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学科主题: 药学
题名:
Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: Analogues of the quinazoline-type anti-obesity Y-5 antagonist CGP 71683A
作者: Li, LT; Mayer, M; Schneider, E; Schreiber, E; Bernhardt, G; Peng, SQ; Buschauer, A
关键词: neuropeptide Y ; Y-5 receptor antagonist ; fluorescence labelling ; quinazoline ; CGP 71683A
刊名: ARCHIV DER PHARMAZIE
发表日期: 2003-12-01
DOI: 10.1002/ardp.200300813
卷: 336, 期:12, 页:585-590
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: PHARMACOLOGICAL-ACTIVITY ; FOOD-INTAKE ; NPY Y-1 ; CELLS ; INTERNALIZATION
英文摘要:

Aspartof a programme to develop fluorescence-based methods for the study of the interactions between G-protein coupled receptors (GPCRs) and their ligands the preparation of low molecular weight fluorescence-labelled neuropeptide Y (NPY)Y-5 antagonists is reported. The naphthylsulfonyl group in the potent quinazoline-type NPYY5 receptor antagonist CGP 71683A was replaced with a dansyl, nitrobenzoxadiazole (NBD) or acridine-9-carbonyl group. In radioligand binding studies on human Y-5 receptor expressing HEC-1B cells the substances labelled with acridine (K-i 311 nM) and NBD (K-i > 1000 nM) proved to be moderately active or inactive, respectively By contrast, a K-i value of 49 nM was found for the dansyl analogue compared to 2 nM for CGP 71683A. No binding to Y-1 receptors (SK-N-MC cells, displacement of [H-3]propionyl-NPY) was detected for the new compounds at concentrations less than or equal to 1 muM.

语种: 英语
WOS记录号: WOS:000187892900005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/64077
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Univ Regensburg, Inst Pharm, D-93040 Regensburg, Germany
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Li, LT,Mayer, M,Schneider, E,et al. Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: Analogues of the quinazoline-type anti-obesity Y-5 antagonist CGP 71683A[J]. ARCHIV DER PHARMAZIE,2003,336(12):585-590.
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