• 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

一种用于筛选组胺H3配体的简单快速体外测试系统。

A simple and rapid in vitro test system for the screening of histamine H3 ligands.

作者信息

Vollinga R C, Zuiderveld O P, Scheerens H, Bast A, Timmerman H

机构信息

Department of Pharmacochemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The Netherlands.

出版信息

Methods Find Exp Clin Pharmacol. 1992 Dec;14(10):747-51.

PMID:1338472
Abstract

A simple and rapid functional test system for the screening of histamine H3 ligands is described. It is based on the inhibitory effect of histamine H3 agonists on electrically-evoked contractile response of isolated guinea pig intestine. Whole jejunum segments are continuously stimulated maximally (15 V) by electrical pulses with a frequency of 0.1 Hz and a duration of 0.5 msec. The resulting twitches are recorded isotonically (1.0 g) and can be completely abolished by atropine (0.1 mcM).

摘要

本文描述了一种用于筛选组胺H3配体的简单快速的功能测试系统。该系统基于组胺H3激动剂对离体豚鼠肠电诱发收缩反应的抑制作用。空肠全段以0.1 Hz的频率和0.5毫秒的持续时间通过电脉冲进行最大程度的连续刺激(15 V)。由此产生的抽搐以等张方式(1.0 g)记录,并且可被阿托品(0.1 μM)完全消除。

相似文献

1
A simple and rapid in vitro test system for the screening of histamine H3 ligands.一种用于筛选组胺H3配体的简单快速体外测试系统。
Methods Find Exp Clin Pharmacol. 1992 Dec;14(10):747-51.
2
Inhibition of electrically evoked contractions of guinea-pig ileum preparations mediated by the histamine H3 receptor.对由组胺H3受体介导的豚鼠回肠制剂电诱发收缩的抑制作用。
Eur J Pharmacol. 1990 Sep 21;186(2-3):343-7. doi: 10.1016/0014-2999(90)90458-i.
3
Histamine H3 receptors in the guinea pig small intestine.豚鼠小肠中的组胺H3受体。
Pharmacol Res. 1992 Feb-Mar;25 Suppl 1:57-8. doi: 10.1016/1043-6618(92)90538-m.
4
High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models.新型组胺H3受体拮抗剂GT-2227和GT-2331在两种功能模型中具有高拮抗剂效力。
Eur J Pharmacol. 1998 Jun 26;351(3):307-11. doi: 10.1016/s0014-2999(98)00396-3.
5
Characterization of histamine H3-receptors in guinea-pig ileum with H3-selective ligands.用H3选择性配体对豚鼠回肠中组胺H3受体的表征
Br J Pharmacol. 1990 Nov;101(3):621-4. doi: 10.1111/j.1476-5381.1990.tb14130.x.
6
Inhibition of sympathetic neurotransmission via NEM-sensitive H3-receptors in the guinea pig vas deferens.通过豚鼠输精管中对N-乙基马来酰亚胺(NEM)敏感的H3受体抑制交感神经传递
Methods Find Exp Clin Pharmacol. 1994 Apr;16(3):185-9.
7
Characterization and function of histamine receptors in corpus cavernosum.阴茎海绵体中组胺受体的表征与功能
J Urol. 1995 Feb;153(2):506-10. doi: 10.1097/00005392-199502000-00072.
8
Presynaptic histamine H1- and H3-receptors modulate sympathetic neurotransmission in isolated guinea pig vas deferens.突触前组胺H1和H3受体调节离体豚鼠输精管中的交感神经传递。
Zhongguo Yao Li Xue Bao. 1994 Jan;15(1):60-4.
9
Is there a role for histamine H3-receptors in the control of intestinal peristalsis?
Inflamm Res. 1997 Mar;46 Suppl 1:S99-100.
10
Histamine H3 receptors in the guinea pig ileum: evidence for a postjunctional location.
J Physiol Paris. 2000 Jan-Feb;94(1):1-4. doi: 10.1016/s0928-4257(99)00110-2.

引用本文的文献

1
4-Oxypiperidine Ethers as Multiple Targeting Ligands at Histamine H Receptors and Cholinesterases.4-氧代哌啶类作为组胺 H 受体和胆碱酯酶的多靶点配体。
ACS Chem Neurosci. 2024 Mar 20;15(6):1206-1218. doi: 10.1021/acschemneuro.3c00800. Epub 2024 Mar 5.
2
Guanidines: Synthesis of Novel Histamine HR Antagonists with Additional Breast Anticancer Activity and Cholinesterases Inhibitory Effect.胍类化合物:具有额外乳腺癌抗癌活性和胆碱酯酶抑制作用的新型组胺HR拮抗剂的合成
Pharmaceuticals (Basel). 2023 Apr 30;16(5):675. doi: 10.3390/ph16050675.
3
Guanidine Derivatives: How Simple Structural Modification of Histamine HR Antagonists Has Led to the Discovery of Potent Muscarinic MR/MR Antagonists.
胍衍生物:组胺 HR 拮抗剂的简单结构修饰如何导致发现强效毒蕈碱 MR/MR 拮抗剂。
ACS Chem Neurosci. 2021 Jul 7;12(13):2503-2519. doi: 10.1021/acschemneuro.1c00237. Epub 2021 Jun 8.
4
Design, synthesis, and and characterization of 1-{4-[4-(substituted)piperazin-1-yl]butyl}guanidines and their piperidine analogues as histamine H receptor antagonists.1-{4-[4-(取代)哌嗪-1-基]丁基}胍及其哌啶类似物作为组胺H受体拮抗剂的设计、合成与表征
Medchemcomm. 2019 Jan 11;10(2):234-251. doi: 10.1039/c8md00527c. eCollection 2019 Feb 1.
5
4-Hydroxypiperidines and Their Flexible 3-(Amino)propyloxy Analogues as Non-Imidazole Histamine H₃ Receptor Antagonist: Further Structure⁻Activity Relationship Exploration and In Vitro and In Vivo Pharmacological Evaluation.4-羟基哌啶及其柔性 3-(氨基)丙氧基类似物作为非咪唑组胺 H₃受体拮抗剂:进一步的结构-活性关系探索及体外和体内药理学评价。
Int J Mol Sci. 2018 Apr 19;19(4):1243. doi: 10.3390/ijms19041243.
6
Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines.非咪唑类组氨酸 H₃ 配体。第 VII 部分。5-取代-2-噻唑-4-正丙基哌嗪的合成、体外和体内特性。
Molecules. 2018 Feb 3;23(2):326. doi: 10.3390/molecules23020326.
7
Non-imidazole histamine H ligands: part V. synthesis and preliminary pharmacological investigation of 1-[2-thiazol-4-yl- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4--propylpiperazine derivatives.非咪唑类组胺H配体:第五部分。1-[2-噻唑-4-基]-和1-[2-噻唑-5-基-(2-氨基乙基)]-4-丙基哌嗪衍生物的合成及初步药理学研究
Med Chem Res. 2013 Aug;22(8):3640-3652. doi: 10.1007/s00044-012-0372-8. Epub 2012 Nov 29.
8
SLATE: a method for the superposition of flexible ligands.SLATE:一种柔性配体叠加方法。
J Comput Aided Mol Des. 2001 Jan;15(1):81-96. doi: 10.1023/a:1011102129244.
9
Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea-pig ileum: evidence for H3 receptor heterogeneity?与碘普罗芬化学相关的拮抗剂在小鼠大脑皮层和豚鼠回肠组胺H3受体上的效能:H3受体异质性的证据?
Naunyn Schmiedebergs Arch Pharmacol. 1996 Apr;353(5):482-8. doi: 10.1007/BF00169166.
10
Evaluation of the receptor selectivity of the H3 receptor antagonists, iodophenpropit and thioperamide: an interaction with the 5-HT3 receptor revealed.H3受体拮抗剂碘苯丙胺和硫代哌酰胺的受体选择性评估:揭示了与5-HT3受体的相互作用。
Br J Pharmacol. 1995 Oct;116(4):2315-21. doi: 10.1111/j.1476-5381.1995.tb15071.x.