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Article: Effects of the combined 5-hydroxytryptamine2 receptor and Ca2+ channel antagonist LU49938 on the responsiveness of isolated porcine coronary arteries with and without endothelium

TitleEffects of the combined 5-hydroxytryptamine2 receptor and Ca2+ channel antagonist LU49938 on the responsiveness of isolated porcine coronary arteries with and without endothelium
Authors
Issue Date1994
PublisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/
Citation
Journal Of Cardiovascular Pharmacology, 1994, v. 24 n. 3, p. 517-522 How to Cite?
AbstractWe performed experiments to determine the effects of the combined 5- hydroxytryptamine2 (5-HT2) receptor and Ca2+ channel antagonist LU49938 ((2S)-5-[N-methyl-N-(n-hexyl)]amino-2-isopropyl-2(3.4.5-trimethoxy phenyl)- valeronitril-hydrochloride) on vascular smooth muscle (VSM) and endothelium in isolated porcine coronary arteries. Rings with and without endothelium were suspended in conventional organ chambers for measurement of isometric force. LU49938 inhibited contractions evoked by serotonin, norepinephrine (NE), and prostaglandin F(2α) (PGF(2α)) in a concentration-dependent and noncompetitive manner. The lower concentrations of LU49938 (10-7 and 10- 6 M) did not affect contractions to serotonin in the presence of ketanserin. However, a higher concentration of LU49938 (10-5 M) significantly decreased the concentration-response curve to the monoamine in the presence of ketanserin. These findings suggest that LU49938 has a dual inhibitory effect on contractions: selective inhibition of 5-HT2 receptor and nonselective inhibition of the contractile process in VSM. The mechanism of this nonselective inhibition of VSM is likely to be related to inhibition of Ca2+ entry because LU49938 inhibited responses to several agonists. The time course and degree of relaxation caused by LU49938 were comparable in rings with and without endothelium in control solution or after incubation with nitro-L-arginine and/or indomethacin. LU49938 did not affect endothelium-dependent relaxations induced by serotonin and bradykinin. These results suggest that LU49938 does not affect endothelium-dependent responses in porcine coronary artery.
Persistent Identifierhttp://hdl.handle.net/10722/171129
ISSN
2015 Impact Factor: 2.462
2015 SCImago Journal Rankings: 0.962
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorPark, SJen_US
dc.contributor.authorBoulanger, CMen_US
dc.contributor.authorKirchengast, Men_US
dc.contributor.authorVanhoutte, PMen_US
dc.date.accessioned2012-10-30T06:12:19Z-
dc.date.available2012-10-30T06:12:19Z-
dc.date.issued1994en_US
dc.identifier.citationJournal Of Cardiovascular Pharmacology, 1994, v. 24 n. 3, p. 517-522en_US
dc.identifier.issn0160-2446en_US
dc.identifier.urihttp://hdl.handle.net/10722/171129-
dc.description.abstractWe performed experiments to determine the effects of the combined 5- hydroxytryptamine2 (5-HT2) receptor and Ca2+ channel antagonist LU49938 ((2S)-5-[N-methyl-N-(n-hexyl)]amino-2-isopropyl-2(3.4.5-trimethoxy phenyl)- valeronitril-hydrochloride) on vascular smooth muscle (VSM) and endothelium in isolated porcine coronary arteries. Rings with and without endothelium were suspended in conventional organ chambers for measurement of isometric force. LU49938 inhibited contractions evoked by serotonin, norepinephrine (NE), and prostaglandin F(2α) (PGF(2α)) in a concentration-dependent and noncompetitive manner. The lower concentrations of LU49938 (10-7 and 10- 6 M) did not affect contractions to serotonin in the presence of ketanserin. However, a higher concentration of LU49938 (10-5 M) significantly decreased the concentration-response curve to the monoamine in the presence of ketanserin. These findings suggest that LU49938 has a dual inhibitory effect on contractions: selective inhibition of 5-HT2 receptor and nonselective inhibition of the contractile process in VSM. The mechanism of this nonselective inhibition of VSM is likely to be related to inhibition of Ca2+ entry because LU49938 inhibited responses to several agonists. The time course and degree of relaxation caused by LU49938 were comparable in rings with and without endothelium in control solution or after incubation with nitro-L-arginine and/or indomethacin. LU49938 did not affect endothelium-dependent relaxations induced by serotonin and bradykinin. These results suggest that LU49938 does not affect endothelium-dependent responses in porcine coronary artery.en_US
dc.languageengen_US
dc.publisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/en_US
dc.relation.ispartofJournal of Cardiovascular Pharmacologyen_US
dc.subject.meshAnalysis Of Varianceen_US
dc.subject.meshAnimalsen_US
dc.subject.meshCalcium-Binding Proteins - Antagonists & Inhibitorsen_US
dc.subject.meshCoronary Vessels - Drug Effectsen_US
dc.subject.meshDinoprost - Pharmacologyen_US
dc.subject.meshDose-Response Relationship, Drugen_US
dc.subject.meshEndothelium, Vascular - Drug Effectsen_US
dc.subject.meshKetanserin - Pharmacologyen_US
dc.subject.meshMaleen_US
dc.subject.meshMuscle Contraction - Drug Effectsen_US
dc.subject.meshMuscle Relaxation - Drug Effectsen_US
dc.subject.meshMuscle, Smooth, Vascular - Drug Effectsen_US
dc.subject.meshNorepinephrine - Pharmacologyen_US
dc.subject.meshSerotonin - Pharmacologyen_US
dc.subject.meshSerotonin Antagonists - Pharmacologyen_US
dc.subject.meshSwineen_US
dc.subject.meshVerapamil - Analogs & Derivatives - Pharmacologyen_US
dc.titleEffects of the combined 5-hydroxytryptamine2 receptor and Ca2+ channel antagonist LU49938 on the responsiveness of isolated porcine coronary arteries with and without endotheliumen_US
dc.typeArticleen_US
dc.identifier.emailVanhoutte, PM:vanhoutt@hku.hken_US
dc.identifier.authorityVanhoutte, PM=rp00238en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1097/00005344-199409000-00022-
dc.identifier.pmid7528308-
dc.identifier.scopuseid_2-s2.0-0028148085en_US
dc.identifier.volume24en_US
dc.identifier.issue3en_US
dc.identifier.spage517en_US
dc.identifier.epage522en_US
dc.identifier.isiWOS:A1994PC92900022-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridPark, SJ=7501828826en_US
dc.identifier.scopusauthoridBoulanger, CM=7006599024en_US
dc.identifier.scopusauthoridKirchengast, M=7004242148en_US
dc.identifier.scopusauthoridVanhoutte, PM=7202304247en_US

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