ACTIVATION OF KV7.2 TO KV7.5 CHANNELS BY RETIGABINE MODULATES THE EFFECTS OF HISTAMINE AND 2-(2-PYRIDYL) ETHYLAMINE ON SMOOTH MUSCLES

被引：1

作者：

Zagorchev, Plamen ^{[1
]}

Apostolova, Elisaveta ^{[2
]}

Kokova, Vesela ^{[2
]}

Peychev, Lyudmil ^{[2
]}

Peychev, Zhivko ^{[3
]}

Draganova-Filipova, Milena ^{[4
,5
]}

机构：

[1] Med Univ Plovdiv, Dept Med Phys & Biophys, Fac Pharm, 15A Vassil Aprilov Blvd, Plovdiv 4002, Bulgaria

[2] Med Univ Plovdiv, Dept Pharmacol & Drug Toxicol, Fac Pharm, 15A Vassil Aprilov Blvd, Plovdiv 4002, Bulgaria

[3] Med Univ Plovdiv, Dept Med Informat Biostat & E Learning, Fac Publ Hlth, 15A Vassil Aprilov Blvd, Plovdiv 4002, Bulgaria

[4] Med Univ Plovdiv, Dept Med Biol, Fac Med, 15A Vassil Aprilov Blvd, Plovdiv 4002, Bulgaria

[5] Technol Ctr Emergency Med, 15A Vassil Aprilov Blvd, Plovdiv 4002, Bulgaria

来源：

COMPTES RENDUS DE L ACADEMIE BULGARE DES SCIENCES | 2018年 / 71卷 / 10期

关键词：

membrane hyperpolarization; guinea pig corpus smooth muscle; spontaneous smooth muscle contraction; EXPRESSION; ACETYLCHOLINE; CELLS;

D O I：

10.7546/CRABS.2018.10.18

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

Retigabine is an antiepileptic drug whose main mechanism of action involves opening of voltage-gated potassium channels (Kv7.2-Kv7.5). The aim of this study is to evaluate the effect of retigabine on the cell response to histamine and H-1 receptor agonist 2-(2-Pyridyl) ethylamine. We examined the effect of 10 mu M histamine and 10 mu M 2-(2-Pyridyl) ethylamine on spontaneous smooth muscle contraction of guinea pig gastric corpus strips before and after 20-min treatment with 2 mu M retigabine. The effect of 10 mu M histamine on the spontaneous smooth muscle contractility was diminished after treatment with 2 mu M retigabine. Similar results were observed with 2-(2-Pyridyl) ethylamine (H-1 receptor agonist). Activation of Kv7.2 to Kv7.5 channels by retigabine may lead to membrane hyperpolarization and may result in attenuated effects of histamine and 2-(2-Pyridyl) ethylamine on smooth muscles. A similar process could occur in the neurons, where Kv7 channels and Hi receptors are present.

引用

页码：1428 / 1436

页数：9

共 6 条

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Wuttke, TV
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MOLECULAR PHARMACOLOGY, 2005, 67 (04) : 1009 - 1017
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PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY, 2013, 465 (06): : 797 - 804
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Pflügers Archiv - European Journal of Physiology, 2013, 465 : 797 - 804
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Brueggemann, Lyubov, I
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MOLECULAR PHARMACOLOGY, 2020, 97 (03) : 145 - 158
[6] Interaction of Gq- and Gs-coupled Pathways in the Regulation of Ca2+ Spiking and Activity of Kv7.5 Potassium Channels in A7r5 Vascular Smooth Muscle Cells
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FASEB JOURNAL, 2016, 30

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