title: Y-27632, a Rho-Associated Protein Kinase Inhibitor, Inhibits Voltage-Dependent K+ Channels in Rabbit Coronary Arterial Smooth Muscle Cells.
abstract: We examined the effects of the Rho-associated protein kinase (ROCK) inhibitor Y-27632 on voltage-dependent K+ (Kv) channels in rabbit coronary arterial smooth muscle cells using the whole-cell patch clamp technique. Y-27632 reduced the amplitude of the Kv current in a concentration-dependent manner, with an IC50 of 0.87 ± 0.06 μmol/l and a Hill coefficient of 1.48 ± 0.06. Y-27632 did not affect the steady-state activation or inactivation curves, suggesting that the drug does not affect the voltage sensitivity of Kv channels. Another ROCK inhibitor, H-1152, did not affect the Kv current and had no significant effect on the Y-27632-induced inhibition of Kv channels, indicating that the inhibitory effect of Y-27632 on the Kv current is independent of ROCK signaling. From these results, we conclude that Y-27632 inhibits the Kv channel current in a dose-dependent and ROCK signaling-independent manner.
authors.affiliation: Department of Physiology, Kangwon National University School of Medicine, Chuncheon, South Korea.
authors.forename: Hongliang
authors.initials: H
authors.lastname: Li
authors.forename: Sung Eun
authors.initials: SE
authors.lastname: Shin
authors.forename: Hye Won
authors.initials: HW
authors.lastname: Kim
authors.forename: Han Sol
authors.initials: HS
authors.lastname: Kim
authors.forename: Won-Kyo
authors.initials: WK
authors.lastname: Jung
authors.forename: Kwon-Soo
authors.initials: KS
authors.lastname: Ha
authors.forename: Eun-Taek
authors.initials: ET
authors.lastname: Han
authors.forename: Seok-Ho
authors.initials: SH
authors.lastname: Hong
authors.forename: Il-Whan
authors.initials: IW
authors.lastname: Choi
authors.forename: Young Min
authors.initials: YM
authors.lastname: Bae
authors.forename: Amy L
authors.initials: AL
authors.lastname: Firth
authors.forename: Hyoweon
authors.initials: H
authors.lastname: Bang
authors.forename: Won Sun
authors.initials: WS
authors.lastname: Park
mesh_terms: D000577:Amides / Q000494:pharmacology*; D000818:Animals; D003331:Coronary Vessels / Q000187:drug effects* / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D008297:Male; D032389:Myocytes, Smooth Muscle / Q000187:drug effects* / Q000502:physiology; D024642:Potassium Channels, Voltage-Gated / Q000037:antagonists & inhibitors* / Q000502:physiology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D011725:Pyridines / Q000494:pharmacology*; D011817:Rabbits; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors* / Q000502:physiology
chemical_list: D000577:Amides; D024642:Potassium Channels, Voltage-Gated; D047428:Protein Kinase Inhibitors; D011725:Pyridines; C108830:Y 27632; D054460:rho-Associated Kinases