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Direct inhibition of a PKA inhibitor, H-89 on KV channels in rabbit coronary arterial smooth muscle cells

Cited 26 time in Web of Science Cited 0 time in Scopus
Authors
Son, Youn Kyoung; Park, Won Sun; Kim, Sung Joon; Earm, Yung E.; Kim, Nari; Youm, Jae Boum; Warda, Mohamad; Kim, Euiyong; Han, Jin
Issue Date
2006-02-04
Publisher
Elsevier
Citation
Biochem Biophys Res Commun. 2006 Mar 24;341(4):931-7. Epub 2006 Jan 23.
Keywords
AnimalsCarbazoles/pharmacologyCoronary Vessels/cytology/drug effectsCyclic AMP/analogs & derivatives/pharmacologyCyclic AMP-Dependent Protein Kinases/*antagonists & inhibitorsFemaleIndoles/pharmacologyIsoquinolines/*pharmacologyMaleMuscle, Smooth, Vascular/*cytology/drug effectsPotassium Channels, Voltage-Gated/*drug effectsPyrroles/pharmacologyRabbitsSulfonamides/*pharmacologyThionucleotides/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

http://hdl.handle.net/10371/23380
DOI
https://doi.org/10.1016/j.bbrc.2006.01.053
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College of Medicine/School of Medicine (의과대학/대학원)Dept. of Physiology (생리학교실)Journal Papers (저널논문_생리학교실)
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