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Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: Analogues of the quinazoline-type anti-obesity Y-5 antagonist CGP 71683A
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
2003-12-01
DOI10.1002/ardp.200300813
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
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被引频次:8[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/400002259/64077
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
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GB/T 7714
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.
APA Li, LT.,Mayer, M.,Schneider, E.,Schreiber, E.,Bernhardt, G.,...&Buschauer, A.(2003).Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: Analogues of the quinazoline-type anti-obesity Y-5 antagonist CGP 71683A.ARCHIV DER PHARMAZIE,336(12),585-590.
MLA Li, LT,et al."Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: Analogues of the quinazoline-type anti-obesity Y-5 antagonist CGP 71683A".ARCHIV DER PHARMAZIE 336.12(2003):585-590.
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