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Synthesis and in vivo evaluation of the putative breast cancer resistance protein inhibitor 11Cmethyl 4-((4-(2-(67-dimethoxy-1234-tetrahydroisoquinolin-2-yl)ethyl)phenyl)amino-carbonyl)-2-(quinoline-2-carbonylamino)benzoate

机译：合成和体内评价推定的乳腺癌抗性蛋白抑制剂11c甲基4 - （（4-（2-（2-（2-（2-（67-二甲氧基-1234-四氢喹啉-2-基）乙基）苯基）氨基 - 羰基）-2-（喹啉-2-羰基氨基）苯甲酸盐

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IntroductionThe multidrug efflux transporter breast cancer resistance protein (BCRP) is highly expressed in the blood-brain barrier (BBB), where it limits brain entry of a broad range of endogenous and exogenous substrates. Methyl 4-((4-(2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl)phenyl)amino-carbonyl)-2-(quinoline-2-carbonylamino)benzoate (>1) is a recently discovered BCRP-selective inhibitor, which is structurally derived from the potent P-glycoprotein (P-gp) inhibitor tariquidar. The aim of this study was to develop a new PET tracer based on >1 to map BCRP expression levels in vivo.

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作者
Severin Mairinger; Oliver Langer; Claudia Kuntner; Thomas Wanek; Jens P. Bankstahl; Marion Bankstahl; Johann Stanek; Bernd Dörner; Florian Bauer; Christoph Baumgartner; Wolfgang Löscher; Thomas Erker; Markus Müller;
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年(卷),期 -1(37),5
年度 -1
页码 637–644
总页数 15
原文格式 PDF
正文语种
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关键词
breast cancer resistance protein P-glycoprotein blood-brain barrier PET inhibitor tariquidar;

机译：乳腺癌抗性蛋白;P-糖蛋白;血脑屏障;PET;抑制剂;tariquidar;

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1. Synthesis and in vivo evaluation of the putative breast cancer resistance protein inhibitor (11C)methyl 4-((4-(2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl)phenyl)amino-car bonyl)-2-(quinoline-2-carbonylamino)benzoate. [J] . Mairinger S, Langer O, Kuntner C, Nuclear Medicine and Biology . 2010,第5期

机译：推定的乳腺癌抗性蛋白抑制剂（11C）甲基4-（（4-（2-（6,7-二甲氧基-1,2,3,4-四氢异喹啉-2-基）乙基）苯基）的合成及体内评价）氨基-汽车羰基）-2-（喹啉-2-羰基氨基）苯甲酸酯。
2. Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 4-{4-[2-(4-(2-substitutedquinoxalin-3-yl)piperazin-l-yl)ethyl]phenyl}thiazoles as atypical antipsychotic agents [J] . Kondapalli Venkata Gowri Chra Sekhar, Vajja Sambasiva Rao, Winnie Deuther-Conrad, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2013,第4期

机译：非典型抗精神病药4- {4- [2-（4-（2-（2-取代的喹喔啉-3-基）哌嗪-1-基）乙基]苯基]噻唑的设计，合成及体外和体内初步药理评估
3. Synthesis and initial PET imaging of new potential NK1 receptor radioligands 1-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-4-[C-11]methyl-piperazine and {4-[2-(3,5-bis-trifluoromethyl-benzyloxy)-1-phenyl-ethyl]-piperazine-1-yl}-acetic acid [J] . Gao MZ, Mock BH, Hutchins GD, Nuclear Medicine and Biology . 2005,第5期

机译：新的潜在NK1受体放射性配体1- [2-（3,5-双-三氟甲基-苄氧基）-1-苯基-乙基] -4- [C-11]甲基-哌嗪和{4- [ 2-（3,5-双三氟甲基-苄氧基）-1-苯基-乙基]-哌嗪-1-基}-乙酸
4. Synthesis of 2-(4-((6-bromo-3-nitroquinolin-4-yl)amino) phenyl)-2-methylpropanenitrile [C] . Fei Lei, Yuanbiao Tu, Min Wang, International Conference on Applied Science and Engineering Innovation . 2015

机译：合成2-（4 - （（6-溴-3-硝基喹啉-4-基）氨基）苯基）-2-甲基丙二腈
5. Synthesis and in vivo evaluation of 18F2-(4-(4-(2-(2-fluoroethoxy)phenyl)piperazin-1-yl)butyl)-4-methyl-124-triazine-35(2H4H)-dione (18FFECUMI-101) as an imaging probe for 5-HT1A receptor agonist in nonhuman primates [O] . Vattoly J. Majo, Matthew S. Milak, Jaya Prabhakaran, -1

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6. Synthesis and in vivo evaluation of the putative breast cancer resistance protein inhibitor 11Cmethyl 4-((4-(2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl)phenyl)amino-carbonyl)-2-(quinoline-2-carbonylamino)benzoate [O] . Severin Mairinger, Oliver Langer, Claudia Kuntner, 2010

机译：合成和体内评价推定的乳腺癌抗性蛋白抑制剂11c甲基4 - （（4-（2-（2-（2-（2-（6,7-二甲氧基-1,2,3,4-四氢喹啉-2-基）乙基）苯基）氨基 - 羰基）-2-（喹啉-2-羰基氨基）苯甲酸盐
7. Results of a OECD 422 Combined Repeated Dose Toxicity Study with the Reproduction/Development Toxicity Screening Test in Rats with (2- ((2-cyano-3-(4- (diethylamino)phenyl) -1-oxoallyl)oxy)ethyl) (3- ((2-cyano-3-(4- (diethylamino)phenyl) -1-oxoallyl)oxy)p [R] . 2012

机译：OECD 422联合重复剂量毒性研究结果与大鼠（2 - （（2-氰基-3-（4-（二乙基氨基）苯基）-1-氧代烯丙基）氧基）乙基）的生殖/发育毒性筛选试验结果（ 3-（（2-氰基-3-（4-（二乙基氨基）苯基）-1-氧代烯丙基）氧基）p

Synthesis and in vivo evaluation of the putative breast cancer resistance protein inhibitor 11Cmethyl 4-((4-(2-(67-dimethoxy-1234-tetrahydroisoquinolin-2-yl)ethyl)phenyl)amino-carbonyl)-2-(quinoline-2-carbonylamino)benzoate

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