• 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

PET measurement of neuroreceptor occupancy by typical and atypical neuroleptics.

作者信息

Goyer P F, Berridge M S, Morris E D, Semple W E, Compton-Toth B A, Schulz S C, Wong D F, Miraldi F, Meltzer H Y

机构信息

Cleveland Veterans Affairs Medical Center, Ohio 44141, USA.

出版信息

J Nucl Med. 1996 Jul;37(7):1122-7.

PMID:8965181
Abstract

UNLABELLED

The goal of this study was to use PET and 11C-N-methylspiperone (11C-NMSP) to measure the difference in relative occupancy of serotonin (5-hydroxytryptamine-2 or 5-HT2A) and dopamine-2 (D2) neuroreceptors in subjects being treated with typical or atypical antipsychotic drugs.

METHODS

We used PET and single-dose 11C-NMSP to measure receptor indices and relative receptor occupancy of 5-HT2A receptors in frontal cortex and D2 receptors in basal ganglia in five subjects who were neuroleptic free, five subjects who were being treated with typical antipsychotic drugs and five subjects who were being treated with clozapine, an atypical antipsychotic drug.

RESULTS

Among the three groups, there were significant differences in 5-HT2A indices, D2 indices and the ratio of 5-HT2A to D2 indices. With no overlap, the 5-HT2A index separated all subjects who received clozapine and the D2 index separated the remaining two groups.

CONCLUSION

Typical antipsychotic and atypical antipsychotic subjects do have differing patterns of 5-HT2A and D2 relative receptor occupancy when measured with a single PET scan, single 11C-NMSP radiotracer dose and no separately injected "cold" pharmaceutical.

摘要

相似文献

1
PET measurement of neuroreceptor occupancy by typical and atypical neuroleptics.
J Nucl Med. 1996 Jul;37(7):1122-7.
2
Suggested minimal effective dose of risperidone based on PET-measured D2 and 5-HT2A receptor occupancy in schizophrenic patients.基于正电子发射断层扫描(PET)测量的精神分裂症患者D2和5-羟色胺2A(5-HT2A)受体占有率的利培酮建议最小有效剂量。
Am J Psychiatry. 1999 Jun;156(6):869-75. doi: 10.1176/ajp.156.6.869.
3
Binding of antipsychotic drugs to cortical 5-HT2A receptors: a PET study of chlorpromazine, clozapine, and amisulpride in schizophrenic patients.抗精神病药物与皮质5-羟色胺2A受体的结合:一项关于氯丙嗪、氯氮平和氨磺必利在精神分裂症患者中的正电子发射断层扫描研究。
Am J Psychiatry. 1998 Apr;155(4):505-8. doi: 10.1176/ajp.155.4.505.
4
Clinical and theoretical implications of 5-HT2 and D2 receptor occupancy of clozapine, risperidone, and olanzapine in schizophrenia.氯氮平、利培酮和奥氮平对5-HT2和D2受体的占据在精神分裂症中的临床及理论意义。
Am J Psychiatry. 1999 Feb;156(2):286-93. doi: 10.1176/ajp.156.2.286.
5
Atypical antipsychotics: mechanism of action.非典型抗精神病药物:作用机制
Can J Psychiatry. 2002 Feb;47(1):27-38.
6
A positron emission tomography study of quetiapine in schizophrenia: a preliminary finding of an antipsychotic effect with only transiently high dopamine D2 receptor occupancy.一项关于喹硫平治疗精神分裂症的正电子发射断层扫描研究:仅短暂性高多巴胺D2受体占有率的抗精神病作用的初步发现。
Arch Gen Psychiatry. 2000 Jun;57(6):553-9. doi: 10.1001/archpsyc.57.6.553.
7
Differential effects of aripiprazole on D(2), 5-HT(2), and 5-HT(1A) receptor occupancy in patients with schizophrenia: a triple tracer PET study.阿立哌唑对精神分裂症患者D(2)、5-HT(2)和5-HT(1A)受体占有率的差异效应:一项三重示踪正电子发射断层扫描研究
Am J Psychiatry. 2007 Sep;164(9):1411-7. doi: 10.1176/appi.ajp.2007.06091479.
8
Characterization of typical and atypical antipsychotic drugs based on in vivo occupancy of serotonin2 and dopamine2 receptors.基于5-羟色胺2和多巴胺2受体的体内占有率对典型和非典型抗精神病药物的表征
J Pharmacol Exp Ther. 1993 Sep;266(3):1374-84.
9
5-HT2 and D2 receptor occupancy of olanzapine in schizophrenia: a PET investigation.奥氮平对精神分裂症患者5-HT2和D2受体的占有率:一项正电子发射断层扫描(PET)研究
Am J Psychiatry. 1998 Jul;155(7):921-8. doi: 10.1176/ajp.155.7.921.
10
High 5-HT2 receptor occupancy in clozapine treated patients demonstrated by PET.正电子发射断层扫描(PET)显示氯氮平治疗的患者5-HT2受体占有率高。
Psychopharmacology (Berl). 1993;110(3):365-7. doi: 10.1007/BF02251294.

引用本文的文献

1
Classics in Chemical Neuroscience: Aripiprazole.《化学神经科学经典:阿立哌唑》
ACS Chem Neurosci. 2017 Jun 21;8(6):1135-1146. doi: 10.1021/acschemneuro.7b00087. Epub 2017 Apr 13.
2
Glutamate and dopamine in schizophrenia: an update for the 21st century.精神分裂症中的谷氨酸和多巴胺:21世纪的最新进展
J Psychopharmacol. 2015 Feb;29(2):97-115. doi: 10.1177/0269881114563634. Epub 2015 Jan 13.
3
Neuroprotection of paliperidone on SH-SY5Y cells against β-amyloid peptide(25-35), N-methyl-4-phenylpyridinium ion, and hydrogen peroxide-induced cell death.
帕利哌酮对 SH-SY5Y 细胞抵抗β-淀粉样肽(25-35)、N-甲基-4-苯基吡啶离子和过氧化氢诱导的细胞死亡的神经保护作用。
Psychopharmacology (Berl). 2011 Oct;217(3):397-410. doi: 10.1007/s00213-011-2291-7. Epub 2011 Apr 27.
4
Mechanisms underlying psychosis and antipsychotic treatment response in schizophrenia: insights from PET and SPECT imaging.精神分裂症中精神病性症状及抗精神病药物治疗反应的潜在机制:PET与SPECT成像研究的见解
Curr Pharm Des. 2009;15(22):2550-9. doi: 10.2174/138161209788957528.
5
Activation of the JAK-STAT pathway by olanzapine is necessary for desensitization of serotonin2A receptor-stimulated phospholipase C signaling in rat frontal cortex but not serotonin2A receptor-stimulated hormone release.奥氮平激活 JAK-STAT 通路对于大鼠前额叶皮质中 5-羟色胺 2A 受体刺激的磷酯酶 C 信号转导脱敏是必需的,但对 5-羟色胺 2A 受体刺激的激素释放则不是必需的。
J Psychopharmacol. 2010 Jul;24(7):1079-88. doi: 10.1177/0269881109103090. Epub 2009 Mar 20.
6
A review of the literature on neuroimaging of serotoninergic function in Alzheimer's disease and related disorders.关于阿尔茨海默病及相关疾病中血清素能功能的神经影像学文献综述。
J Neural Transm (Vienna). 2007 Sep;114(9):1179-85. doi: 10.1007/s00702-007-0636-5. Epub 2007 Feb 19.
7
Mechanism of action of atypical antipsychotic drugs and the neurobiology of schizophrenia.非典型抗精神病药物的作用机制与精神分裂症的神经生物学
CNS Drugs. 2006;20(5):389-409. doi: 10.2165/00023210-200620050-00004.
8
Family-based association study of the serotonin-2A receptor gene (5-HT2A) and bipolar disorder.基于家系的血清素-2A受体基因(5-HT2A)与双相情感障碍的关联研究。
Neuromolecular Med. 2002;2(3):251-9. doi: 10.1385/NMM:2:3:251.