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11C标记的(±)-5-甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺[(±)-[11C]MK801]的合成

Synthesis of 11C-labeled (+-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imin e [(+-)-[11C]MK801].

作者信息

Kiesewetter D O, Finn R D, Rice K C, Monn J A

机构信息

Department of Nuclear Medicine, Warren Grant Magnuson Clinical Center, National Institutes of Health, Bethesda, MD 20892.

出版信息

Int J Rad Appl Instrum A. 1990;41(2):139-42. doi: 10.1016/0883-2889(90)90098-2.

DOI:10.1016/0883-2889(90)90098-2
PMID:2158943
Abstract

The synthesis of C5 labeled (+-)-5-[11C]methyl-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten- 5,10-imine [(+-)-[11C]MK801] has been accomplished via alkylation of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-5,10-imine-N-t- butylformamidine [(+-)-5-des-methyl MK801 formamidine). The 11C labeling is accomplished by reaction of the anion of (+-)-5-des-methyl MK801 formamidine, generated with s-butyllithium, and [11C]methyl iodide.

摘要

通过对(±)-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺-N-叔丁基甲脒[(±)-5-去甲基MK801甲脒]进行烷基化反应,已完成C5标记的(±)-5-[11C]甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺[(±)-[11C]MK801]的合成。11C标记是通过用仲丁基锂生成的(±)-5-去甲基MK801甲脒的阴离子与[11C]碘甲烷反应来实现的。

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Synthesis of 11C-labeled (+-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imin e [(+-)-[11C]MK801].11C标记的(±)-5-甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺[(±)-[11C]MK801]的合成
Int J Rad Appl Instrum A. 1990;41(2):139-42. doi: 10.1016/0883-2889(90)90098-2.
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Synthesis and structure-activity relationship of C5-substituted analogues of (+-)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine [(+-)-desmethyl-MK801]: ligands for the NMDA receptor-coupled phencyclidine binding site.
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Structure and activity of hydrogenated derivatives of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801).
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Effects of the NMDA receptor/channel antagonists CPP and MK801 on hippocampal field potentials and long-term potentiation in anesthetized rats.
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Disposition and metabolism of (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imine in rats, dogs, and monkeys.(+)-5-甲基-10,11-二氢-5H-二苯并[a,d]环庚烯-5,10-亚胺在大鼠、狗和猴子体内的处置与代谢
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Amitriptyline metabolites. Synthesis of (R,S)-(Z)- and (R,S)-(E)- N-methyl(10,11-dihydro-10-hydroxy-5H-dibenzo(a,d)cycloheptene)- 5, -propylamine.
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Regional variations in [3H]MK801 binding to rat brain N-methyl-D-aspartate receptors.大鼠脑 N-甲基-D-天冬氨酸受体上[3H]MK801 结合的区域差异。
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Attenuation and reversal of morphine tolerance by the competitive N-methyl-D-aspartate receptor antagonist, LY274614.
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MK-801 blocks NMDA receptor-mediated synaptic transmission and long term potentiation in rat hippocampal slices.MK-801阻断大鼠海马切片中N-甲基-D-天冬氨酸(NMDA)受体介导的突触传递和长时程增强。
Neurosci Lett. 1987 Sep 11;80(1):111-4. doi: 10.1016/0304-3940(87)90505-2.

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