 7 arteries) or sumatriptan and L-741,519 (Study 2, n=8 arteries) were then performed in a consecutive and random manner. The response to repeated application of 5-HT was obtained in separate segments. 3One artery showed severe atheroma and was not included in the analysis. ANOVA showed that 5-HT responsiveness varied significantly between arteries from different patients, but not between arterial segments from the same patient. Desensitization was seen consistently across all agonists but did not significantly affect inter-agonist comparisons. 4There was graded effectiveness in the ability of the agonists to cause contraction with the rank order of Emax values being 5-HTsumatriptan>L-741,519>rizatriptan. In terms of EC50 values, L-741,519 was significantly more potent than sumatriptan. 5The present study (using a ‘cross-over’ experimental protocol) confirms our previous observation that rizatriptan is less effective than sumatriptan in causing contraction of human isolated coronary artery. Furthermore, it shows that the lower maximum contractile response to rizatriptan, compared with that of sumatriptan, is not merely the consequence of variability in response to 5-HT1D- receptor agonists between patients or between segments from the same artery." @default.
- W4246295056 created "2022-05-12" @default.
- W4246295056 creator A5003820499 @default.
- W4246295056 creator A5016061416 @default.
- W4246295056 creator A5044002950 @default.
- W4246295056 creator A5047282711 @default.
- W4246295056 creator A5058336621 @default.
- W4246295056 creator A5062560561 @default.
- W4246295056 date "1996-10-01" @default.
- W4246295056 modified "2023-10-03" @default.
- W4246295056 title "5-HT<sub>1D</sub> receptor agonists and human coronary artery reactivity <i>in vitro</i> : crossover comparisons of 5-HT and sumatriptan with rizatriptan and L-741,519" @default.
- W4246295056 cites W1967018240 @default.
- W4246295056 cites W1982559853 @default.
- W4246295056 cites W1985538065 @default.
- W4246295056 cites W1996049651 @default.
- W4246295056 cites W2008546096 @default.
- W4246295056 cites W2008915415 @default.
- W4246295056 cites W2009150874 @default.
- W4246295056 cites W2021812411 @default.
- W4246295056 cites W2031764142 @default.
- W4246295056 cites W2034188749 @default.
- W4246295056 cites W2042173017 @default.
- W4246295056 cites W2054563478 @default.
- W4246295056 cites W2075487573 @default.
- W4246295056 cites W2104496018 @default.
- W4246295056 cites W2341579207 @default.
- W4246295056 doi "https://doi.org/10.1111/j.1365-2125.1996.tb00005.x" @default.
- W4246295056 hasPublicationYear "1996" @default.
- W4246295056 type Work @default.
- W4246295056 citedByCount "32" @default.
- W4246295056 countsByYear W42462950562012 @default.
- W4246295056 countsByYear W42462950562013 @default.
- W4246295056 countsByYear W42462950562017 @default.
- W4246295056 countsByYear W42462950562020 @default.
- W4246295056 countsByYear W42462950562021 @default.
- W4246295056 crossrefType "journal-article" @default.
- W4246295056 hasAuthorship W4246295056A5003820499 @default.
- W4246295056 hasAuthorship W4246295056A5016061416 @default.
- W4246295056 hasAuthorship W4246295056A5044002950 @default.
- W4246295056 hasAuthorship W4246295056A5047282711 @default.
- W4246295056 hasAuthorship W4246295056A5058336621 @default.
- W4246295056 hasAuthorship W4246295056A5062560561 @default.
- W4246295056 hasBestOaLocation W42462950562 @default.
- W4246295056 hasConcept C126322002 @default.
- W4246295056 hasConcept C170493617 @default.
- W4246295056 hasConcept C2775864247 @default.
- W4246295056 hasConcept C2776820930 @default.
- W4246295056 hasConcept C2777030092 @default.
- W4246295056 hasConcept C2778742706 @default.
- W4246295056 hasConcept C2778871607 @default.
- W4246295056 hasConcept C2778938600 @default.
- W4246295056 hasConcept C2779961880 @default.
- W4246295056 hasConcept C42219234 @default.
- W4246295056 hasConcept C53910766 @default.
- W4246295056 hasConcept C71924100 @default.
- W4246295056 hasConcept C98274493 @default.
- W4246295056 hasConceptScore W4246295056C126322002 @default.
- W4246295056 hasConceptScore W4246295056C170493617 @default.
- W4246295056 hasConceptScore W4246295056C2775864247 @default.
- W4246295056 hasConceptScore W4246295056C2776820930 @default.
- W4246295056 hasConceptScore W4246295056C2777030092 @default.
- W4246295056 hasConceptScore W4246295056C2778742706 @default.
- W4246295056 hasConceptScore W4246295056C2778871607 @default.
- W4246295056 hasConceptScore W4246295056C2778938600 @default.
- W4246295056 hasConceptScore W4246295056C2779961880 @default.
- W4246295056 hasConceptScore W4246295056C42219234 @default.
- W4246295056 hasConceptScore W4246295056C53910766 @default.
- W4246295056 hasConceptScore W4246295056C71924100 @default.
- W4246295056 hasConceptScore W4246295056C98274493 @default.
- W4246295056 hasIssue "4" @default.
- W4246295056 hasLocation W42462950561 @default.
- W4246295056 hasLocation W42462950562 @default.
- W4246295056 hasOpenAccess W4246295056 @default.
- W4246295056 hasPrimaryLocation W42462950561 @default.
- W4246295056 hasRelatedWork W1537143364 @default.
- W4246295056 hasRelatedWork W1985065034 @default.
- W4246295056 hasRelatedWork W2051549061 @default.
- W4246295056 hasRelatedWork W2102231552 @default.
- W4246295056 hasRelatedWork W2123730244 @default.
- W4246295056 hasRelatedWork W2277781552 @default.
- W4246295056 hasRelatedWork W2414935001 @default.
- W4246295056 hasRelatedWork W2417308169 @default.
- W4246295056 hasRelatedWork W4245764066 @default.
- W4246295056 hasRelatedWork W2950091852 @default.
- W4246295056 hasVolume "42" @default.
- W4246295056 isParatext "false" @default.
- W4246295056 isRetracted "false" @default.
- W4246295056 workType "article" @default.