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Direct modulation of Ca(2+)-activated K(+) current by H-89 in rabbit coronary arterial smooth muscle cells

Cited 19 time in Web of Science Cited 0 time in Scopus
Authors
Park, Won Sun; Son, Youn Kyoung; Kim, Nari; Youm, Jae Boum; Warda, Mohamad; Ko, Jae-Hong; Ko, Eun A; Kang, Sung Hyun; Kim, Euiyong; Earm, Yung E.; Han, Jin
Issue Date
2006-10-21
Publisher
Elsevier
Citation
Vascul Pharmacol. 2007 Feb;46(2):105-13. Epub 2006 Sep 8.
Keywords
AnimalsCarbazoles/pharmacologyCoronary Circulation/drug effectsCoronary Vessels/drug effects/metabolismCyclic AMP/analogs & derivatives/pharmacologyCyclic AMP-Dependent Protein Kinases/antagonists & inhibitorsDose-Response Relationship, DrugEnzyme Inhibitors/pharmacologyIndoles/pharmacologyIsoquinolines/*pharmacologyMembrane Potentials/drug effectsMuscle, Smooth, Vascular/*drug effects/metabolismOkadaic Acid/pharmacologyPatch-Clamp TechniquesPhosphoprotein Phosphatases/antagonists & inhibitorsPotassium Channels, Calcium-Activated/*drug effects/metabolismProtein Kinase Inhibitors/*pharmacologyPyrroles/pharmacologyRabbitsSulfonamides/*pharmacologyThionucleotides/pharmacologyTime FactorsVascular Resistance/drug effects
Abstract
The effects of H-89, a potent and selective inhibitor of protein kinase A (PKA) on Ca(2+)-activated K(+) (BK(Ca)) channels in coronary arterial smooth muscle cells were examined using a patch-clamp technique. In inside-out configuration, H-89 increased the NP(o) of the BK(Ca) channel, but it reduced the dwell time of BK(Ca) currents. In whole-cell configuration, H-89 markedly increased BK(Ca) currents in a concentration-dependent manner. The EC(50) was 0.470+/-0.0741 microM based on dwell time, 0.582+/-0.0691 microM based on the NP(o), and 0.519+/-0.0295 microM based on the whole-cell current, respectively. H-85, which is an inactive form of H-89, increased BK(Ca) currents, similar to the result of H-89. The other PKA inhibitors (Rp-8-CPT-cAMPs and KT 5720) and protein phosphatase inhibitor (okadaic acid, 1 microM) had little effect on BK(Ca) currents and did not significantly alter the stimulatory effects of 1 microM H-89. These findings suggest that H-89 increases the BK(Ca) current independently of PKA.
ISSN
1537-1891 (Print)
Language
English
URI
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=17052962

http://hdl.handle.net/10371/26635
DOI
https://doi.org/10.1016/j.vph.2006.08.413
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College of Medicine/School of Medicine (의과대학/대학원)Dept. of Physiology (생리학교실)Journal Papers (저널논문_생리학교실)
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