Novel and potent human and rat beta(3)-Adrenergic receptor agonists containing substituted 3-indolylalkylamines.

Harada H; Hirokawa Y; Suzuki K; Hiyama Y; Oue M; Kawashima H; Yoshida N; Furutani Y; Kato S

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Novel and potent human and rat beta(3)-Adrenergic receptor agonists containing substituted 3-indolylalkylamines.

【24h】

Novel and potent human and rat beta(3)-Adrenergic receptor agonists containing substituted 3-indolylalkylamines.

机译：新型和有效的人类和大鼠β（3）-肾上腺素能受体激动剂，含有取代的3-吲哚基烷基胺。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanols was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human beta(3)-AR. The optically active 30a was found to be the most potent and selective human beta(3)-AR agonist in this series with an EC(50) value of 0.062nM. In addition, 30a selectivity for human beta(3)-AR was 210-fold and 103-fold that for human beta(2)-AR and beta(1)-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat beta(3)-AR.

机译：制备了一系列新型的2-（3-吲哚基）烷基氨基-1-（3-氯苯基）乙醇，并评估了体外刺激表达克隆的人β（3）-AR的中国仓鼠卵巢细胞中cAMP产生的能力。发现旋光性30a是该系列中最有效和选择性最强的人β（3）-AR激动剂，EC（50）值为0.062nM。此外，对人beta（3）-AR的30a选择性分别为对人beta（2）-AR和beta（1）-AR的210倍和103倍。此外，30a对大鼠beta（3）-AR表现出强大的激动作用。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2003年第7期|共5页
作者
Harada H; Hirokawa Y; Suzuki K; Hiyama Y; Oue M; Kawashima H; Yoshida N; Furutani Y; Kato S;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
Human; receptor; agonists; novel;

机译：人;受体;激动剂;新颖;

相似文献

外文文献
中文文献
专利

1. Novel and potent human and rat beta(3)-Adrenergic receptor agonists containing substituted 3-indolylalkylamines. [J] . Harada H, Hirokawa Y, Suzuki K, Bioorganic and Medicinal Chemistry Letters . 2003,第7期

机译：新型和有效的人类和大鼠β（3）-肾上腺素能受体激动剂，含有取代的3-吲哚基烷基胺。
2. Metabolism of a thiazole benzenesulfonamide derivative, a potent and elective agonist of the human beta3-adrenergic receptor, in rats: identification of a novel isethionic acid conjugate. [J] . Tang W, Stearns RA, Miller RR, Drug Metabolism and Disposition: The Biological Fate of Chemicals . 2002,第7期

机译：噻唑苯磺酰胺衍生物（一种人β3-肾上腺素能受体的强效和选择性激动剂）在大鼠中的代谢：新型异乙酸共轭物的鉴定。
3. Discovery of a novel and potent human and rat beta(3)-adrenergic receptor agonist, [3-[(2R)-[[(2R)-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1H-indol-7-yloxy]acetic acid [J] . Harada H, Hirokawa Y, Suzuki K, Chemical and Pharmaceutical Bulletin . 2005,第2期

机译：发现新型和有效的人类和大鼠β（3）-肾上腺素能受体激动剂，[3-[（2R）-[[（2R）-（3-氯苯基）-2-羟乙基]氨基]丙基] -1H-吲哚-7-酰氧基]乙酸
4. Selective Agonists for the Human Vasopressin V_(1b) Receptor are Potent Antidiuretic Agonists in the Rat [C] . Stoytcho B. Stoev, LingLing Cheng, Maurice Manning American Peptide Symposium . 2006

机译：用于人血管加压素V_（1B）受体的选择性激动剂是大鼠有效的抗硫酸激动剂
5. The role of beta3-adrenergic receptors in control of brown and white adipose tissues and of energy balance: Reversal of obesity by CL 316,243, a new beta3-adrenergic agonist. [D] . Ghorbani, Masoud. 1998

机译：β3肾上腺素受体在控制棕色和白色脂肪组织以及能量平衡中的作用：一种新型的β3肾上腺素激动剂CL 316,243逆转肥胖。
6. Site-directed mutagenesis of human beta-adrenergic receptors: substitution of aspartic acid-130 by asparagine produces a receptor with high-affinity agonist binding that is uncoupled from adenylate cyclase. [O] . C M Fraser, F Z Chung, C D Wang, 1988

机译：人β-肾上腺素受体的定点诱变：天冬酰胺取代天冬氨酸130产生具有高亲和力激动剂结合的受体该受体与腺苷酸环化酶脱钩。
7. Discovery of a Novel and Potent Human and Rat .BETA.3-Adrenergic Receptor Agonist, 3-(2R)-(2R)-(3-Chlorophenyl)-2-hydroxyethylaminopropyl-1H-indol-7-yloxyacetic Acid [O] . Hiroshi Harada, Yoshimi Hirokawa, Kenji Suzuki, 2005

机译：发现一种新颖和有效的人和大鼠.Beta.3-肾上腺素能受体激动剂，3 - （2R） - （2R） - （3-氯苯基）-2-羟乙基氨基 -1H- Indol -7-基氧基乙酸
8. Regulation of Postnatal beta-Adrenergic Receptor/Adenylate Cyclase Development byPrenatal Agonist Stimulation and Steroids: Alterations in Rat Kidney and Lung after Exposure to Terbutaline or Dexamethasone [R] . Kudlacz, E. M., Navarro, H. A., Kavlock, R. J., 1990

机译：通过激动剂刺激和类固醇调节出生后β-肾上腺素能受体/腺苷酸环化酶的发生：接触特布他林或地塞米松后大鼠肾和肺的改变

Novel and potent human and rat beta(3)-Adrenergic receptor agonists containing substituted 3-indolylalkylamines.

摘要

著录项

相似文献

相关主题

期刊订阅