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Article: Effects of SCA40 on bovine trachealis muscle and on cyclic nucleotide phosphodiesterases

TitleEffects of SCA40 on bovine trachealis muscle and on cyclic nucleotide phosphodiesterases
Authors
Issue Date1997
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejphar
Citation
European Journal Of Pharmacology, 1997, v. 334 n. 1, p. 75-85 How to Cite?
AbstractWhile UK-93,928 (1-[[3-(6,9-dihydro-6-oxo-9-propyl-1H-purin-2-yl)-4-ethoxyphenyl] sulfonyl]-4-methylpiperazine; 5 nM-5 μM) was devoid of relaxant activity, benzafentrine, isoprenaline, levcromakalim and SCA40 (6-bromo-8-methylaminoimidazo [1,2-a]pyrazine-2-carbonitrile) each relaxed histamine (460 μM)-precontracted bovine isolated trachealis. Each of these relaxants was antagonised by a K +-rich (80 mM) medium. Except in the case of levcromakalim, nifedipine (1 μM) offset this antagonism. Charybdotoxin (100 nM) antagonised isoprenaline in a nifedipine-sensitive manner but did not antagonise SCA40 or benzafentrine. Iberiotoxin (100 nM) did not antagonise SCA40. Acting on tissue precontracted with carbachol, SCA40 potentiated isoprenaline but did not potentiate sodium nitroprusside. While levcromakalim (1 and 10 μM) induced hyperpolarisation, SCA40 (1 and 10 μM) induced little change in the membrane potential of bovine trachealis. In trachealis preloaded with 86Rb +, levcromakalim (1 and 10 μM) promoted efflux of the radiotracer while SCA40 (1 and 10 μM) had no effect. Tested as an inhibitor of isoenzymes of cyclic nucleotide phosphodiesterase, SCA40 was most potent against the type III, less potent against the type IV and least potent against the type I isoenzyme. It is concluded that neither inhibition of phosphodiesterase type V nor the promotion of BK(Ca) channel opening explains the tracheal smooth muscle relaxant activity of SCA40. This compound relaxes bovine tracheal smooth muscle mainly by inhibiting phosphodiesterase isoenzyme types III and IV.
Persistent Identifierhttp://hdl.handle.net/10722/170009
ISSN
2015 Impact Factor: 2.73
2015 SCImago Journal Rankings: 1.115
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorPocock, TMen_US
dc.contributor.authorLaurent, Fen_US
dc.contributor.authorIsaac, LMen_US
dc.contributor.authorChiu, Pen_US
dc.contributor.authorElliott, KRFen_US
dc.contributor.authorFoster, RWen_US
dc.contributor.authorMichel, Aen_US
dc.contributor.authorBonnet, PAen_US
dc.contributor.authorSmall, RCen_US
dc.date.accessioned2012-10-30T06:04:42Z-
dc.date.available2012-10-30T06:04:42Z-
dc.date.issued1997en_US
dc.identifier.citationEuropean Journal Of Pharmacology, 1997, v. 334 n. 1, p. 75-85en_US
dc.identifier.issn0014-2999en_US
dc.identifier.urihttp://hdl.handle.net/10722/170009-
dc.description.abstractWhile UK-93,928 (1-[[3-(6,9-dihydro-6-oxo-9-propyl-1H-purin-2-yl)-4-ethoxyphenyl] sulfonyl]-4-methylpiperazine; 5 nM-5 μM) was devoid of relaxant activity, benzafentrine, isoprenaline, levcromakalim and SCA40 (6-bromo-8-methylaminoimidazo [1,2-a]pyrazine-2-carbonitrile) each relaxed histamine (460 μM)-precontracted bovine isolated trachealis. Each of these relaxants was antagonised by a K +-rich (80 mM) medium. Except in the case of levcromakalim, nifedipine (1 μM) offset this antagonism. Charybdotoxin (100 nM) antagonised isoprenaline in a nifedipine-sensitive manner but did not antagonise SCA40 or benzafentrine. Iberiotoxin (100 nM) did not antagonise SCA40. Acting on tissue precontracted with carbachol, SCA40 potentiated isoprenaline but did not potentiate sodium nitroprusside. While levcromakalim (1 and 10 μM) induced hyperpolarisation, SCA40 (1 and 10 μM) induced little change in the membrane potential of bovine trachealis. In trachealis preloaded with 86Rb +, levcromakalim (1 and 10 μM) promoted efflux of the radiotracer while SCA40 (1 and 10 μM) had no effect. Tested as an inhibitor of isoenzymes of cyclic nucleotide phosphodiesterase, SCA40 was most potent against the type III, less potent against the type IV and least potent against the type I isoenzyme. It is concluded that neither inhibition of phosphodiesterase type V nor the promotion of BK(Ca) channel opening explains the tracheal smooth muscle relaxant activity of SCA40. This compound relaxes bovine tracheal smooth muscle mainly by inhibiting phosphodiesterase isoenzyme types III and IV.en_US
dc.languageengen_US
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejpharen_US
dc.relation.ispartofEuropean Journal of Pharmacologyen_US
dc.subject.meshAnimalsen_US
dc.subject.meshBronchodilator Agents - Pharmacologyen_US
dc.subject.meshCattleen_US
dc.subject.meshCromakalim - Pharmacologyen_US
dc.subject.meshDose-Response Relationship, Drugen_US
dc.subject.meshElectrophysiologyen_US
dc.subject.meshGlycoproteins - Drug Effectsen_US
dc.subject.meshImidazoles - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshIsoproterenol - Pharmacologyen_US
dc.subject.meshMembrane Potentials - Drug Effectsen_US
dc.subject.meshMuscle Relaxation - Drug Effectsen_US
dc.subject.meshParasympatholytics - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshPyrazines - Antagonists & Inhibitors - Pharmacologyen_US
dc.subject.meshRubidium - Metabolismen_US
dc.subject.meshTrachea - Drug Effects - Metabolismen_US
dc.titleEffects of SCA40 on bovine trachealis muscle and on cyclic nucleotide phosphodiesterasesen_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.doi10.1016/S0014-2999(97)01147-3en_US
dc.identifier.pmid9346331-
dc.identifier.scopuseid_2-s2.0-0030760455en_US
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0030760455&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume334en_US
dc.identifier.issue1en_US
dc.identifier.spage75en_US
dc.identifier.epage85en_US
dc.identifier.isiWOS:A1997YB22100010-
dc.publisher.placeNetherlandsen_US
dc.identifier.scopusauthoridPocock, TM=6603270266en_US
dc.identifier.scopusauthoridLaurent, F=7101921601en_US
dc.identifier.scopusauthoridIsaac, LM=8083681800en_US
dc.identifier.scopusauthoridChiu, P=7202988127en_US
dc.identifier.scopusauthoridElliott, KRF=7102778451en_US
dc.identifier.scopusauthoridFoster, RW=7402461906en_US
dc.identifier.scopusauthoridMichel, A=7201401514en_US
dc.identifier.scopusauthoridBonnet, PA=20733537000en_US
dc.identifier.scopusauthoridSmall, RC=7202801795en_US

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