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Article: β-Adrenoceptor subtypes and the opening of plasmalemmal K +-channels in bovine trachealis muscle: Studies of mechanical activity and ion fluxes

Titleβ-Adrenoceptor subtypes and the opening of plasmalemmal K +-channels in bovine trachealis muscle: Studies of mechanical activity and ion fluxes
Authors
Issue Date1993
PublisherJohn Wiley & Sons Ltd. The Journal's web site is located at http://www.wiley.com/bw/journal.asp?ref=0007-1188&site=1
Citation
British Journal Of Pharmacology, 1993, v. 109 n. 4, p. 1149-1156 How to Cite?
Abstract1. Studies of mechanical activity and 86Rb + efflux have been made in bovine isolated trachealis with the objectives of (a) identifying which of the β-adrenoceptor subtypes mediates the opening of plasmalemmal K +-channels, (b) gaining further insight into the properties of the novel, long-acting β 2-adrenoceptor agonist, salmeterol and (c) clarifying the role of K +-channel opening in mediating the mechano-inhibitory actions of agonists at β-adrenoceptors. 2. In bovine trachealis muscle strips precontracted with histamine (460 μM), isoprenaline (0.1 nM-1 μM), procaterol (0.1-10 nm) and samleterol (0.1-10 nM) each caused concentration-dependent relaxation. 3. ICI 118551 (10 nM-1 μM) antagonized isoprenaline, procaterol and salmeterol in suppressing histamine-induced tone of the isolated trachealis muscle. The antagonism was concentration-dependent. In contrast, CGP 20712A (10 nM-1 μM) failed to antagonize isoprenaline, procaterol or salmeterol. 4. Salmeterol (1-10 μM) antagonized isoprenaline in relaxing strips of bovine trachea which had been precontracted with carbachol (1 μM). 5. Cromakalim (10 μM), isoprenaline (100 nM-10 μM), procaterol (10 nM-1 μM) and salbutamol (100 nM-10 μM) each promoted the efflux of 86Rb + from strips of bovine trachealis muscle preloaded with the radiotracer. In contrast, salmeterol (100 nM-10 μM) filed to promote 86Rb + efflux. 6. CGP 20712A (1 μM), ICI 118551 (100 nM) and salmeterol (1 μM) did not themselves modify 86Rb + efflux from trachealis muscle strips, nor did they affect the promotion of 86Rb + efflux induced by cromakalim (10 μM). In contrast, CGP 20712A (1 μM) and ICI 118551 (100 nM) were each able to inhibit the promotion of 86Rb + efflux induced by isoprenaline (1 μM) or procaterol (100 nM). Furthermore, salmeterol (10 μM) inhibited isoprenaline (1 μM)-induced promotion of 86Rb + efflux. 7. It is concluded that, in bovine trachealis, activation of either β 1- or β 2-adrenoceptors can promote the opening of 86Rb +-permeable K +-channels in the plasmalemma. The failure of salmeterol to promote plasmalemmal K +-channel opening may reflect, not its selectivity in activating β 2- as opposed to β 1-adrenoceptors, but rather its low intrinsic efficacy at β 2-adrenoceptors. The opening of plasmalemmal K +-channels plays a supportive rather than a crucial role in mediating the mechano-inhibitory effects of agonists at β-adrenoceptors acting on trachealis muscle.
Persistent Identifierhttp://hdl.handle.net/10722/169994
ISSN
2015 Impact Factor: 5.259
2015 SCImago Journal Rankings: 2.368
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorChiu, Pen_US
dc.contributor.authorCook, SJen_US
dc.contributor.authorSmall, RCen_US
dc.contributor.authorBerry, JLen_US
dc.contributor.authorCarpenter, JRen_US
dc.contributor.authorDowning, SJen_US
dc.contributor.authorFoster, RWen_US
dc.contributor.authorMiller, AJen_US
dc.contributor.authorSmall, AMen_US
dc.date.accessioned2012-10-30T06:04:36Z-
dc.date.available2012-10-30T06:04:36Z-
dc.date.issued1993en_US
dc.identifier.citationBritish Journal Of Pharmacology, 1993, v. 109 n. 4, p. 1149-1156en_US
dc.identifier.issn0007-1188en_US
dc.identifier.urihttp://hdl.handle.net/10722/169994-
dc.description.abstract1. Studies of mechanical activity and 86Rb + efflux have been made in bovine isolated trachealis with the objectives of (a) identifying which of the β-adrenoceptor subtypes mediates the opening of plasmalemmal K +-channels, (b) gaining further insight into the properties of the novel, long-acting β 2-adrenoceptor agonist, salmeterol and (c) clarifying the role of K +-channel opening in mediating the mechano-inhibitory actions of agonists at β-adrenoceptors. 2. In bovine trachealis muscle strips precontracted with histamine (460 μM), isoprenaline (0.1 nM-1 μM), procaterol (0.1-10 nm) and samleterol (0.1-10 nM) each caused concentration-dependent relaxation. 3. ICI 118551 (10 nM-1 μM) antagonized isoprenaline, procaterol and salmeterol in suppressing histamine-induced tone of the isolated trachealis muscle. The antagonism was concentration-dependent. In contrast, CGP 20712A (10 nM-1 μM) failed to antagonize isoprenaline, procaterol or salmeterol. 4. Salmeterol (1-10 μM) antagonized isoprenaline in relaxing strips of bovine trachea which had been precontracted with carbachol (1 μM). 5. Cromakalim (10 μM), isoprenaline (100 nM-10 μM), procaterol (10 nM-1 μM) and salbutamol (100 nM-10 μM) each promoted the efflux of 86Rb + from strips of bovine trachealis muscle preloaded with the radiotracer. In contrast, salmeterol (100 nM-10 μM) filed to promote 86Rb + efflux. 6. CGP 20712A (1 μM), ICI 118551 (100 nM) and salmeterol (1 μM) did not themselves modify 86Rb + efflux from trachealis muscle strips, nor did they affect the promotion of 86Rb + efflux induced by cromakalim (10 μM). In contrast, CGP 20712A (1 μM) and ICI 118551 (100 nM) were each able to inhibit the promotion of 86Rb + efflux induced by isoprenaline (1 μM) or procaterol (100 nM). Furthermore, salmeterol (10 μM) inhibited isoprenaline (1 μM)-induced promotion of 86Rb + efflux. 7. It is concluded that, in bovine trachealis, activation of either β 1- or β 2-adrenoceptors can promote the opening of 86Rb +-permeable K +-channels in the plasmalemma. The failure of salmeterol to promote plasmalemmal K +-channel opening may reflect, not its selectivity in activating β 2- as opposed to β 1-adrenoceptors, but rather its low intrinsic efficacy at β 2-adrenoceptors. The opening of plasmalemmal K +-channels plays a supportive rather than a crucial role in mediating the mechano-inhibitory effects of agonists at β-adrenoceptors acting on trachealis muscle.en_US
dc.languageengen_US
dc.publisherJohn Wiley & Sons Ltd. The Journal's web site is located at http://www.wiley.com/bw/journal.asp?ref=0007-1188&site=1en_US
dc.relation.ispartofBritish Journal of Pharmacologyen_US
dc.subject.meshAdrenergic Beta-Agonists - Pharmacologyen_US
dc.subject.meshAdrenergic Beta-Antagonists - Pharmacologyen_US
dc.subject.meshAminophylline - Pharmacologyen_US
dc.subject.meshAnimalsen_US
dc.subject.meshCattleen_US
dc.subject.meshCell Membrane - Drug Effects - Metabolismen_US
dc.subject.meshHistamine - Pharmacologyen_US
dc.subject.meshImidazoles - Pharmacologyen_US
dc.subject.meshIsometric Contraction - Drug Effects - Physiologyen_US
dc.subject.meshMuscle Relaxation - Drug Effects - Physiologyen_US
dc.subject.meshMuscle, Smooth - Drug Effects - Metabolismen_US
dc.subject.meshPotassium Channels - Drug Effects - Metabolismen_US
dc.subject.meshPropanolamines - Pharmacologyen_US
dc.subject.meshReceptors, Adrenergic, Beta - Drug Effects - Metabolismen_US
dc.subject.meshRubidium - Metabolismen_US
dc.subject.meshRubidium Radioisotopes - Diagnostic Useen_US
dc.subject.meshTrachea - Drug Effects - Metabolism - Physiologyen_US
dc.titleβ-Adrenoceptor subtypes and the opening of plasmalemmal K +-channels in bovine trachealis muscle: Studies of mechanical activity and ion fluxesen_US
dc.typeArticleen_US
dc.identifier.emailChiu, P:pkychiu@hkucc.hku.hken_US
dc.identifier.authorityChiu, P=rp00379en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1111/j.1476-5381.1993.tb13742.x-
dc.identifier.pmid8104644-
dc.identifier.scopuseid_2-s2.0-0027292138en_US
dc.identifier.volume109en_US
dc.identifier.issue4en_US
dc.identifier.spage1149en_US
dc.identifier.epage1156en_US
dc.identifier.isiWOS:A1993LN91700041-
dc.publisher.placeUnited Kingdomen_US
dc.identifier.scopusauthoridChiu, P=7202988127en_US
dc.identifier.scopusauthoridCook, SJ=15827218000en_US
dc.identifier.scopusauthoridSmall, RC=7202801795en_US
dc.identifier.scopusauthoridBerry, JL=7402634711en_US
dc.identifier.scopusauthoridCarpenter, JR=7402041041en_US
dc.identifier.scopusauthoridDowning, SJ=35615957500en_US
dc.identifier.scopusauthoridFoster, RW=7402461906en_US
dc.identifier.scopusauthoridMiller, AJ=7406230358en_US
dc.identifier.scopusauthoridSmall, AM=7005344072en_US

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