• 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

中枢神经系统药物的构效关系研究。第24部分：N-叔丁基-3-[4-(2-甲氧基苯基)-1-哌嗪基]-2-苯基丙酰胺（WAY-100135）的新类似物

Structure-activity relationship studies of CNS agents. Part 24: New analogs of N-tert.-butyl-3-[4-(2-methoxyphenyl)-1-piperazinyl]-2-phenylpropanamide (WAY-100135).

作者信息

Boksa J, Klodzińska A, Charakchieva-Minol S, Chojnacka-Wójcik E, Mokrosz J L

机构信息

Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków.

出版信息

Pharmazie. 1996 Feb;51(2):72-6.

PMID:8720802
Abstract

A series of new N-substituted derivatives of 3-[4-(2-methoxyphenyl)-1-piperazinyl]-2-phenylpropanamide, 6-10, were synthesized and their 5-HT1A, 5-HT2A, and alpha 1 receptor affinities were determined. All the compounds were highly potent 5-HT1A ligands with a moderate or low 5-HT2A and alpha 1 affinity. It was shown that the 5-HT2A affinity of 1 and 6-10 depended crucially on the volume of amide substituents. None of the investigated racemic mixtures 1 and 6-8 antagonized the 8-OH-DPAT-induced lower lip retraction in rats, whereas (+/-)-7 behaved like a weak agonist of 5-HT1A receptors in the model used.

摘要

合成了一系列新的3-[4-(2-甲氧基苯基)-1-哌嗪基]-2-苯基丙酰胺的N-取代衍生物6 - 10，并测定了它们对5-HT1A、5-HT2A和α1受体的亲和力。所有化合物都是高效的5-HT1A配体，对5-HT2A和α1的亲和力中等或较低。结果表明，1和6 - 10对5-HT2A的亲和力关键取决于酰胺取代基的体积。所研究的外消旋混合物1和6 - 8均未拮抗8-OH-DPAT诱导的大鼠下唇回缩，而(±)-7在所用模型中表现为5-HT1A受体的弱激动剂。

相似文献

1
Structure-activity relationship studies of CNS agents. Part 24: New analogs of N-tert.-butyl-3-[4-(2-methoxyphenyl)-1-piperazinyl]-2-phenylpropanamide (WAY-100135).中枢神经系统药物的构效关系研究。第24部分：N-叔丁基-3-[4-(2-甲氧基苯基)-1-哌嗪基]-2-苯基丙酰胺（WAY-100135）的新类似物
Pharmazie. 1996 Feb;51(2):72-6.
2
Synthesis, 5-HT1A and 5-HT2A receptor activity of new 1-phenylpiperazinylpropyl derivatives with arylalkyl substituents in position 7 of purine-2,6-dione.嘌呤-2,6-二酮7位带有芳基烷基取代基的新型1-苯基哌嗪基丙基衍生物的合成、5-HT1A和5-HT2A受体活性
Pol J Pharmacol. 2001 Jul-Aug;53(4):359-68.
3
1,4-Benzoxazin-3(4H)-one derivatives and related compounds as 5-HT1A and 5-HT2A receptor ligands; the effect of the terminal amide fragment on the 5-HT1A/5-HT2A affinity and functional activity.1,4-苯并恶嗪-3(4H)-酮衍生物及相关化合物作为5-HT1A和5-HT2A受体配体；末端酰胺片段对5-HT1A/5-HT2A亲和力和功能活性的影响。
Pol J Pharmacol. 1998 Jul-Oct;50(4-5):333-40.
4
9-substituted 1,2,3,4-tetrahydro-beta-carbolin-1-ones, new 5-HT1A and 5-HT2A receptor ligands.9-取代的1,2,3,4-四氢-β-咔啉-1-酮，新型5-HT1A和5-HT2A受体配体。
Pol J Pharmacol. 1999 Jul-Aug;51(4):351-6.
5
2-H- and 2-acyl-9- [omega-[4-(2-methoxyphenyl)piperazinyl]-alkyl]-1,2,3,4-tetrahydro-beta-carbolines as ligands of 5-HT1A and 5-HT2A receptors.2-H-和2-酰基-9-[ω-[4-(2-甲氧基苯基)哌嗪基]-烷基]-1,2,3,4-四氢-β-咔啉作为5-HT1A和5-HT2A受体的配体。
Pol J Pharmacol. 2001 Sep-Oct;53(5):501-8.
6
MP-3022, a new putative antagonist at pre- and postsynaptic 5-HT1A receptors.MP - 3022，一种新型的突触前和突触后5 - HT1A受体潜在拮抗剂。
Pol J Pharmacol. 1996 Jan-Feb;48(1):13-22.
7
Influence of the aliphatic spacer length on the 5-HT1A receptor activity of new arylpiperazines with an indazole system.脂肪族间隔长度对具有吲唑系统的新型芳基哌嗪5-HT1A受体活性的影响。
Pol J Pharmacol. 2000 May-Jun;52(3):209-16.
8
Some pharmacological properties of new analogs of MP 3022, the 5-HT1A receptor antagonist.5-羟色胺1A受体拮抗剂MP 3022新类似物的一些药理学特性。
Pol J Pharmacol. 1999 Sep-Oct;51(5):405-13.
9
In vitro profile of the antidepressant candidate OPC-14523 at rat and human 5-HT1A receptors.抗抑郁候选药物OPC-14523对大鼠和人类5-羟色胺1A受体的体外研究概况
Eur J Pharmacol. 2005 Jul 11;517(3):165-73. doi: 10.1016/j.ejphar.2005.05.035.
10
Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist.氨甲基色满衍生物BAY x 3702作为高效5-羟色胺1A受体激动剂的特性研究。
J Pharmacol Exp Ther. 1998 Mar;284(3):1082-94.