Discovery of the first potent, selective 5-hydroxytryptamine(1D) receptor antagonist

Ward SE; Harrington FP; Gordon LJ; Hopley SC; Scott CM; Watson JM

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Discovery of the first potent, selective 5-hydroxytryptamine(1D) receptor antagonist

机译：发现第一个有效的，选择性的5-羟色胺（1D）受体拮抗剂

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A series of 5-(piperidinylethyloxy)quinoline 5-hydroxytryptamine(1D) (5-HT1D) receptor antagonists have been discovered from elaboration of the series of dual 5-hydroxy-tryptamine(1) -selective serotonin reuptake inhibitors (5HT(1)-SSRIs) reported previously. This is the first report of highly potent, selective antagonists for the 5-HT1D receptor, which represents an extremely useful set of pharmacological tools for further understanding the roles of the 5-HT1 receptor subtypes.

机译：通过精心设计一系列5-羟色胺（1）-选择性5-羟色胺再摄取抑制剂（5HT（1）），发现了一系列5-（哌啶基乙氧基）喹啉5-羟色胺（5-HT1D）受体拮抗剂。 -SSRIs）。这是有关5-HT1D受体的高效，选择性拮抗剂的首次报道，它是进一步了解5-HT1D受体亚型作用的极为有用的一组药理学工具。

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《Journal of Medicinal Chemistry》 |2005年第10期|共3页
作者
Ward SE; Harrington FP; Gordon LJ; Hopley SC; Scott CM; Watson JM;
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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
5-HT AUTORECEPTOR FUNCTION; IN-VITRO; SUBTYPES; AGONISTS; BRAIN;

机译：5-HT受体功能;体外;亚型;激动剂;脑;

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1. Discovery of the first potent, selective 5-hydroxytryptamine(1D) receptor antagonist [J] . Ward SE, Harrington FP, Gordon LJ, Journal of Medicinal Chemistry . 2005,第10期

机译：发现第一个有效的，选择性的5-羟色胺（1D）受体拮抗剂
2. Multiparameter Optimization in CNS Drug Discovery: Design of Pyrimido[4,5-d]azepines as Potent 5-Hydroxytryptamine 2C (5-HT_(2C)) Receptor Agonists with Exquisite Functional Selectivity over 5-HT_(2A) and 5-HT_(2B) Receptors [J] . R. Ian Storer, Paul E. Brennan, Alan D. Brown, Journal of Medicinal Chemistry . 2014,第12期

机译：在中枢神经系统药物发现中的多参数优化：嘧啶基[4,5-d]氮杂烷作为有效的5-羟色胺2C（5-HT_（2C））受体激动剂的设计，在5-HT_（2A）和5-HT_（ 2B）受体
3. Structure-Activity Relationships of a Novel Class of Endothelin-A Receptor Antagonists and Discovery of Potent and Selective Receptor Antagonist, 2-(Benzo[1,3]dioxol-5-yl)-6-isopropyloxy-4-(4-methoxyphenyl)-2H-chromene-3-carboxylic Acid (S-1255). 1. [J] . Natsuki Ishizuka, Ken-ichi Matsumura, Katsunori Sakai, Journal of Medicinal Chemistry . 2002,第10期

机译：一类新型内皮素-A受体拮抗剂的结构-活性关系和有效和选择性受体拮抗剂2-（苯并[1,3]二氧杂-5-基）-6-异丙氧基-4-（4-甲氧基苯基）的发现-2H-苯甲基-3-羧酸（S-1255）。 1。
4. Potent and selective peptide agonist/antagonist analogues at human melanocortin receptor-4 [C] . Minying Cai, Paolo Grieco, Dev Trivedi, European Peptide Symposium . 2002

机译：有效和选择性肽激动剂/拮抗剂类似物在人黑色主义素受体-4
5. Potent derivatives of the bradykinin B2 receptor antagonist Hoe 140 containing analogues of arginine and lysine with increased hydrophobicity. [D] . Kennedy, Kevin Joseph. 1999

机译：缓激肽B2受体拮抗剂Hoe 140的强效衍生物含有精氨酸和赖氨酸的类似物，疏水性增强。
6. Design and Microwave-Assisted Synthesis of Novel Macrocyclic Peptides Active at Melanocortin Receptors: Discovery of Potent and Selective hMC5R Receptor Antagonists [O] . Paolo Grieco, Minying Cai, Lu Liu, -1

机译：黑色素皮质激素受体活性的新型大环肽的设计和微波辅助合成：有效和选择性hMC5R受体拮抗剂的发现。
7. Design and Microwave-Assisted Synthesis of Novel Macrocyclic Peptides Active at Melanocortin Receptors: Discovery of Potent and Selective hMC5R Receptor Antagonists. [O] . Grieco P., Cai M., Liu L., 2008

机译：设计和微波辅助合成在黑皮质素受体中活跃的新型大环肽：发现有效和选择性hmC5R受体拮抗剂。
8. Mercuric Ions are Potent Noncompetitive Antagonists of Human Brain Kainate Receptors Expressed in 'Xenopus oocytes'. [R] . Umbach, J. A., Gundersen, C. B. 1989

机译：汞离子是非洲爪蟾卵母细胞中表达的人脑红藻氨酸受体的强效非竞争性拮抗剂。

Discovery of the first potent, selective 5-hydroxytryptamine(1D) receptor antagonist

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