[3H]-MRE 2029-F20, a selective antagonist radioligand for the human A2B adenosine receptors

被引：33

作者：

Baraldi, PG ^{[1
]}

Tabrizi, MA

Preti, D

Bovero, A

Fruttarolo, F

Romagnoli, R

Moorman, AR

Gessi, S

Merighi, S

Varani, K

Borea, PA

机构：

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Univ Ferrara, Dipartimento Med Clin & Sperimentale, Sez Farmacol, I-44100 Ferrara, Italy

[3] King Pharmaceut R&D, Cary, NC 27513 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 13期

关键词：

selective antagonist; adenosine receptors; radioligand; pharmacological characterization;

D O I：

10.1016/j.bmcl.2004.03.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

MRE 2029-F20 [N-benzo[1,3]dioxol-5-yl-2-[5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide] is a selective antagonist ligand of A(2B) adenosine receptors. For use as a radioligand, 1,3-diallyl-xanthine, the precursor of [H-3]-MRE 2029-F20, was synthesized, and tritiated on the allyl groups. [H-3]-MRE 2029-F20 bound to human A(2B) receptors expressed in CHO cells showed a K-D value of 1.65 +/- 0.10 nM and B-max value of 36 +/- 4 fmol/mg protein. [H-3]-MRE2029-F20 represents a useful tool for the pharmacological characterization of human A(2)B adenosine receptor subtype. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3607 / 3610

页数：4

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