S-Space College of Medicine/School of Medicine (의과대학/대학원) Dept. of Physiology (생리학교실) Journal Papers (저널논문_생리학교실)
Direct inhibition of a PKA inhibitor, H-89 on KV channels in rabbit coronary arterial smooth muscle cells
- 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
- Biochem Biophys Res Commun. 2006 Mar 24;341(4):931-7. Epub 2006 Jan 23.
- 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
- 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.
- 0006-291X (Print)
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