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Article: Effects of CRL 40134 on the adrenergic neuroeffector interaction in the canine saphenous vein

TitleEffects of CRL 40134 on the adrenergic neuroeffector interaction in the canine saphenous vein
Authors
Keywordsadrenergic neurotransmission
buflomedil
release of norepinephrine
subtypes of alpha adrenergic receptors
Issue Date1990
PublisherBlackwell Publishing Ltd. The Journal's web site is located at http://www.blackwellpublishing.com/journals/FCP
Citation
Fundamental And Clinical Pharmacology, 1990, v. 4 n. 5, p. 525-538 How to Cite?
AbstractExperiments were designed to determine the effect of CRL 41034, a buflomedil analogue, on the adrenergic responsiveness of canine veins. Rings of saphenous vein (without endothelium) were suspended for isometric tension recording in modified Krebs-Ringer bicarbonate solution at 37°C. CRL 41034 produced a concentration-dependent inhibition of the contractions evoked by the alpha adrenergic agonists norepinephrine, phenylephrine and UK 14304 which was insensitive to the blockade of neuronal uptake by cocaine. CRL 41034 was more potent in inhibiting the concentration-dependent contractions evoked by UK 14304 than those by phenylephrine and the antagonism it caused against the response to UK 14304 fulfilled the criteria for competitivity. CRL 41034, at 10-5 M significantly depressed, and at 10-4 M abolished the contractions induced by electrical stimulation of the adrenergic nerves and those evoked by the indirect sympathomimetic amine tyramine. Strips of canine saphenous vein were superfused after incubation with [3H] norepinephrine. During sympathetic nerve activation, CRL 41304 increased the stimulation-evoked overflow of [3H] norepinephrine and 3-methoxy-4-dihydroxyphenylglycol; in the presence of rauwolscine the compound only increased the stimulation-evoked overflow of 3,4-dihydroxyphenylglycol. These experiments suggest that the major vascular effects of CRL 41304 in canine veins are blockade of alpha2-adrenoceptors on vascular smooth muscle, and inhibition of prejunctional alpha2-adrenoceptors on adrenergic nerve endings.
Persistent Identifierhttp://hdl.handle.net/10722/170980
ISSN
2023 Impact Factor: 2.1
2023 SCImago Journal Rankings: 0.586
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorBoulanger, Cen_US
dc.contributor.authorFlavahan, NAen_US
dc.contributor.authorKatusic, ZSen_US
dc.contributor.authorKomori, Ken_US
dc.contributor.authorVos, AAen_US
dc.contributor.authorVanhoutte, PMen_US
dc.date.accessioned2012-10-30T06:11:42Z-
dc.date.available2012-10-30T06:11:42Z-
dc.date.issued1990en_US
dc.identifier.citationFundamental And Clinical Pharmacology, 1990, v. 4 n. 5, p. 525-538en_US
dc.identifier.issn0767-3981en_US
dc.identifier.urihttp://hdl.handle.net/10722/170980-
dc.description.abstractExperiments were designed to determine the effect of CRL 41034, a buflomedil analogue, on the adrenergic responsiveness of canine veins. Rings of saphenous vein (without endothelium) were suspended for isometric tension recording in modified Krebs-Ringer bicarbonate solution at 37°C. CRL 41034 produced a concentration-dependent inhibition of the contractions evoked by the alpha adrenergic agonists norepinephrine, phenylephrine and UK 14304 which was insensitive to the blockade of neuronal uptake by cocaine. CRL 41034 was more potent in inhibiting the concentration-dependent contractions evoked by UK 14304 than those by phenylephrine and the antagonism it caused against the response to UK 14304 fulfilled the criteria for competitivity. CRL 41034, at 10-5 M significantly depressed, and at 10-4 M abolished the contractions induced by electrical stimulation of the adrenergic nerves and those evoked by the indirect sympathomimetic amine tyramine. Strips of canine saphenous vein were superfused after incubation with [3H] norepinephrine. During sympathetic nerve activation, CRL 41304 increased the stimulation-evoked overflow of [3H] norepinephrine and 3-methoxy-4-dihydroxyphenylglycol; in the presence of rauwolscine the compound only increased the stimulation-evoked overflow of 3,4-dihydroxyphenylglycol. These experiments suggest that the major vascular effects of CRL 41304 in canine veins are blockade of alpha2-adrenoceptors on vascular smooth muscle, and inhibition of prejunctional alpha2-adrenoceptors on adrenergic nerve endings.en_US
dc.languageengen_US
dc.publisherBlackwell Publishing Ltd. The Journal's web site is located at http://www.blackwellpublishing.com/journals/FCPen_US
dc.relation.ispartofFundamental and Clinical Pharmacologyen_US
dc.subjectadrenergic neurotransmission-
dc.subjectbuflomedil-
dc.subjectrelease of norepinephrine-
dc.subjectsubtypes of alpha adrenergic receptors-
dc.subject.meshAdrenergic Alpha-Agonists - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshAdrenergic Alpha-Antagonists - Pharmacologyen_US
dc.subject.meshAnimalsen_US
dc.subject.meshDogsen_US
dc.subject.meshElectric Stimulationen_US
dc.subject.meshFemaleen_US
dc.subject.meshIsometric Contraction - Drug Effectsen_US
dc.subject.meshMaleen_US
dc.subject.meshNorepinephrine - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshPhenylephrine - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshPiperidines - Pharmacologyen_US
dc.subject.meshPyrrolidines - Pharmacologyen_US
dc.subject.meshQuinoxalines - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshSaphenous Vein - Drug Effects - Physiologyen_US
dc.titleEffects of CRL 40134 on the adrenergic neuroeffector interaction in the canine saphenous veinen_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.doi10.1111/j.1472-8206.1990.tb00037.x-
dc.identifier.pmid1981202-
dc.identifier.scopuseid_2-s2.0-0025197391en_US
dc.identifier.volume4en_US
dc.identifier.issue5en_US
dc.identifier.spage525en_US
dc.identifier.epage538en_US
dc.identifier.isiWOS:A1990EC87200005-
dc.publisher.placeUnited Kingdomen_US
dc.identifier.scopusauthoridBoulanger, C=7006599024en_US
dc.identifier.scopusauthoridFlavahan, NA=7006398882en_US
dc.identifier.scopusauthoridKatusic, ZS=7006971465en_US
dc.identifier.scopusauthoridKomori, K=8977740100en_US
dc.identifier.scopusauthoridVos, AA=7102306924en_US
dc.identifier.scopusauthoridVanhoutte, PM=7202304247en_US
dc.identifier.issnl0767-3981-

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