• 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

5-羟色胺受体亚型对 25I-NBOMe 致幻活性及其对神经递质传递影响的贡献。

Contribution of serotonin receptor subtypes to hallucinogenic activity of 25I-NBOMe and to its effect on neurotransmission.

机构信息

Department of Pharmacology, Maj Institute of Pharmacology, Polish Academy of Sciences, 12 Smętna, 31-343, Kraków, Poland.

出版信息

Pharmacol Rep. 2020 Dec;72(6):1593-1603. doi: 10.1007/s43440-020-00181-4. Epub 2020 Nov 10.

DOI:10.1007/s43440-020-00181-4
PMID:33174181
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7704505/
Abstract

BACKGROUND

4-Iodo-2,5-dimethoxy-N-(2-methoxybenzyl)phenethylamine (25I-NBOMe) is a potent serotonin (5-HT) receptor agonist with hallucinogenic properties. The aim of our research was to examine the role of the 5-HT, 5-HT and 5-HT serotonin receptor subtypes in 25I-NBOMe hallucinogenic activity and its effect on dopamine (DA), 5-HT and glutamate release in the rat frontal cortex.

METHODS

Hallucinogenic activity was investigated using the wet dog shake (WDS) test. The release of DA, 5-HT and glutamate in the rat frontal cortex was studied using a microdialysis in freely moving rats. Neurotransmitter levels were analyzed by HPLC with electrochemical detection. The selective antagonists of the 5-HT, 5-HT and 5-HT serotonin receptor subtypes: M100907, SB242084 and WAY100635, respectively were applied through a microdialysis probe.

RESULTS

The WDS response to 25I-NBOMe (1 and 3 mg/kg) was significantly reduced by local administration of M100907 and SB242084 (100 nM). The 25I-NBOMe-induced increase in glutamate, DA and 5-HT release was inhibited by M100907 and SB242084. WAY100635 had no effect on 25I-NBOMe-induced WDS and glutamate release, while it decreased DA and 5-HT release from cortical neuronal terminals.

CONCLUSION

The obtained results suggest that 5-HT and 5-HT receptors play a role in 25I-NBOMe-induced hallucinogenic activity and in glutamate, DA and 5-HT release in the rat frontal cortex as their respective antagonists attenuated the effect of this hallucinogen. The disinhibition of GABA cells by the 5-HT receptor antagonist seems to underlie the mechanism of decreased DA and 5-HT release from neuronal terminals in the frontal cortex.

摘要

背景

4-碘-2,5-二甲氧基-N-(2-甲氧基苄基)苯乙胺（25I-NBOMe）是一种具有致幻特性的强效血清素（5-HT）受体激动剂。我们的研究目的是研究 5-HT、5-HT 和 5-HT 血清素受体亚型在 25I-NBOMe 致幻活性中的作用及其对大鼠前额皮质多巴胺（DA）、5-HT 和谷氨酸释放的影响。

方法

使用湿狗抖动（WDS）测试研究致幻活性。使用微透析在自由移动的大鼠中研究大鼠前额皮质中 DA、5-HT 和谷氨酸的释放。通过 HPLC 与电化学检测分析神经递质水平。分别通过微透析探针应用 5-HT、5-HT 和 5-HT 血清素受体亚型的选择性拮抗剂：M100907、SB242084 和 WAY100635。

结果

局部给予 M100907 和 SB242084（100 nM）可显著减少 25I-NBOMe（1 和 3 mg/kg）引起的 WDS 反应。M100907 和 SB242084 抑制 25I-NBOMe 诱导的谷氨酸、DA 和 5-HT 释放增加。WAY100635 对 25I-NBOMe 诱导的 WDS 和谷氨酸释放没有影响，但它降低了皮质神经元末梢的 DA 和 5-HT 释放。

结论

研究结果表明，5-HT 和 5-HT 受体在 25I-NBOMe 诱导的致幻活性以及大鼠前额皮质中谷氨酸、DA 和 5-HT 释放中起作用，因为它们各自的拮抗剂减弱了这种致幻剂的作用。5-HT 受体拮抗剂对 GABA 细胞的抑制作用似乎是前额皮质中神经元末梢 DA 和 5-HT 释放减少的机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/4f06a3b84f66/43440_2020_181_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/e898f26eb30e/43440_2020_181_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/1158c46b41eb/43440_2020_181_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/9bfe3552ea88/43440_2020_181_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/ee180f3a8414/43440_2020_181_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/4f06a3b84f66/43440_2020_181_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/e898f26eb30e/43440_2020_181_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/1158c46b41eb/43440_2020_181_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/9bfe3552ea88/43440_2020_181_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/ee180f3a8414/43440_2020_181_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2759/7704505/4f06a3b84f66/43440_2020_181_Fig4_HTML.jpg

相似文献

1
Contribution of serotonin receptor subtypes to hallucinogenic activity of 25I-NBOMe and to its effect on neurotransmission.5-羟色胺受体亚型对 25I-NBOMe 致幻活性及其对神经递质传递影响的贡献。
Pharmacol Rep. 2020 Dec;72(6):1593-1603. doi: 10.1007/s43440-020-00181-4. Epub 2020 Nov 10.
2
Hallucinogen-Like Action of the Novel Designer Drug 25I-NBOMe and Its Effect on Cortical Neurotransmitters in Rats.新型设计毒品 25I-NBOMe 的致幻样作用及其对大鼠皮质神经递质的影响。
Neurotox Res. 2019 Jul;36(1):91-100. doi: 10.1007/s12640-019-00033-x. Epub 2019 Apr 15.
3
Tolerance to neurochemical and behavioral effects of the hallucinogen 25I-NBOMe.对致幻剂 25I-NBOMe 的神经化学和行为效应的耐受性。
Psychopharmacology (Berl). 2021 Aug;238(8):2349-2364. doi: 10.1007/s00213-021-05860-5. Epub 2021 May 25.
4
Comparative neuropharmacology of N-(2-methoxybenzyl)-2,5-dimethoxyphenethylamine (NBOMe) hallucinogens and their 2C counterparts in male rats.比较 N-(2-甲氧基苄基)-2,5-二甲氧基苯乙胺（NBOMe）致幻剂及其 2C 类似物在雄性大鼠中的神经药理学。
Neuropharmacology. 2018 Nov;142:240-250. doi: 10.1016/j.neuropharm.2018.02.033. Epub 2018 Mar 1.
5
Neurochemical pharmacology of psychoactive substituted N-benzylphenethylamines: High potency agonists at 5-HT receptors.精神活性取代 N-苄基苯乙胺的神经化学药理学：5-羟色胺受体的高活性激动剂。
Biochem Pharmacol. 2018 Dec;158:27-34. doi: 10.1016/j.bcp.2018.09.024. Epub 2018 Sep 25.
6
Neurotoxicological profile of the hallucinogenic compound 25I-NBOMe.致幻化合物 25I-NBOMe 的神经毒性特征。
Sci Rep. 2022 Feb 21;12(1):2939. doi: 10.1038/s41598-022-07069-8.
7
Pharmacology and Toxicology of N-Benzylphenethylamine ("NBOMe") Hallucinogens.N-苄基苯乙胺（“NBOMe”）类致幻剂的药理学与毒理学
Curr Top Behav Neurosci. 2017;32:283-311. doi: 10.1007/7854_2016_64.
8
Effects of the hallucinogen 2,5-dimethoxy-4-iodophenethylamine (2C-I) and superpotent N-benzyl derivatives on the head twitch response.2,5-二甲氧基-4-碘苯乙胺（2C-I）和超强效 N-苄基衍生物对头部震颤反应的影响。
Neuropharmacology. 2014 Feb;77:200-7. doi: 10.1016/j.neuropharm.2013.08.025. Epub 2013 Sep 4.
9
Preclinical characterization of toluene as a non-classical hallucinogen drug in rats: participation of 5-HT, dopamine and glutamate systems.甲苯作为大鼠非经典致幻剂的临床前特征：5-羟色胺、多巴胺和谷氨酸系统的参与
Psychopharmacology (Berl). 2015 Oct;232(20):3797-808. doi: 10.1007/s00213-015-4041-8. Epub 2015 Aug 9.
10
Neurochemical and Behavioral Effects of a New Hallucinogenic Compound 25B-NBOMe in Rats.新型致幻化合物 25B-NBOMe 对大鼠的神经化学和行为影响。
Neurotox Res. 2021 Apr;39(2):305-326. doi: 10.1007/s12640-020-00297-8. Epub 2020 Dec 18.

引用本文的文献

1
Sublethal Concentrations of 2C-I and 25I-NBOMe Designer Drugs Impact Development and Reproductive Behavior.2C-I和25I-NBOMe这类设计药物的亚致死浓度会影响发育和生殖行为。
Int J Mol Sci. 2025 Mar 26;26(7):3039. doi: 10.3390/ijms26073039.
2
Acute Effects of the Psychedelic Phenethylamine 25I-NBOMe in C57BL/6J Male Mice.致幻苯乙胺25I-NBOMe对C57BL/6J雄性小鼠的急性影响。
Int J Mol Sci. 2025 Mar 20;26(6):2815. doi: 10.3390/ijms26062815.
3
Toxicodynamic insights of 2C and NBOMe drugs - Is there abuse potential?2C类和N-苄基苯乙胺类药物的毒代动力学见解——是否存在滥用可能性？

本文引用的文献

1
Hallucinogen-Like Action of the Novel Designer Drug 25I-NBOMe and Its Effect on Cortical Neurotransmitters in Rats.新型设计毒品 25I-NBOMe 的致幻样作用及其对大鼠皮质神经递质的影响。
Neurotox Res. 2019 Jul;36(1):91-100. doi: 10.1007/s12640-019-00033-x. Epub 2019 Apr 15.
2
Comparative neuropharmacology of N-(2-methoxybenzyl)-2,5-dimethoxyphenethylamine (NBOMe) hallucinogens and their 2C counterparts in male rats.比较 N-(2-甲氧基苄基)-2,5-二甲氧基苯乙胺（NBOMe）致幻剂及其 2C 类似物在雄性大鼠中的神经药理学。
Neuropharmacology. 2018 Nov;142:240-250. doi: 10.1016/j.neuropharm.2018.02.033. Epub 2018 Mar 1.
3
Toxicol Rep. 2025 Jan 3;14:101890. doi: 10.1016/j.toxrep.2025.101890. eCollection 2025 Jun.
4
Effect of Compounds on Sensorimotor, Motor, and Prepulse Inhibition Responses in Mice in Comparison With the Analogs and Lysergic Acid Diethylamide: From Preclinical Evidence to Forensic Implication in Driving Under the Influence of Drugs.与类似物和麦角酸二乙酰胺相比，化合物对小鼠感觉运动、运动和前脉冲抑制反应的影响：从临床前证据到药物影响下驾驶的法医学意义
Front Psychiatry. 2022 Apr 21;13:875722. doi: 10.3389/fpsyt.2022.875722. eCollection 2022.
5
Neurotoxicological profile of the hallucinogenic compound 25I-NBOMe.致幻化合物 25I-NBOMe 的神经毒性特征。
Sci Rep. 2022 Feb 21;12(1):2939. doi: 10.1038/s41598-022-07069-8.
6
Tolerance to neurochemical and behavioral effects of the hallucinogen 25I-NBOMe.对致幻剂 25I-NBOMe 的神经化学和行为效应的耐受性。
Psychopharmacology (Berl). 2021 Aug;238(8):2349-2364. doi: 10.1007/s00213-021-05860-5. Epub 2021 May 25.
Receptor binding profiles and behavioral pharmacology of ring-substituted N,N-diallyltryptamine analogs.
环状取代的 N,N-二烯丙基色胺类似物的受体结合谱和行为药理学。
Neuropharmacology. 2018 Nov;142:231-239. doi: 10.1016/j.neuropharm.2018.02.028. Epub 2018 Feb 27.
4
Tolerance and Tachyphylaxis to Head Twitches Induced by the 5-HT2A Agonist 25CN-NBOH in Mice.小鼠对5-HT2A激动剂25CN-NBOH诱导的头部抽搐的耐受性和快速耐受性
Front Pharmacol. 2018 Feb 6;9:17. doi: 10.3389/fphar.2018.00017. eCollection 2018.
5
Neurotoxic Effects of 5-MeO-DIPT: A Psychoactive Tryptamine Derivative in Rats.5-甲氧基-N,N-二异丙基色胺的神经毒性作用：一种大鼠体内的精神活性色胺衍生物
Neurotox Res. 2016 Nov;30(4):606-619. doi: 10.1007/s12640-016-9654-0. Epub 2016 Jul 26.
6
Expression of Serotonin2C Receptors in Pyramidal and GABAergic Neurons of Rat Prefrontal Cortex: A Comparison with Striatum.大鼠前额叶皮层锥体神经元和γ-氨基丁酸能神经元中5-羟色胺2C受体的表达：与纹状体的比较。
Cereb Cortex. 2017 Jun 1;27(6):3125-3139. doi: 10.1093/cercor/bhw148.
7
Receptor interaction profiles of novel N-2-methoxybenzyl (NBOMe) derivatives of 2,5-dimethoxy-substituted phenethylamines (2C drugs).2,5-二甲氧基取代苯乙胺（2C类药物）新型N-2-甲氧基苄基（NBOMe）衍生物的受体相互作用谱
Neuropharmacology. 2015 Dec;99:546-53. doi: 10.1016/j.neuropharm.2015.08.034. Epub 2015 Aug 25.
8
Serotonin-2C and -2a receptor co-expression on cells in the rat medial prefrontal cortex.5-羟色胺-2C和-2A受体在大鼠内侧前额叶皮质细胞上的共表达。
Neuroscience. 2015 Jun 25;297:22-37. doi: 10.1016/j.neuroscience.2015.03.050. Epub 2015 Mar 27.
9
5-HT(1A) [corrected] receptors in mood and anxiety: recent insights into autoreceptor versus heteroreceptor function.5-HT(1A) [校正] 受体在情绪和焦虑中的作用：对自身受体与异源受体功能的最新认识。
Psychopharmacology (Berl). 2014 Feb;231(4):623-36. doi: 10.1007/s00213-013-3389-x. Epub 2013 Dec 12.
10
Effects of the hallucinogen 2,5-dimethoxy-4-iodophenethylamine (2C-I) and superpotent N-benzyl derivatives on the head twitch response.2,5-二甲氧基-4-碘苯乙胺（2C-I）和超强效 N-苄基衍生物对头部震颤反应的影响。
Neuropharmacology. 2014 Feb;77:200-7. doi: 10.1016/j.neuropharm.2013.08.025. Epub 2013 Sep 4.