• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

ICS 205 - 930对心肌钾离子电导的抑制以及BRL 34915对其刺激的证据。

Evidence for inhibition by ICS 205-930 and stimulation by BRL 34915 of K+ conductance in cardiac muscle.

作者信息

Scholtysik G

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1987 Jun;335(6):692-6. doi: 10.1007/BF00166988.

DOI:10.1007/BF00166988
PMID:2442630
Abstract

Electrophysiological effects of the 5-HT3 receptor antagonist ICS 205-930 [(3 alpha-tropanyl)-1H-indole-3-carboxylic acid ester] were investigated in guinea pig isolated heart preparations. ICS 205-930 prolonged the functional refractory period and decreased the force of contraction in left driven atria. It decreased spontaneous beating rate in right atria. These effects were concentration dependent between 3 X 10(-6) and 10(-4) mol/l of ICS 205-930. In fast action potentials of papillary muscles ICS 205-930 concentration-dependently depressed Vmax and prolonged the action potential duration (APD) between 10(-6) and 10(-5) mol/l. The action potential amplitude (APA) and the resting membrane potential (RMP) remained unchanged. In papillary muscles partially depolarized by high K+ (22 mmol/l) and reactivated by high voltage stimulation, slow response APs were prolonged by ICS 205-930 10(-6) to 3 X 10(-5) mol. Vmax, APA and RMP were not affected. Similar effects on APD were obtained with sotalol (3 X 10(-5) mol/l), an inhibitor of outward K+ current. The slow-APD prolongation induced by ICS 205-930 as well as by sotalol was reversed by BRL 34915 (6-cyano-3,4-dihydro-2,2-dimethyltrans-4-(2-oxo-1-pyrrolidyl )-2H-benzo[b]pyran-3-ol), known to open K+ channels. BRL 34915 alone reduced slow-APD stereoselectively. The results suggest that ICS 205-930 may inhibit and BRL 34915 may stimulate the K+ conductance of guinea pig myocardial cell membranes.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在豚鼠离体心脏标本中研究了5-羟色胺3（5-HT3）受体拮抗剂ICS 205-930 [（3α-托烷）-1H-吲哚-3-羧酸酯]的电生理效应。ICS 205-930延长了功能性不应期，并降低了左驱动心房的收缩力。它降低了右心房的自发搏动率。在3×10⁻⁶至10⁻⁴mol/L的ICS 205-930浓度范围内，这些效应呈浓度依赖性。在乳头肌的快动作电位中，在10⁻⁶至10⁻⁵mol/L之间，ICS 205-930浓度依赖性地降低Vmax并延长动作电位持续时间（APD）。动作电位幅度（APA）和静息膜电位（RMP）保持不变。在被高钾（22 mmol/L）部分去极化并通过高压刺激重新激活的乳头肌中，慢反应动作电位被10⁻⁶至3×10⁻⁵mol的ICS 205-930延长。Vmax、APA和RMP不受影响。用索他洛尔（3×10⁻⁵mol/L，一种外向钾电流抑制剂）对APD也获得了类似的效应。由ICS 205-930以及索他洛尔诱导的慢APD延长可被已知能开放钾通道的BRL 34915（6-氰基-3,4-二氢-2,2-二甲基反式-4-（2-氧代-1-吡咯烷基）-2H-苯并[b]吡喃-3-醇）逆转。单独使用BRL 34915可立体选择性地降低慢APD。结果表明，ICS 205-930可能抑制而BRL 34915可能刺激豚鼠心肌细胞膜的钾电导。（摘要截短于250字）

相似文献

1
Evidence for inhibition by ICS 205-930 and stimulation by BRL 34915 of K+ conductance in cardiac muscle.ICS 205 - 930对心肌钾离子电导的抑制以及BRL 34915对其刺激的证据。
Naunyn Schmiedebergs Arch Pharmacol. 1987 Jun;335(6):692-6. doi: 10.1007/BF00166988.
2
BRL 34915 (cromakalim) activates ATP-sensitive K+ current in cardiac muscle.BRL 34915（克罗卡林）可激活心肌中的ATP敏感性钾电流。
Proc Natl Acad Sci U S A. 1988 Nov;85(21):8360-4. doi: 10.1073/pnas.85.21.8360.
3
5-Hydroxytryptamine antagonist ICS 205-930 blocks cardiac potassium, sodium and calcium currents.
J Pharmacol Exp Ther. 1988 Jun;245(3):773-8.
4
Differential class III and glibenclamide effects on action potential duration in guinea-pig papillary muscle during normoxia and hypoxia/ischaemia.在常氧及缺氧/缺血条件下，Ⅲ类药物与格列本脲对豚鼠乳头肌动作电位时程的不同影响。
Br J Pharmacol. 1993 Oct;110(2):531-8. doi: 10.1111/j.1476-5381.1993.tb13843.x.
5
Multiple cellular electrophysiological effects of a novel antiarrhythmic furoquinoline derivative HA-7 [N-benzyl-7-methoxy-2,3,4,9-tetrahydrofuro[2,3-b]quinoline-3,4-dione] in guinea pig cardiac preparations.新型抗心律失常呋喃喹啉衍生物HA-7 [N-苄基-7-甲氧基-2,3,4,9-四氢呋喃并[2,3-b]喹啉-3,4-二酮]对豚鼠心脏标本的多种细胞电生理效应。
J Pharmacol Exp Ther. 2006 Jan;316(1):380-91. doi: 10.1124/jpet.105.092106. Epub 2005 Sep 20.
6
Effects of SR 44866, a potassium channel opener, on action potentials of rabbit, guinea pig, and human heart fibers.钾通道开放剂SR 44866对兔、豚鼠和人心肌纤维动作电位的影响。
J Cardiovasc Pharmacol. 1991 May;17(5):692-700. doi: 10.1097/00005344-199105000-00002.
7
Differential rate and potassium-dependent effects of the class III agents d-sotalol and dofetilide on guinea pig papillary muscle.Ⅲ类药物d-索他洛尔和多非利特对豚鼠乳头肌的差异速率及钾依赖性效应
Cardiovasc Drugs Ther. 1998 Dec;12(6):573-83. doi: 10.1023/a:1007743521932.
8
Electrophysiological characterization of the class III activity of sotalol and its enantiomers. New interpretation of use-dependent effects.索他洛尔及其对映体Ⅲ类活性的电生理特性。使用依赖性效应的新解释。
Arzneimittelforschung. 1988 Feb;38(2):231-6.
9
Electromechanical action of dofetilide and D-sotalol during simulated metabolic acidosis in isolated guinea pig ventricular muscle.豚鼠离体心室肌模拟代谢性酸中毒时多非利特和D-索他洛尔的电机械作用
J Cardiovasc Pharmacol. 1992 Dec;20(6):889-94. doi: 10.1097/00005344-199212000-00007.
10
Voltage-dependent effects of YC-170, a dihydropyridine calcium channel modulator, in cardiovascular tissues.二氢吡啶类钙通道调节剂YC-170在心血管组织中的电压依赖性效应。
Naunyn Schmiedebergs Arch Pharmacol. 1986 Aug;333(4):421-30. doi: 10.1007/BF00500019.

引用本文的文献

1
The effects of SB 204070, a highly potent and selective 5-HT4 receptor antagonist, on guinea-pig distal colon.强效选择性5-羟色胺4（5-HT4）受体拮抗剂SB 204070对豚鼠远端结肠的作用。
Br J Pharmacol. 1994 Jul;112(3):789-94. doi: 10.1111/j.1476-5381.1994.tb13148.x.
2
Block of the delayed rectifier current (IK) by the 5-HT3 antagonists ondansetron and granisetron in feline ventricular myocytes.5-羟色胺3受体拮抗剂昂丹司琼和格拉司琼对猫心室肌细胞延迟整流电流（IK）的阻断作用
Br J Pharmacol. 1994 Oct;113(2):527-35. doi: 10.1111/j.1476-5381.1994.tb17021.x.
3
The negative inotropic effect of nicorandil is independent of cyclic GMP changes: a comparison with pinacidil and cromakalim in canine atrial muscle.

本文引用的文献

1
Drugs with a class III antiarrhythmic action.
Pharmacol Ther. 1982;17(3):315-55. doi: 10.1016/0163-7258(82)90020-1.
2
An investigation into the characteristics of reperfusion-induced arrhythmias in the anaesthetized rat and their susceptibility to antiarrhythmic agents.麻醉大鼠再灌注诱导性心律失常的特征及其对抗心律失常药物敏感性的研究。
Br J Pharmacol. 1984 Jun;82(2):349-57. doi: 10.1111/j.1476-5381.1984.tb10769.x.
3
Effect of 2-nicotinamidethyl nitrate (SG-75) on the membrane potential of left atrial muscle fibres of the dog. Increase in potassium conductance.2-硝酸烟酰胺乙酯（SG-75）对犬左心房肌纤维膜电位的影响。钾电导增加。
尼可地尔的负性肌力作用与环磷酸鸟苷变化无关：与匹莫齐特和克罗卡林在犬心房肌中的比较。
Br J Pharmacol. 1988 Oct;95(2):393-8. doi: 10.1111/j.1476-5381.1988.tb11658.x.
4
Phentolamine and structurally related compounds selectively antagonize the vascular actions of the K+ channel opener, cromromakalim.酚妥拉明及结构相关化合物可选择性拮抗钾通道开放剂色满卡林的血管作用。
Br J Pharmacol. 1989 Jul;97(3):941-9. doi: 10.1111/j.1476-5381.1989.tb12035.x.
5
Inhibition of the 5-HT-induced cardiogenic hypertensive chemoreflex by the selective 5-HT3 receptor antagonist ICS 205-930.选择性5-羟色胺3受体拮抗剂ICS 205-930对5-羟色胺诱导的心源性高血压化学反射的抑制作用。
Naunyn Schmiedebergs Arch Pharmacol. 1989 Mar;339(3):259-62. doi: 10.1007/BF00173574.
6
The pharmacology of ATP-sensitive K+ channels in the heart.
Pflugers Arch. 1989;414 Suppl 1:S93-8. doi: 10.1007/BF00582255.
7
The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons.胃肠道促动力苯甲酰胺衍生物是神经元中与腺苷酸环化酶正性偶联的非经典5-羟色胺受体（5-HT4）的激动剂。
Naunyn Schmiedebergs Arch Pharmacol. 1989 Oct;340(4):403-10. doi: 10.1007/BF00167041.
8
Interaction of potassium channel openers and blockers in canine atrial muscle.钾通道开放剂与阻滞剂在犬心房肌中的相互作用。
Br J Pharmacol. 1989 Jul;97(3):753-62. doi: 10.1111/j.1476-5381.1989.tb12013.x.
9
Electrophysiological effects of flecainide enantiomers in canine Purkinje fibres.氟卡尼对映体在犬浦肯野纤维中的电生理效应。
Naunyn Schmiedebergs Arch Pharmacol. 1989 Jun;339(6):625-9. doi: 10.1007/BF00168654.
10
BRL 34915 (cromakalim) activates ATP-sensitive K+ current in cardiac muscle.BRL 34915（克罗卡林）可激活心肌中的ATP敏感性钾电流。
Proc Natl Acad Sci U S A. 1988 Nov;85(21):8360-4. doi: 10.1073/pnas.85.21.8360.
Naunyn Schmiedebergs Arch Pharmacol. 1980 May;312(1):69-76. doi: 10.1007/BF00502577.
4
Effects of SG-75 (nicorandil) on electrical activity of canine cardiac Purkinje fibers: possible increase in potassium conductance.SG - 75（尼可地尔）对犬心脏浦肯野纤维电活动的影响：钾电导可能增加。
J Pharmacol Exp Ther. 1983 Apr;225(1):198-205.
5
Stimulation of slow action potentials in guinea pig papillary muscle cells by intracellular injection of cAMP, Gpp(NH)p, and cholera toxin.通过向豚鼠乳头肌细胞内注射环磷酸腺苷（cAMP）、鸟苷-5'-三磷酸-γ-亚胺（Gpp(NH)p）和霍乱毒素来刺激慢动作电位。
Circ Res. 1983 Jan;52(1):111-7. doi: 10.1161/01.res.52.1.111.
6
Antiarrhythmic and antifibrillatory actions of the levo- and dextrorotatory isomers of sotalol.索他洛尔左旋和右旋异构体的抗心律失常及抗纤颤作用。
J Cardiovasc Pharmacol. 1984 Nov-Dec;6(6):1132-41.
7
Prevention of ventricular fibrillation induced by coronary ligation.预防冠状动脉结扎诱发的心室颤动。
J Pharmacol Exp Ther. 1968 Dec;164(2):326-32.
8
Temporal relation between long-lasting aftercontractions and action potentials in cat papillary muscles.猫乳头肌中持续性后收缩与动作电位之间的时间关系。
Science. 1968 Jul 19;161(3838):293-5. doi: 10.1126/science.161.3838.293.
9
A third class of anti-arrhythmic action. Effects on atrial and ventricular intracellular potentials, and other pharmacological actions on cardiac muscle, of MJ 1999 and AH 3474.第三类抗心律失常作用。MJ 1999和AH 3474对心房和心室细胞内电位的影响以及对心肌的其他药理作用。
Br J Pharmacol. 1970 Aug;39(4):675-87. doi: 10.1111/j.1476-5381.1970.tb09893.x.
10
The effect of amiodarone, a new anti-anginal drug, on cardiac muscle.一种新型抗心绞痛药物胺碘酮对心肌的作用。
Br J Pharmacol. 1970 Aug;39(4):657-67. doi: 10.1111/j.1476-5381.1970.tb09891.x.