• 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

In vivo displacement by 3-PPP enantiomers of N,N-dipropyl-5,6-ADTN from dopamine receptor-binding sites in rat striatum.

作者信息

Carlsson A, Löfberg L

出版信息

J Neural Transm. 1985;64(3-4):173-85. doi: 10.1007/BF01256465.

DOI:10.1007/BF01256465
PMID:4086990
Abstract

The enantiomers of 3-PPP or haloperidol were injected in various doses to rats 1 hour after the established dopamine receptor ligand N,N-dipropyl-5,6-ADTN. After another 40 minutes the binding of the ligand to the striatum was measured by high performance liquid chromatography, using the level in the cerebellum as "blank". (-)-3-PPP was found to cause a maximum 71% displacement of the ligand from the striatal binding sites. Haloperidol proved to be more potent but not significantly more efficacious in displacing the ligand. However, the combined treatment with (-)-3-PPP and haloperidol caused a stronger displacement of the ligand than (-)-3-PPP alone, suggesting that the binding-site populations available for the two agents are not fully identical. (+)-3-PPP also caused displacement of the ligand but was considerably less potent than its enantiomeric twin. The results are discussed against the background of the different pharmacological profiles of the 3-PPP enantiomers and haloperidol. It is suggested that an inverse relationship may exist between receptor affinity and intrinsic activity and that such a relationship may be inherent in the mechanism underlying receptor stimulation.

摘要

相似文献

1
In vivo displacement by 3-PPP enantiomers of N,N-dipropyl-5,6-ADTN from dopamine receptor-binding sites in rat striatum.
J Neural Transm. 1985;64(3-4):173-85. doi: 10.1007/BF01256465.
2
S(-)DP-5,6-ADTN as an in vivo dopamine receptor ligand: relation between displacement by dopamine agonists and their pharmacological effects.
Naunyn Schmiedebergs Arch Pharmacol. 1986 Apr;332(4):338-45. doi: 10.1007/BF00500084.
3
In vivo dopamine receptor binding studies with a non-radioactively labeled agonist, dipropyl-5,6-ADTN.使用非放射性标记激动剂二丙基-5,6-ADTN进行的体内多巴胺受体结合研究。
Life Sci. 1983 Mar 21;32(12):1313-23. doi: 10.1016/0024-3205(83)90805-6.
4
Striatal binding of 2-amino-6,7-[3H]dihydroxy-1,2,3,4-tetrahydronaphthalene to two dopaminergic sites distinguished by their low and high affinity for neuroleptics.2-氨基-6,7-[3H]二羟基-1,2,3,4-四氢萘在纹状体与两个多巴胺能位点的结合，这两个位点对神经阻滞剂具有低亲和力和高亲和力。
J Neurosci. 1982 Jul;2(7):895-906. doi: 10.1523/JNEUROSCI.02-07-00895.1982.
5
Similar binding of 3H-ADTN and 3H-apomorphine to calf brain dopamine receptors.3H-ADTN和3H-阿扑吗啡与小牛脑多巴胺受体的相似结合。
Eur J Pharmacol. 1979 Apr 15;55(2):137-42. doi: 10.1016/0014-2999(79)90385-6.
6
Kinetic and pharmacological profiles of the in vitro binding of the potent dopamine agonist [3H]N,N-dipropyl-5,6-dihydroxy-2-aminotetralin to rat striatal membranes.
Eur J Pharmacol. 1985 May 28;112(1):73-9. doi: 10.1016/0014-2999(85)90240-7.
7
Identification of dopamine "D3" and "D4" binding sites, labelled with [3H]2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene, as high agonist affinity states of the D1 and D2 dopamine receptors, respectively.分别鉴定用[³H]2-氨基-6,7-二羟基-1,2,3,4-四氢萘标记的多巴胺“D3”和“D4”结合位点，作为D1和D2多巴胺受体的高激动剂亲和力状态。
J Neurochem. 1986 Apr;46(4):1058-67. doi: 10.1111/j.1471-4159.1986.tb00618.x.
8
Binding of [3H]ADTN to rat striatal membranes.
Biochem Pharmacol. 1982 Apr 15;31(8):1629-32. doi: 10.1016/0006-2952(82)90391-4.
9
Relative selectivity of 6,7-dihydroxy-2-dimethylaminotetralin, N-n-propyl-3-(3-hydroxyphenyl)piperidine, N-n-propylnorapomorphine and pergolide as agonists at striatal dopamine autoreceptors and postsynaptic dopamine receptors.6,7-二羟基-2-二甲基氨基四氢萘、N-正丙基-3-(3-羟基苯基)哌啶、N-正丙基去甲阿扑吗啡和培高利特作为纹状体多巴胺自身受体和突触后多巴胺受体激动剂的相对选择性。
J Pharmacol Exp Ther. 1985 Feb;232(2):519-25.
10
Evidence for loss of brain [3H]spiroperidil and [3H]ADTN binding sites in rabbit brain with aging.家兔脑内[³H]螺哌啶醇和[³H]ADTN结合位点随衰老而丧失的证据。
Brain Res. 1980 Jun 16;192(1):185-94. doi: 10.1016/0006-8993(80)91018-5.

引用本文的文献

1
Differential effects of dopamine D2 and D3 receptor antagonists in regard to dopamine release, in vivo receptor displacement and behaviour.多巴胺D2和D3受体拮抗剂在多巴胺释放、体内受体置换及行为方面的差异效应。
J Neural Transm Gen Sect. 1994;98(1):39-55. doi: 10.1007/BF01277593.
2
A homologous series of N-alkylated cis-(+)-(1 S, 2 R)-5-methoxy-1-methyl-2-aminotetralins: central dopamine receptor antagonists showing profiles ranging from classical antagonism to selectivity for autoreceptors.一系列N-烷基化的顺式-(+)-(1S,2R)-5-甲氧基-1-甲基-2-氨基四氢萘：中枢多巴胺受体拮抗剂，其作用谱从经典拮抗作用到对自身受体的选择性。
J Neural Transm. 1986;65(1):29-38. doi: 10.1007/BF01249609.
3

本文引用的文献

1
In vivo dopamine receptor agonist binding in rat brain: relation with pharmacological effects.
Eur J Pharmacol. 1983 Jun 17;90(4):433-6. doi: 10.1016/0014-2999(83)90567-8.
2
In vivo dopamine receptor binding studies with a non-radioactively labeled agonist, dipropyl-5,6-ADTN.使用非放射性标记激动剂二丙基-5,6-ADTN进行的体内多巴胺受体结合研究。
Life Sci. 1983 Mar 21;32(12):1313-23. doi: 10.1016/0024-3205(83)90805-6.
3
Dopamine receptor-mediated hypothermia induced in rats by (+)-, but not by (-)-3-PPP.（+）-3-PPP可诱导大鼠多巴胺受体介导的体温过低，而（-）-3-PPP则不能。
Dopamine-receptor agonists: mechanisms underlying autoreceptor selectivity. I. Review of the evidence.
多巴胺受体激动剂：自身受体选择性的潜在机制。I. 证据综述
J Neural Transm. 1985;62(1-2):1-52. doi: 10.1007/BF01260414.
4
S(-)DP-5,6-ADTN as an in vivo dopamine receptor ligand: relation between displacement by dopamine agonists and their pharmacological effects.
Naunyn Schmiedebergs Arch Pharmacol. 1986 Apr;332(4):338-45. doi: 10.1007/BF00500084.
5
In vivo dopamine (DA) receptor binding and behavioural effects of the putative DA autoreceptor antagonists (+)-AJ 76 and (+)-UH 232 in rats with a unilateral nigral 6-OH-DA lesion.在单侧黑质6-羟基多巴胺损伤大鼠中，推定的多巴胺自身受体拮抗剂（+）-AJ 76和（+）-UH 232的体内多巴胺（DA）受体结合及行为效应。
Exp Brain Res. 1988;70(3):577-84. doi: 10.1007/BF00247605.
6
In vivo receptor binding, neurochemical and functional studies with the dopamine D-1 receptor antagonist SCH23390.使用多巴胺D-1受体拮抗剂SCH23390进行的体内受体结合、神经化学和功能研究。
J Neural Transm. 1988;72(2):83-97. doi: 10.1007/BF01250232.
7
(+)-AJ 76 and (+)-UH 232: central stimulants acting as preferential dopamine autoreceptor antagonists.（+）-AJ 76和（+）-UH 232：作为优先多巴胺自身受体拮抗剂的中枢兴奋剂。
Naunyn Schmiedebergs Arch Pharmacol. 1986 Nov;334(3):234-45. doi: 10.1007/BF00508777.
Eur J Pharmacol. 1985 Jan 8;107(3):299-304. doi: 10.1016/0014-2999(85)90254-7.
4
Dopamine-receptor agonists: mechanisms underlying autoreceptor selectivity. I. Review of the evidence.多巴胺受体激动剂：自身受体选择性的潜在机制。I. 证据综述
J Neural Transm. 1985;62(1-2):1-52. doi: 10.1007/BF01260414.
5
Dopamine receptor agonists: mechanisms underlying autoreceptor selectivity. II. Theoretical considerations.
J Neural Transm. 1985;62(3-4):171-207. doi: 10.1007/BF01252236.
6
In-vitro and in-vivo metabolism of the presynaptic dopamine agonist 3-PPP to a catecholic analogue in rats.大鼠体内突触前多巴胺激动剂3-PPP向儿茶酚类似物的体外和体内代谢
J Pharm Pharmacol. 1985 May;37(5):314-9. doi: 10.1111/j.2042-7158.1985.tb05073.x.