• 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

HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia.

作者信息

Kozikowski Alan P, Cho Sung Jin, Jensen Niels H, Allen John A, Svennebring Andreas M, Roth Bryan L

机构信息

Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 60612-7230, USA.

出版信息

ChemMedChem. 2010 Aug 2;5(8):1221-5. doi: 10.1002/cmdc.201000186.

DOI:10.1002/cmdc.201000186
PMID:20533502
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2951742/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/ce2792f7b4ce/nihms-241143-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/616b274840cc/nihms-241143-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/e114edd93f91/nihms-241143-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/618771f5b583/nihms-241143-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/ba90cd5dc41d/nihms-241143-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/db15dd8be38b/nihms-241143-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/ce2792f7b4ce/nihms-241143-f0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/616b274840cc/nihms-241143-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/e114edd93f91/nihms-241143-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/618771f5b583/nihms-241143-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/ba90cd5dc41d/nihms-241143-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/db15dd8be38b/nihms-241143-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2ad6/2951742/ce2792f7b4ce/nihms-241143-f0006.jpg

相似文献

1
HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia.高通量筛选和合理药物设计以生成一类可能用于精神分裂症治疗的5-羟色胺(2C)选择性配体。
ChemMedChem. 2010 Aug 2;5(8):1221-5. doi: 10.1002/cmdc.201000186.
2
Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.发现N-取代的(2-苯基环丙基)甲胺作为功能选择性5-羟色胺2C受体激动剂,有潜力用作抗精神病药物。
J Med Chem. 2017 Jul 27;60(14):6273-6288. doi: 10.1021/acs.jmedchem.7b00584. Epub 2017 Jul 18.
3
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT) receptor agonist without 5-HT agonism.设计含氟环丙基取代的 2-苯环丙基甲胺衍生物,鉴定出一种无 5-HT 激动活性的选择性 5-羟色胺 2C(5-HT)受体激动剂。
Eur J Med Chem. 2019 Nov 15;182:111626. doi: 10.1016/j.ejmech.2019.111626. Epub 2019 Aug 14.
4
Development of homogeneous high-affinity agonist binding assays for 5-HT2 receptor subtypes.5-羟色胺2受体亚型的均相高亲和力激动剂结合分析方法的开发。
Assay Drug Dev Technol. 2005 Dec;3(6):649-59. doi: 10.1089/adt.2005.3.649.
5
A novel aminotetralin-type serotonin (5-HT) 2C receptor-specific agonist and 5-HT2A competitive antagonist/5-HT2B inverse agonist with preclinical efficacy for psychoses.一种新型的氨四氢萘型血清素(5-HT)2C 受体特异性激动剂和 5-HT2A 竞争性拮抗剂/5-HT2B 反向激动剂,具有治疗精神疾病的临床前疗效。
J Pharmacol Exp Ther. 2014 May;349(2):310-8. doi: 10.1124/jpet.113.212373. Epub 2014 Feb 21.
6
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.5-羟色胺(5-HT)2A、2B和2C受体激动剂放射性配体结合位点的药理学特性
Naunyn Schmiedebergs Arch Pharmacol. 2004 Aug;370(2):114-23. doi: 10.1007/s00210-004-0951-4. Epub 2004 Jul 30.
7
(1R, 3S)-(-)-trans-PAT: a novel full-efficacy serotonin 5-HT2C receptor agonist with 5-HT2A and 5-HT2B receptor inverse agonist/antagonist activity.(1R, 3S)-(-)-反式-PAT:一种新型的具有5-HT2A和5-HT2B受体反向激动剂/拮抗剂活性的全效血清素5-HT2C受体激动剂。
Eur J Pharmacol. 2009 Aug 1;615(1-3):1-9. doi: 10.1016/j.ejphar.2009.04.035. Epub 2009 May 3.
8
Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist.瓦比沙林(SCA-136)的特性研究,一种选择性 5-羟色胺 2C 受体激动剂。
J Pharmacol Exp Ther. 2011 Jun;337(3):673-80. doi: 10.1124/jpet.111.179572. Epub 2011 Mar 14.
9
Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors.预测激动剂和拮抗剂与血清素 5-HT2B 和 5-HT2C 受体结合的结构和动力学。
J Chem Inf Model. 2011 Feb 28;51(2):420-33. doi: 10.1021/ci100375b. Epub 2011 Feb 7.
10
New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands.新型卤代三(苯基烷基)胺作为5-羟色胺2B受体配体
Bioorg Med Chem Lett. 2016 Jul 15;26(14):3216-3219. doi: 10.1016/j.bmcl.2016.05.079. Epub 2016 May 28.

引用本文的文献

1
"Selective" serotonin 5-HT receptor antagonists.“选择性”血清素 5-HT 受体拮抗剂。
Biochem Pharmacol. 2022 Jun;200:115028. doi: 10.1016/j.bcp.2022.115028. Epub 2022 Apr 4.
2
Synthesis and Biological Evaluation of Disubstituted Pyrimidines as Selective 5-HT Agonists.二取代嘧啶的合成及作为选择性 5-HT 激动剂的生物评价。
Molecules. 2019 Sep 5;24(18):3234. doi: 10.3390/molecules24183234.
3
Identification of Optically Active Pyrimidine Derivatives as Selective 5-HT Modulators.鉴定具有光学活性的嘧啶衍生物为选择性 5-HT 调节剂。

本文引用的文献

1
A Soluble Polymer-Bound Ruthenium Carbene Complex: A Robust and Reusable Catalyst for Ring-Closing Olefin Metathesis.一种可溶性聚合物负载的钌卡宾配合物:用于烯烃复分解关环反应的稳健且可重复使用的催化剂。
Angew Chem Int Ed Engl. 2000 Nov 3;39(21):3896-3898. doi: 10.1002/1521-3773(20001103)39:21<3896::AID-ANIE3896>3.0.CO;2-8.
2
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.三环二氢喹唑啉酮类作为新型 5-HT2C 选择性和口服有效的抗肥胖药物。
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. doi: 10.1016/j.bmcl.2009.12.014. Epub 2009 Dec 6.
3
The expanded biology of serotonin.
Molecules. 2017 Aug 26;22(9):1416. doi: 10.3390/molecules22091416.
4
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.优化(2-苯基环丙基)甲胺作为新型5-羟色胺2C激动剂的进一步进展:对运动亢进、前脉冲抑制和认知模型的影响
J Med Chem. 2016 Jan 28;59(2):578-91. doi: 10.1021/acs.jmedchem.5b01153. Epub 2016 Jan 13.
5
We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.我们需要2C而非2B:开发用于治疗中枢神经系统疾病的5-羟色胺2C(5-HT2C)受体激动剂
ChemMedChem. 2015 Dec;10(12):1963-7. doi: 10.1002/cmdc.201500437. Epub 2015 Oct 28.
6
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.2-苯环丙基甲胺类化合物作为选择性 5-羟色胺 2C 受体激动剂的优化及其作为潜在抗精神病药物的评估。
J Med Chem. 2015 Feb 26;58(4):1992-2002. doi: 10.1021/jm5019274. Epub 2015 Feb 10.
7
Application of palladium-mediated (18)F-fluorination to PET radiotracer development: overcoming hurdles to translation.钯介导的(18)F-氟代在正电子发射断层扫描放射性示踪剂开发中的应用:克服转化障碍。
PLoS One. 2013;8(3):e59187. doi: 10.1371/journal.pone.0059187. Epub 2013 Mar 12.
8
Reward circuitry dysfunction in psychiatric and neurodevelopmental disorders and genetic syndromes: animal models and clinical findings.奖赏回路功能障碍与精神神经发育障碍和遗传综合征:动物模型与临床研究发现。
J Neurodev Disord. 2012 Jul 6;4(1):19. doi: 10.1186/1866-1955-4-19.
9
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.合理药物设计促成一种强效且无5-HT(2B)活性的5-HT(2C)激动剂的鉴定。
ACS Med Chem Lett. 2011 Dec 8;2(12):929-932. doi: 10.1021/ml200206z. Epub 2011 Oct 10.
10
A fluoride-derived electrophilic late-stage fluorination reagent for PET imaging.一种来源于氟化物的亲电晚期氟代试剂,用于正电子发射断层成像术(PET 成像)。
Science. 2011 Nov 4;334(6056):639-42. doi: 10.1126/science.1212625.
血清素的扩展生物学
Annu Rev Med. 2009;60:355-66. doi: 10.1146/annurev.med.60.042307.110802.
4
PSD-95 is essential for hallucinogen and atypical antipsychotic drug actions at serotonin receptors.PSD - 95对于致幻剂和非典型抗精神病药物作用于血清素受体至关重要。
J Neurosci. 2009 Jun 3;29(22):7124-36. doi: 10.1523/JNEUROSCI.1090-09.2009.
5
(1R, 3S)-(-)-trans-PAT: a novel full-efficacy serotonin 5-HT2C receptor agonist with 5-HT2A and 5-HT2B receptor inverse agonist/antagonist activity.(1R, 3S)-(-)-反式-PAT:一种新型的具有5-HT2A和5-HT2B受体反向激动剂/拮抗剂活性的全效血清素5-HT2C受体激动剂。
Eur J Pharmacol. 2009 Aug 1;615(1-3):1-9. doi: 10.1016/j.ejphar.2009.04.035. Epub 2009 May 3.
6
Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.源自先导化合物反苯环丙胺的选择性5-羟色胺2C受体激动剂:具有抗抑郁样作用药物的鉴定。
J Med Chem. 2009 Apr 9;52(7):1885-902. doi: 10.1021/jm801354e.
7
Food and drugs: Arena Pharmaceuticals develops next generation obesity drug.食品与药品:Arena制药公司研发下一代减肥药。
Chem Biol. 2008 Nov 24;15(11):1139-40. doi: 10.1016/j.chembiol.2008.11.002.
8
Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases.血清素5-HT2C受体激动剂:多种疾病的临床前及临床进展
Curr Opin Drug Discov Devel. 2008 Jul;11(4):438-45.
9
N-desalkylquetiapine, a potent norepinephrine reuptake inhibitor and partial 5-HT1A agonist, as a putative mediator of quetiapine's antidepressant activity.N-去烷基喹硫平,一种有效的去甲肾上腺素再摄取抑制剂和5-HT1A部分激动剂,被认为是喹硫平抗抑郁活性的介质。
Neuropsychopharmacology. 2008 Sep;33(10):2303-12. doi: 10.1038/sj.npp.1301646. Epub 2007 Dec 5.
10
Stimulation of serotonin2C receptors influences cocaine-seeking behavior in response to drug-associated stimuli in rats.刺激5-羟色胺2C受体可影响大鼠对与药物相关刺激产生反应时的觅可卡因行为。
Psychopharmacology (Berl). 2008 Jan;196(1):15-27. doi: 10.1007/s00213-007-0916-7. Epub 2007 Sep 27.