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Direct modulation of Ca(2+)-activated K(+) current by H-89 in rabbit coronary arterial smooth muscle cells
Cited 20 time in
Web of Science
Cited 21 time in Scopus
- Authors
- Issue Date
- 2006-10-21
- Publisher
- Elsevier
- Citation
- Vascul Pharmacol. 2007 Feb;46(2):105-13. Epub 2006 Sep 8.
- Keywords
- Animals ; Carbazoles/pharmacology ; Coronary Circulation/drug effects ; Coronary Vessels/drug effects/metabolism ; Cyclic AMP/analogs & derivatives/pharmacology ; Cyclic AMP-Dependent Protein Kinases/antagonists & inhibitors ; Dose-Response Relationship, Drug ; Enzyme Inhibitors/pharmacology ; Indoles/pharmacology ; Isoquinolines/*pharmacology ; Membrane Potentials/drug effects ; Muscle, Smooth, Vascular/*drug effects/metabolism ; Okadaic Acid/pharmacology ; Patch-Clamp Techniques ; Phosphoprotein Phosphatases/antagonists & inhibitors ; Potassium Channels, Calcium-Activated/*drug effects/metabolism ; Protein Kinase Inhibitors/*pharmacology ; Pyrroles/pharmacology ; Rabbits ; Sulfonamides/*pharmacology ; Thionucleotides/pharmacology ; Time Factors ; Vascular 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
https://hdl.handle.net/10371/26635
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