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Direct inhibition of a PKA inhibitor, H-89 on KV channels in rabbit coronary arterial smooth muscle cells
Cited 27 time in
Web of Science
Cited 26 time in Scopus
- Authors
- Issue Date
- 2006-02-04
- Publisher
- Elsevier
- Citation
- Biochem Biophys Res Commun. 2006 Mar 24;341(4):931-7. Epub 2006 Jan 23.
- Keywords
- Animals ; Carbazoles/pharmacology ; Coronary Vessels/cytology/drug effects ; Cyclic AMP/analogs & derivatives/pharmacology ; Cyclic AMP-Dependent Protein Kinases/*antagonists & inhibitors ; Female ; Indoles/pharmacology ; Isoquinolines/*pharmacology ; Male ; Muscle, Smooth, Vascular/*cytology/drug effects ; Potassium Channels, Voltage-Gated/*drug effects ; Pyrroles/pharmacology ; Rabbits ; Sulfonamides/*pharmacology ; Thionucleotides/pharmacology
- Abstract
- We examined the effects of the protein kinase A (PKA) inhibitor H-89 on voltage-dependent K(+) (K(V)) currents in freshly isolated rabbit coronary arterial smooth muscle cells, using a whole-cell patch clamp technique. H-89 inhibited the K(V) current in a concentration-dependent manner, with a K(d) value of 1.02 microM. However, the PKA inhibitors KT 5720 and Rp-8-CPT-cAMPS did not significantly alter the K(V) current or the inhibitory effects of H-89 on the K(V) current. Moreover, H-85, a structurally similar but inactive analog of H-89, showed similar inhibitory effects on the K(V) channel. H-89 had no effect on the voltage-dependency of activation or inactivation, or on recovery kinetics. These results suggest that in rabbit coronary arterial smooth muscle cells, H-89 inhibits the K(V) current directly by blocking the pore cavity, an effect independent of PKA inhibition.
- ISSN
- 0006-291X (Print)
- Language
- English
- URI
- http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=16455049
https://hdl.handle.net/10371/23380
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