• 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

（+）-顺式-8-羟基-1-甲基-2-（二正丙基氨基）四氢萘：一种强效且高度立体选择性的5-羟色胺受体激动剂。

(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist.

作者信息

Arvidsson L E, Johansson A M, Hacksell U, Nilsson J L, Svensson K, Hjorth S, Magnusson T, Carlsson A, Andersson B, Wikström H

机构信息

Department of Organic Pharmaceutical Chemistry, University of Uppsala,Sweden.

出版信息

J Med Chem. 1987 Nov;30(11):2105-9. doi: 10.1021/jm00394a029.

DOI:10.1021/jm00394a029
PMID:2959776
Abstract

C1-Methylated derivatives of the potent 5-hydroxytryptamine (5-HT) receptor agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT, 1) were synthesized and tested for central 5-HT and dopamine receptor activity by use of a biochemical test method in rats. cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin (8) was found to be a 5-HT receptor agonist. The (+)-enantiomer of 8 had a potency equal to that of 1, whereas (-)-8 and the trans isomer (+/-)-9 were inactive.

摘要

合成了强效5-羟色胺（5-HT）受体激动剂8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT，1）的C1-甲基化衍生物，并通过生化测试方法在大鼠中测试其对中枢5-HT和多巴胺受体的活性。发现顺式-8-羟基-1-甲基-2-（二正丙基氨基）四氢萘（8）是一种5-HT受体激动剂。8的（+）-对映体的效力与1相当，而（-）-8和反式异构体（+/-）-9无活性。

相似文献

1
(+)-cis-8-Hydroxy-1-methyl-2-(di-n-propylamino)tetralin: a potent and highly stereoselective 5-hydroxytryptamine receptor agonist.（+）-顺式-8-羟基-1-甲基-2-（二正丙基氨基）四氢萘：一种强效且高度立体选择性的5-羟色胺受体激动剂。
J Med Chem. 1987 Nov;30(11):2105-9. doi: 10.1021/jm00394a029.
2
Central dopaminergic and 5-hydroxytryptaminergic effects of C3-methylated derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin.8-羟基-2-（二正丙基氨基）四氢萘的C3-甲基化衍生物的中枢多巴胺能和5-羟色胺能效应
J Med Chem. 1988 Jun;31(6):1130-40. doi: 10.1021/jm00401a012.
3
Structural factors of importance for 5-hydroxytryptaminergic activity. Conformational preferences and electrostatic potentials of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and some related agents.对5-羟色胺能活性重要的结构因素。8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT）及一些相关药物的构象偏好和静电势。
J Med Chem. 1988 Jan;31(1):212-21. doi: 10.1021/jm00396a034.
4
Resolved N,N-dialkylated 2-amino-8-hydroxytetralins: stereoselective interactions with 5-HT1A receptors in the brain.拆分的N,N-二烷基化2-氨基-8-羟基四氢萘：与大脑中5-HT1A受体的立体选择性相互作用
J Med Chem. 1989 Apr;32(4):779-83. doi: 10.1021/jm00124a009.
5
A C2-methylated derivative of the 5-hydroxy-tryptamine-receptor agonist 8-hydroxy-2-(dipropylamino)tetralin (8-OH DPAT).5-羟色胺受体激动剂8-羟基-2-（二丙基氨基）四氢萘（8-OH DPAT）的一种C2-甲基化衍生物。
Acta Pharm Suec. 1987;24(4):153-60.
6
C1-Methylated 5-hydroxy-2-(dipropylamino)tetralins: central dopamine-receptor stimulating activity.1-甲基化5-羟基-2-（二丙基氨基）四氢萘：中枢多巴胺受体刺激活性
J Med Chem. 1984 Aug;27(8):1003-7. doi: 10.1021/jm00374a012.
7
8-Hydroxy-2-(alkylamino)tetralins and related compounds as central 5-hydroxytryptamine receptor agonists.8-羟基-2-（烷基氨基）四氢萘及其相关化合物作为中枢5-羟色胺受体激动剂。
J Med Chem. 1984 Jan;27(1):45-51. doi: 10.1021/jm00367a009.
8
Partial postsynaptic 5-HT1A agonist properties of the novel stereoselective 8-OH-DPAT analogue (+)cis-8-hydroxy-1-methyl-2-(di-n-propylamino)tetralin, (+)ALK-3.新型立体选择性8-OH-DPAT类似物（+）顺式-8-羟基-1-甲基-2-（二正丙基氨基）四氢化萘（+）ALK-3的部分突触后5-HT1A激动剂特性
Eur J Pharmacol. 1989 Nov 7;170(3):269-74. doi: 10.1016/0014-2999(89)90549-9.
9
Effects of the C3-methylated derivatives of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) on central 5-hydroxytryptamine receptors.8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT）的C3-甲基化衍生物对中枢5-羟色胺受体的影响。
Eur J Pharmacol. 1987 Nov 3;143(1):55-63. doi: 10.1016/0014-2999(87)90734-5.
10
C3-methylated 5-hydroxy-2-(dipropylamino)tetralins: conformational and steric parameters of importance for central dopamine receptor activation.C3-甲基化的5-羟基-2-（二丙基氨基）四氢萘：对中枢多巴胺受体激活具有重要意义的构象和空间参数。
J Med Chem. 1987 Jul;30(7):1135-44. doi: 10.1021/jm00390a004.

引用本文的文献

1
Clozapine increases cutaneous blood flow and reduces sympathetic cutaneous vasomotor alerting responses (SCVARs) in rats: comparison with effects of haloperidol.氯氮平可增加大鼠皮肤血流量并降低交感神经皮肤血管运动警觉反应（SCVARs）：与氟哌啶醇的作用比较。
Psychopharmacology (Berl). 2005 Sep;181(3):518-28. doi: 10.1007/s00213-005-0012-9. Epub 2005 Oct 12.
2
5-Hydroxytryptamine 1A receptors inhibit cold-induced sympathetically mediated cutaneous vasoconstriction in rabbits.5-羟色胺1A受体抑制兔冷诱导的交感神经介导的皮肤血管收缩。
J Physiol. 2003 Oct 1;552(Pt 1):303-14. doi: 10.1113/jphysiol.2003.048041. Epub 2003 Aug 8.
3
cis-(+)-8-OH-1-CH3-DPAT, (+)ALK-3, a novel stereoselective pharmacological probe for characterizing 5-HT release-controlling 5-HT1A autoreceptors. An in vivo brain microdialysis study.
顺式-(+)-8-羟基-1-甲基-DPAT，(+)ALK-3，一种用于表征5-羟色胺释放控制5-羟色胺1A自身受体的新型立体选择性药理学探针。一项体内脑微透析研究。
Naunyn Schmiedebergs Arch Pharmacol. 1990 Mar;341(3):149-57. doi: 10.1007/BF00169724.