评估新型 5-HT1B 放射性配体 [¹¹C]p943 对内源性血清素释放的敏感性。
Assessing the sensitivity of [¹¹C]p943, a novel 5-HT1B radioligand, to endogenous serotonin release.
机构信息
Department of Psychiatry, Yale University School of Medicine, New Haven, Connecticut, USA.
出版信息
Synapse. 2011 Oct;65(10):1113-7. doi: 10.1002/syn.20942. Epub 2011 May 3.
Abstract
The main objective of the current study was to determine the sensitivity of the positron emission tomography (PET) radioligand [¹¹C]P943 to fenfluramine-induced changes in endogenous 5-HT in nonhuman primate brain. Fenfluramine-induced changes in 5-HT(1B) occupancy were compared to those obtained by self-block with unlabeled P943. Two baboons and 1 rhesus monkey were given preblocking or displacing doses of fenfluramine (1-5 mg/kg) or preblocking doses of unlabeled P943 (0.2 mg/kg) and imaged with [¹¹C]P943 PET. Receptor occupancy by the low dose of fenfluramine (1 mg/kg) in the baboons was 25 and 29% and by the high dose of fenfluramine (5 mg/kg) in the rhesus macaque was 42%. Receptor occupancy by P943 (0.2 mg/kg) was 68 and 86% in the baboons. PET imaging of 5-HT(1B) receptors with [¹¹C]P943 may be a useful approach for measuring changes in endogenous 5-HT in the living human brain.
摘要
本研究的主要目的是确定正电子发射断层扫描（PET）示踪剂 [¹¹C]P943 对非人类灵长类动物脑内内源性 5-HT 诱导变化的敏感性。将芬氟拉明诱导的 5-HT（1B）占有率变化与用未标记的 P943 进行的自阻断获得的变化进行比较。给两只狒狒和 1 只恒河猴给予预阻断或置换剂量的芬氟拉明（1-5mg/kg）或未标记的 P943（0.2mg/kg）预阻断剂量，并进行 [¹¹C]P943 PET 成像。低剂量芬氟拉明（1mg/kg）在狒狒中的受体占有率为 25%和 29%，高剂量芬氟拉明（5mg/kg）在恒河猴中的受体占有率为 42%。P943（0.2mg/kg）在狒狒中的受体占有率为 68%和 86%。用 [¹¹C]P943 对 5-HT（1B）受体进行 PET 成像可能是测量活体人脑内内源性 5-HT 变化的一种有用方法。
相似文献
1
Assessing the sensitivity of [¹¹C]p943, a novel 5-HT1B radioligand, to endogenous serotonin release.评估新型 5-HT1B 放射性配体 [¹¹C]p943 对内源性血清素释放的敏感性。
Synapse. 2011 Oct;65(10):1113-7. doi: 10.1002/syn.20942. Epub 2011 May 3.
2
Characterization of in vivo pharmacological properties and sensitivity to endogenous serotonin of [11C] P943: a positron emission tomography study in Papio anubis.在 Papio anubis 中进行的 [11C] P943 正电子发射断层扫描研究：体内药理学特性和对内源性 5-羟色胺敏感性的特征
Synapse. 2011 Nov;65(11):1119-27. doi: 10.1002/syn.20946. Epub 2011 May 19.
3
High-resolution imaging of brain 5-HT 1B receptors in the rhesus monkey using [11C]P943.使用[11C]P943 对恒河猴大脑 5-HT1B 受体进行高分辨率成像。
Nucl Med Biol. 2010 Feb;37(2):205-14. doi: 10.1016/j.nucmedbio.2009.10.007. Epub 2009 Dec 1.
4
Fenfluramine-induced serotonin release decreases [11C]AZ10419369 binding to 5-HT1B-receptors in the primate brain.芬氟拉明诱导的血清素释放降低了灵长类动物大脑中 5-HT1B 受体对 [11C]AZ10419369 的结合。
Synapse. 2010 Jul;64(7):573-7. doi: 10.1002/syn.20780.
5
Kinetic modeling of the serotonin 5-HT(1B) receptor radioligand [(11)C]P943 in humans.人类血清素 5-HT(1B)受体放射性配体 [(11)C]P943 的动力学建模。
J Cereb Blood Flow Metab. 2010 Jan;30(1):196-210. doi: 10.1038/jcbfm.2009.195. Epub 2009 Sep 23.
6
[C]AZ10419096 - a full antagonist PET radioligand for imaging brain 5-HT receptors.[C]AZ10419096——一种用于脑5-羟色胺受体成像的完全拮抗剂正电子发射断层显像放射性配体。
Nucl Med Biol. 2017 Nov;54:34-40. doi: 10.1016/j.nucmedbio.2017.07.007. Epub 2017 Jul 21.
7
Test-retest reliability of the novel 5-HT1B receptor PET radioligand [11C]P943.新型 5-HT1B 受体 PET 放射性配体 [11C]P943 的重测信度。
Eur J Nucl Med Mol Imaging. 2015 Mar;42(3):468-77. doi: 10.1007/s00259-014-2958-5. Epub 2014 Nov 27.
8
The effect of early trauma exposure on serotonin type 1B receptor expression revealed by reduced selective radioligand binding.早期创伤暴露对血清素1B型受体表达的影响通过选择性放射性配体结合减少得以揭示。
Arch Gen Psychiatry. 2011 Sep;68(9):892-900. doi: 10.1001/archgenpsychiatry.2011.91.
9
Reduced ventral striatal/ventral pallidal serotonin1B receptor binding potential in major depressive disorder.在重度抑郁症患者中，腹侧纹状体/腹侧苍白球 5-羟色胺 1B 受体结合潜能降低。
Psychopharmacology (Berl). 2011 Feb;213(2-3):547-53. doi: 10.1007/s00213-010-1881-0. Epub 2010 May 18.
10
Dose-dependent binding of AZD3783 to brain 5-HT1B receptors in non-human primates and human subjects: a positron emission tomography study with [11C]AZ10419369.在非人类灵长类动物和人类受试者中，AZD3783 与脑 5-HT1B 受体的剂量依赖性结合：使用 [11C]AZ10419369 的正电子发射断层扫描研究。
Psychopharmacology (Berl). 2011 Feb;213(2-3):533-45. doi: 10.1007/s00213-011-2165-z. Epub 2011 Jan 15.
引用本文的文献
1
Inverse changes in raphe and cortical 5-HT receptor availability after acute tryptophan depletion in healthy human subjects.健康人体中急性色氨酸耗竭后中缝核和皮质 5-HT 受体可用性的反向变化。
Synapse. 2020 Oct;74(10):e22159. doi: 10.1002/syn.22159. Epub 2020 May 7.
2
Serotonin concentration enhancers at clinically relevant doses reduce [C]AZ10419369 binding to the 5-HT receptors in the nonhuman primate brain.在临床相关剂量下，血清素浓度增强剂可降低 [C]AZ10419369 与非人类灵长类动物大脑中 5-HT 受体的结合。
Transl Psychiatry. 2018 Jul 16;8(1):132. doi: 10.1038/s41398-018-0178-7.
3
Cerebral serotonin release correlates with [C]AZ10419369 PET measures of 5-HT receptor binding in the pig brain.大脑中血清素的释放与猪脑 5-HT 受体结合的 [C]AZ10419369 PET 测量结果相关。
J Cereb Blood Flow Metab. 2018 Jul;38(7):1243-1252. doi: 10.1177/0271678X17719390. Epub 2017 Jul 7.
4
OCD is associated with an altered association between sensorimotor gating and cortical and subcortical 5-HT1b receptor binding.强迫症与感觉运动门控和皮质及皮质下5-羟色胺1b受体结合之间的关联改变有关。
J Affect Disord. 2016 May 15;196:87-96. doi: 10.1016/j.jad.2016.02.021. Epub 2016 Feb 9.
5
Serotonin transporter occupancy by escitalopram and citalopram in the non-human primate brain: a [(11)C]MADAM PET study.艾司西酞普兰和西酞普兰对非人灵长类动物大脑中5-羟色胺转运体的占据情况：一项[(11)C]MADAM PET研究。
Psychopharmacology (Berl). 2015 Nov;232(21-22):4159-67. doi: 10.1007/s00213-015-3961-7. Epub 2015 May 17.
6
Application of cross-species PET imaging to assess neurotransmitter release in brain.跨物种正电子发射断层显像（PET）成像在评估脑内神经递质释放中的应用。
Psychopharmacology (Berl). 2015 Nov;232(21-22):4129-57. doi: 10.1007/s00213-015-3938-6. Epub 2015 Apr 30.
7
Test-retest reliability of the novel 5-HT1B receptor PET radioligand [11C]P943.新型 5-HT1B 受体 PET 放射性配体 [11C]P943 的重测信度。
Eur J Nucl Med Mol Imaging. 2015 Mar;42(3):468-77. doi: 10.1007/s00259-014-2958-5. Epub 2014 Nov 27.
8
PET tracers for serotonin receptors and their applications.用于血清素受体的正电子发射断层显像（PET）示踪剂及其应用。
Cent Nerv Syst Agents Med Chem. 2014;14(2):96-112. doi: 10.2174/1871524914666141030124316.
9
Reductions in brain 5-HT1B receptor availability in primarily cocaine-dependent humans.原发性可卡因依赖者大脑5-HT1B受体可用性降低。
Biol Psychiatry. 2014 Nov 15;76(10):816-22. doi: 10.1016/j.biopsych.2013.11.022. Epub 2013 Nov 28.
10
Creating dynamic images of short-lived dopamine fluctuations with lp-ntPET: dopamine movies of cigarette smoking.利用正电子发射断层扫描（lp-ntPET）创建短寿命多巴胺波动的动态图像：吸烟的多巴胺影像
J Vis Exp. 2013 Aug 6(78):50358. doi: 10.3791/50358.
本文引用的文献
1
Measuring endogenous 5-HT release by emission tomography: promises and pitfalls.通过发射型计算机断层扫描测量内源性 5-HT 释放：前景与挑战。
J Cereb Blood Flow Metab. 2010 Oct;30(10):1682-706. doi: 10.1038/jcbfm.2010.104. Epub 2010 Jul 28.
2
Quantification of smoking-induced occupancy of beta2-nicotinic acetylcholine receptors: estimation of nondisplaceable binding.吸烟诱导β2-烟碱型乙酰胆碱受体占有率的定量：不可置换结合的估计。
J Nucl Med. 2010 Aug;51(8):1226-33. doi: 10.2967/jnumed.109.072447. Epub 2010 Jul 21.
3
Reduced ventral striatal/ventral pallidal serotonin1B receptor binding potential in major depressive disorder.在重度抑郁症患者中，腹侧纹状体/腹侧苍白球 5-羟色胺 1B 受体结合潜能降低。
Psychopharmacology (Berl). 2011 Feb;213(2-3):547-53. doi: 10.1007/s00213-010-1881-0. Epub 2010 May 18.
4
Fenfluramine-induced serotonin release decreases [11C]AZ10419369 binding to 5-HT1B-receptors in the primate brain.芬氟拉明诱导的血清素释放降低了灵长类动物大脑中 5-HT1B 受体对 [11C]AZ10419369 的结合。
Synapse. 2010 Jul;64(7):573-7. doi: 10.1002/syn.20780.
5
High-resolution imaging of brain 5-HT 1B receptors in the rhesus monkey using [11C]P943.使用[11C]P943 对恒河猴大脑 5-HT1B 受体进行高分辨率成像。
Nucl Med Biol. 2010 Feb;37(2):205-14. doi: 10.1016/j.nucmedbio.2009.10.007. Epub 2009 Dec 1.
6
Impact of D2 receptor internalization on binding affinity of neuroimaging radiotracers.D2 受体内化对神经影像学示踪剂结合亲和力的影响。
Neuropsychopharmacology. 2010 Feb;35(3):806-17. doi: 10.1038/npp.2009.189. Epub 2009 Dec 2.
7
Kinetic modeling of the serotonin 5-HT(1B) receptor radioligand [(11)C]P943 in humans.人类血清素 5-HT(1B)受体放射性配体 [(11)C]P943 的动力学建模。
J Cereb Blood Flow Metab. 2010 Jan;30(1):196-210. doi: 10.1038/jcbfm.2009.195. Epub 2009 Sep 23.
8
Measuring drug occupancy in the absence of a reference region: the Lassen plot re-visited.在缺乏参照区域的情况下测量药物占有率：重新审视 Lassen 图。
J Cereb Blood Flow Metab. 2010 Jan;30(1):46-50. doi: 10.1038/jcbfm.2009.190. Epub 2009 Sep 9.
9
The 5-HT1B receptor: a novel target for the pathophysiology of depression.5-HT1B 受体：抑郁症病理生理学的新靶点。
Curr Drug Targets. 2009 Nov;10(11):1118-38. doi: 10.2174/138945009789735192.
10
Modified receptor internalization upon coexpression of 5-HT1B receptor and 5-HT2B receptors.5-HT1B受体与5-HT2B受体共表达时受体的内化修饰
Mol Pharmacol. 2007 Jun;71(6):1463-74. doi: 10.1124/mol.106.032656. Epub 2007 Feb 26.
Zotero 插件