• 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

Blockade of human atrial 5-HT4 receptors by SB 207710, a selective and high affinity 5-HT4 receptor antagonist.

作者信息

Kaumann A J, Gaster L M, King F D, Brown A M

机构信息

Clinical Pharmacology Unit, University of Cambridge, Addenbrooke's Hospital, UK.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1994 May;349(5):546-8. doi: 10.1007/BF00169146.

DOI:10.1007/BF00169146
PMID:7915008
Abstract

The mode of antagonism of 5-hydroxytryptamine-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist SB 207710 (1-butyl-4-piperidinyl) methyl 8-amino-7-iodo-1,4-benzodioxan-5-carboxylate) was investigated on isolated preparations of human right atrial appendage. SB 207710 caused concentration-dependent (0.1-10 nmol/l) surmountable antagonism of the effects of 5-hydroxytryptamine with a pKB (mol/l) of 10.1. Due to its high selectivity and affinity, SB 207710 could be a powerful tool for the comparison of human atrial 5-HT4 receptors with 5-HT4 receptors of other organs of man and other species.

摘要

相似文献

1
Blockade of human atrial 5-HT4 receptors by SB 207710, a selective and high affinity 5-HT4 receptor antagonist.
Naunyn Schmiedebergs Arch Pharmacol. 1994 May;349(5):546-8. doi: 10.1007/BF00169146.
2
Blockade of human atrial 5-HT4 receptors by GR 113808.GR 113808对人心房5-羟色胺4受体的阻断作用。
Br J Pharmacol. 1993 Nov;110(3):1172-4. doi: 10.1111/j.1476-5381.1993.tb13937.x.
3
Comparison of the densities of 5-HT4 receptors, beta 1- and beta 2-adrenoceptors in human atrium: functional implications.人心房中5-HT4受体、β1-和β2-肾上腺素能受体密度的比较:功能意义
Naunyn Schmiedebergs Arch Pharmacol. 1996 Apr;353(5):592-5. doi: 10.1007/BF00169181.
4
5-HT3 and 5-HT4 receptors and cholinergic and tachykininergic neurotransmission in the guinea-pig proximal colon.豚鼠近端结肠中的5-羟色胺3和5-羟色胺4受体以及胆碱能和速激肽能神经传递
Eur J Pharmacol. 1996 Jul 18;308(2):173-80. doi: 10.1016/0014-2999(96)00297-x.
5
Labelling with [125I]-SB 207710 of a small 5-HT4 receptor population in piglet right atrium: functional relevance.用[125I]-SB 207710标记仔猪右心房中的一小部分5-羟色胺4(5-HT4)受体:功能相关性
Br J Pharmacol. 1995 Jul;115(6):933-6. doi: 10.1111/j.1476-5381.1995.tb15900.x.
6
Blockade of human and porcine myocardial 5-HT4 receptors by SB 203186.SB 203186对人和猪心肌5 - HT4受体的阻断作用
Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):28-35. doi: 10.1007/BF00168912.
7
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.
8
A 5-HT4-like receptor in human right atrium.人类右心房中的一种5-羟色胺4样受体。
Naunyn Schmiedebergs Arch Pharmacol. 1991 Aug;344(2):150-9. doi: 10.1007/BF00167212.
9
Sensitization of human atrial 5-HT4 receptors by chronic beta-blocker treatment.
Circulation. 1995 Nov 1;92(9):2526-39. doi: 10.1161/01.cir.92.9.2526.
10
Characterization of the 5-HT4 receptor mediating tachycardia in piglet isolated right atrium.介导仔猪离体右心房心动过速的5-羟色胺4受体的特性
Br J Pharmacol. 1993 Nov;110(3):1023-30. doi: 10.1111/j.1476-5381.1993.tb13916.x.

引用本文的文献

1
Cardiac Roles of Serotonin (5-HT) and 5-HT-Receptors in Health and Disease.血清素(5-HT)和 5-HT 受体在健康和疾病中的心脏作用。
Int J Mol Sci. 2023 Mar 1;24(5):4765. doi: 10.3390/ijms24054765.
2
Radiotracers for the Central Serotoninergic System.中枢5-羟色胺能系统的放射性示踪剂
Pharmaceuticals (Basel). 2022 May 3;15(5):571. doi: 10.3390/ph15050571.
3
Associations of Antidepressants With Atrial Fibrillation and Ventricular Arrhythmias: A Systematic Review and Meta-Analysis.抗抑郁药与心房颤动和室性心律失常的关联:一项系统评价和荟萃分析。

本文引用的文献

1
Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Comparison of the positive inotropic effects of serotonin, histamine, angiotensin II, endothelin and isoprenaline in the isolated human right atrium.5-羟色胺、组胺、血管紧张素II、内皮素和异丙肾上腺素对离体人右心房正性肌力作用的比较。
Naunyn Schmiedebergs Arch Pharmacol. 1993 Apr;347(4):347-52. doi: 10.1007/BF00165383.
3
Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.
Front Cardiovasc Med. 2022 Mar 25;9:840452. doi: 10.3389/fcvm.2022.840452. eCollection 2022.
4
Neurohumoral Control of Sinoatrial Node Activity and Heart Rate: Insight From Experimental Models and Findings From Humans.窦房结活动和心率的神经体液控制:来自实验模型的见解和人类研究结果
Front Physiol. 2020 Mar 3;11:170. doi: 10.3389/fphys.2020.00170. eCollection 2020.
5
Evaluation in monkey of two candidate PET radioligands, [ C]RX-1 and [ F]RX-2, for imaging brain 5-HT receptors.在猴子身上对两种用于脑 5-羟色胺(5-HT)受体成像的正电子发射断层扫描(PET)候选放射性配体[C]RX - 1 和[F]RX - 2 进行评估。
Synapse. 2014 Dec;68(12):613-623. doi: 10.1002/syn.21773. Epub 2014 Aug 11.
6
Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.选择性高亲和力 5-HT(4) 受体拮抗剂的合成与结构亲和力关系:在新型单光子发射计算机断层扫描示踪剂设计中的应用。
J Med Chem. 2012 Nov 26;55(22):9693-707. doi: 10.1021/jm300943r. Epub 2012 Nov 9.
7
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.合成、结构-亲和力关系以及选择性高亲和力 5-HT4 受体配体的放射性标记作为正电子发射断层扫描的潜在成像探针。
J Med Chem. 2010 Oct 14;53(19):7035-47. doi: 10.1021/jm100668r.
8
Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure.猪和人心室心肌中的功能性5-羟色胺5-HT4受体,心力衰竭时5-HT4 mRNA增加。
Naunyn Schmiedebergs Arch Pharmacol. 2004 Sep;370(3):157-66. doi: 10.1007/s00210-004-0963-0. Epub 2004 Sep 7.
9
Radioiodinated SB 207710 as a radioligand in vivo: imaging of brain 5-HT4 receptors with SPET.放射性碘化的SB 207710作为体内放射性配体:用单光子发射断层扫描(SPET)对脑5-羟色胺4(5-HT4)受体进行成像
Eur J Nucl Med Mol Imaging. 2003 Nov;30(11):1520-8. doi: 10.1007/s00259-003-1307-x. Epub 2003 Sep 23.
10
An improved in vitro bioassay for the study of 5-HT(4) receptors in the human isolated large intestinal circular muscle.一种用于研究人离体大肠环形肌中5-羟色胺(4)受体的改良体外生物测定法。
Br J Pharmacol. 2000 Apr;129(8):1601-8. doi: 10.1038/sj.bjp.0703254.
豚鼠和大鼠脑中5-羟色胺4型受体放射性配体结合试验的开发。
Br J Pharmacol. 1993 Jul;109(3):618-24. doi: 10.1111/j.1476-5381.1993.tb13617.x.
4
Blockade of human atrial 5-HT4 receptors by GR 113808.GR 113808对人心房5-羟色胺4受体的阻断作用。
Br J Pharmacol. 1993 Nov;110(3):1172-4. doi: 10.1111/j.1476-5381.1993.tb13937.x.
5
Beta 2-adrenoceptor-mediated positive inotropic effect of adrenaline in human ventricular myocardium. Quantitative discrepancies with binding and adenylate cyclase stimulation.β2肾上腺素能受体介导的肾上腺素对人心室肌的正性肌力作用。与结合及腺苷酸环化酶刺激的定量差异。
Naunyn Schmiedebergs Arch Pharmacol. 1987 Apr;335(4):403-11. doi: 10.1007/BF00165555.
6
CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors.CGP 20712 A:一种定量β1和β2肾上腺素能受体的有用工具。
Eur J Pharmacol. 1986 Oct 14;130(1-2):137-9. doi: 10.1016/0014-2999(86)90193-7.
7
The beta 1-adrenoceptor antagonist CGP 20712 A unmasks beta 2-adrenoceptors activated by (-)-adrenaline in rat sinoatrial node.β1 -肾上腺素能受体拮抗剂CGP 20712 A可揭示由(-)-肾上腺素激活的大鼠窦房结中的β2 -肾上腺素能受体。
Naunyn Schmiedebergs Arch Pharmacol. 1986 Apr;332(4):406-9. doi: 10.1007/BF00500096.
8
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.
9
A 5-hydroxytryptamine receptor in human atrium.人类心房中的一种5-羟色胺受体。
Br J Pharmacol. 1990 Aug;100(4):879-85. doi: 10.1111/j.1476-5381.1990.tb14108.x.
10
A 5-HT4-like receptor in human right atrium.人类右心房中的一种5-羟色胺4样受体。
Naunyn Schmiedebergs Arch Pharmacol. 1991 Aug;344(2):150-9. doi: 10.1007/BF00167212.