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Synthesis and pharmacological activity of fluorescent histamine H-2 receptor antagonists related to potentidine
Li, LT; Kracht, J; Peng, SQ; Bernhardt, G; Elz, S; Buschauer, A
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2003-05-19
DOI10.1016/S0960-894X(03)00235-X
13期:10页:1717-1720
收录类别ISTP ; SCI
文章类型Proceedings Paper
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]LIGANDS
英文摘要

Fluorescently labeled histamine H-2 receptor antagonists were synthesized starting from N-cyano-N′-[3-(3-piperidin-1-ylmethylphenoxy)propyl]guanidines with an additional N"-omega-aminoalkyl substituent (chain lengths 2-8 methylene groups) or from 3-(3-piperidin-1-ylmethylphenoxy)propylamine. The primary amino group was derivatized with various fluorophores (fluorescein, acridine, dansyl, nitrobenzoxadiazole (NBD), indolo[2,3-a]quinolizine). On the isolated spontaneously beating guinea pig right atrium most of the fluorescent probes were only weakly active, however, the NBD-labeled substances proved to be potent histamine H-2 receptor antagonists achieving pA(2) values in the range of 7.5-8.0, comparable to the activity of famotidine. (C) 2003 Elsevier Science Ltd. All rights reserved.

语种英语
WOS记录号WOS:000182913600023
引用统计
被引频次:16[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/60560
专题北京大学药学院
作者单位1.Univ Regensburg, Inst Pharm, D-93040 Regensburg, Germany
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
推荐引用方式
GB/T 7714
Li, LT,Kracht, J,Peng, SQ,et al. Synthesis and pharmacological activity of fluorescent histamine H-2 receptor antagonists related to potentidine[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2003,13(10):1717-1720.
APA Li, LT,Kracht, J,Peng, SQ,Bernhardt, G,Elz, S,&Buschauer, A.(2003).Synthesis and pharmacological activity of fluorescent histamine H-2 receptor antagonists related to potentidine.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,13(10),1717-1720.
MLA Li, LT,et al."Synthesis and pharmacological activity of fluorescent histamine H-2 receptor antagonists related to potentidine".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 13.10(2003):1717-1720.
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