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Article: Alpha-1 and alpha-2 adrenoceptor: Response coupling in canine saphenous and femoral veins

TitleAlpha-1 and alpha-2 adrenoceptor: Response coupling in canine saphenous and femoral veins
Authors
Issue Date1986
PublisherAmerican Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.org
Citation
Journal Of Pharmacology And Experimental Therapeutics, 1986, v. 238 n. 1, p. 131-138 How to Cite?
AbstractThe aim of the present study was to analyze alpha-1 and alpha-2 adrenoceptor response coupling in isolated canine blood vessels. Rings of saphenous and femoral veins and of femoral arteries were suspended for isometric tension recording in modified Krebs-Ringer bicarbonate solution, gassed with 95% O2-5% CO2 and maintained at 37°C. Dissociation constants for the alpha-1 adrenergic agonists, phenylephrine and cirazoline, and the alpha-2 adrenergic agonist, UK 14,304, were determined by analysis of concentration-effect curves to the agonists under control conditions and after partial inactivation of alpha adrenoceptors by phenoxybenzamine. The dissociation constant of phenylephrine for alpha-1 adrenoceptors in saphenous veins was approximately 10-fold higher than that obtained for the agonist in femoral arteries or femoral veins. Similarly the dissociation constant for cirazoline in the saphenous vein was higher than that obtained in other alpha-1 adrenergic systems. Dissociation constants were used to determine alpha adrenoceptor occupancy-response relationships. The alpha-1 adrenergic responses evoked by intrinsic-efficacy agonists (cirazoline and phenylephrine) were associated with a very large receptor-reserve in the saphenous vein, but no, or only a limited receptor-reserve in the femoral vein. The dissociation constant for UK 14,304 in saphenous veins was significantly lower than that obtained for alpha-2 adrenergic stimulation by norepinephrine. There was no alpha-2 adrenoceptor reserve in the saphenous vein for these putative high intrinsic-efficacy agonists. The differences in receptor-reserve between alpha-1 adrenoceptors in canine saphenous and femoral veins and between alpha-1 and alpha-2 adrenoceptors in saphenous veins may help to explain the differential modulation of adrenergic responses in these blood vessels.
Persistent Identifierhttp://hdl.handle.net/10722/170814
ISSN
2015 Impact Factor: 3.76
2015 SCImago Journal Rankings: 1.847
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorFlavahan, NAen_US
dc.contributor.authorVanhoutte, PMen_US
dc.date.accessioned2012-10-30T06:10:58Z-
dc.date.available2012-10-30T06:10:58Z-
dc.date.issued1986en_US
dc.identifier.citationJournal Of Pharmacology And Experimental Therapeutics, 1986, v. 238 n. 1, p. 131-138en_US
dc.identifier.issn0022-3565en_US
dc.identifier.urihttp://hdl.handle.net/10722/170814-
dc.description.abstractThe aim of the present study was to analyze alpha-1 and alpha-2 adrenoceptor response coupling in isolated canine blood vessels. Rings of saphenous and femoral veins and of femoral arteries were suspended for isometric tension recording in modified Krebs-Ringer bicarbonate solution, gassed with 95% O2-5% CO2 and maintained at 37°C. Dissociation constants for the alpha-1 adrenergic agonists, phenylephrine and cirazoline, and the alpha-2 adrenergic agonist, UK 14,304, were determined by analysis of concentration-effect curves to the agonists under control conditions and after partial inactivation of alpha adrenoceptors by phenoxybenzamine. The dissociation constant of phenylephrine for alpha-1 adrenoceptors in saphenous veins was approximately 10-fold higher than that obtained for the agonist in femoral arteries or femoral veins. Similarly the dissociation constant for cirazoline in the saphenous vein was higher than that obtained in other alpha-1 adrenergic systems. Dissociation constants were used to determine alpha adrenoceptor occupancy-response relationships. The alpha-1 adrenergic responses evoked by intrinsic-efficacy agonists (cirazoline and phenylephrine) were associated with a very large receptor-reserve in the saphenous vein, but no, or only a limited receptor-reserve in the femoral vein. The dissociation constant for UK 14,304 in saphenous veins was significantly lower than that obtained for alpha-2 adrenergic stimulation by norepinephrine. There was no alpha-2 adrenoceptor reserve in the saphenous vein for these putative high intrinsic-efficacy agonists. The differences in receptor-reserve between alpha-1 adrenoceptors in canine saphenous and femoral veins and between alpha-1 and alpha-2 adrenoceptors in saphenous veins may help to explain the differential modulation of adrenergic responses in these blood vessels.en_US
dc.languageengen_US
dc.publisherAmerican Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.orgen_US
dc.relation.ispartofJournal of Pharmacology and Experimental Therapeuticsen_US
dc.subject.meshAnimalsen_US
dc.subject.meshDogsen_US
dc.subject.meshDose-Response Relationship, Drugen_US
dc.subject.meshFemaleen_US
dc.subject.meshFemoral Vein - Metabolismen_US
dc.subject.meshImidazoles - Metabolismen_US
dc.subject.meshMaleen_US
dc.subject.meshMathematicsen_US
dc.subject.meshNorepinephrine - Pharmacologyen_US
dc.subject.meshPhenoxybenzamine - Pharmacologyen_US
dc.subject.meshPhenylephrine - Metabolismen_US
dc.subject.meshQuinoxalines - Pharmacologyen_US
dc.subject.meshReceptors, Adrenergic, Alpha - Metabolismen_US
dc.subject.meshSaphenous Vein - Metabolismen_US
dc.titleAlpha-1 and alpha-2 adrenoceptor: Response coupling in canine saphenous and femoral veinsen_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.pmid3014111-
dc.identifier.scopuseid_2-s2.0-0022510759en_US
dc.identifier.volume238en_US
dc.identifier.issue1en_US
dc.identifier.spage131en_US
dc.identifier.epage138en_US
dc.identifier.isiWOS:A1986D211300021-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridFlavahan, NA=7006398882en_US
dc.identifier.scopusauthoridVanhoutte, PM=7202304247en_US

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