Jin Ryeol An, Hojung Kang, Hongliang Li, Mi Seon Seo, Hee Seok Jung, Won-Kyo Jung, Il-Whan Choi, Sook Won Ryu, Hongzoo Park, Young Min Bae, Se Min Ryu, Won Sun Park
In this study, we explore the inhibitory effects of protriptyline, a tricyclic antidepressant drug, on voltage-dependent K+ (Kv) channels of rabbit coronary arterial smooth muscle cells using a whole-cell patch clamp technique. Protriptyline inhibited the vascular Kv current in a concentration-dependent manner, with an IC50 value of 5.05 ± 0.97 μM and a Hill coefficient of 0.73 ± 0.04. Protriptyline did not affect the steady-state activation kinetics. However, the drug shifted the steady-state inactivation curve to the left, suggesting that protriptyline inhibited the Kv channels by changing their voltage sensitivity...
March 18, 2020: Acta Biochimica et Biophysica Sinica