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The anticholinergic drug oxybutynin inhibits voltage-dependent K + channels in coronary arterial smooth muscle cells

The anticholinergic drug oxybutynin inhibits voltage-dependent K + channels in coronary arterial smooth muscle cells

Hongliang Li, Mi Seon Seo, Jin Ryeol An, Hee Seok Jung, Kwon-Soo Ha, Eun-Taek Han, Seok-Ho Hong, Young Min Bae, Dong Ryeol Ryu, Won Sun Park

Clin Exp Pharmacol Physiol. 2019 Nov;46(11):1030-1036.

PMID: 31330060

Abstract:

This study demonstrates the inhibitory effect of anticholinergic drug oxybutynin on voltage-dependent K+ (Kv) channels in rabbit coronary arterial smooth muscle cells. Oxybutynin inhibited vascular Kv channels in a concentration-dependent manner, with an IC50 value of 11.51 ± 0.38 μmol/L and a Hill coefficient (n) of 2.25 ± 0.12. Application of oxybutynin shifted the activation curve to the right and the inactivation curve to the left. Pretreatment with the Kv1.5 subtype inhibitor DPO-1 and the Kv2.1 subtype inhibitor guangxitoxin suppressed the oxybutynin-induced inhibition of the Kv current. However, application of the Kv7 subtype inhibitor linopirdine did not affect the inhibition by oxybutynin of the Kv current. The anticholinergic drug atropine did not inhibit the Kv current nor influence oxybutynin-induced inhibition of the Kv current. From these results, we concluded that oxybutynin inhibited the vascular Kv current in a concentration-dependent manner by influencing the steady-state activation and inactivation curves independent of its anticholinergic effect.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP43077301	DPO-1		43077-30-1	Price

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