Effector coupling of stably transfected human A3 adenosine receptors in CHO cells

被引：36

作者：

Englert, M ^{[1
]}

Quitterer, U ^{[1
]}

Klotz, KN ^{[1
]}

机构：

[1] Univ Wurzburg, Inst Pharmakol & Toxikol, D-97078 Wurzburg, Germany

来源：

BIOCHEMICAL PHARMACOLOGY | 2002年 / 64卷 / 01期

关键词：

adenosine; adenosine receptor; A(3) effector coupling; Ca2+ signal; second messenger;

D O I：

10.1016/S0006-2952(02)01071-7

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

CHO cells stably transfected with adenosine receptors are widely utilized models for binding and functional studies. The effector coupling of human A(3) adenosine receptors expressed in such a cellular model was characterized. Inhibition of adenylyl cyclase via a pertussis toxin-sensitive G protein was confirmed and exhibited a pharmacological profile in accordance with agonist binding data. The agonist potency was dependent on the assay system utilized to measure cyclase inhibition. Agonists were more potent in a cell-based assay than in experiments where cyclase inhibition was measured in a membrane preparation suggesting that receptor-effector coupling might be more efficient in intact cells. In addition to the modulation of cyclase activity, stimulation of A(3) receptors elicited a Ca2+ response in CHO cells with agonist potencies corresponding to the values for the whole cell cAMP assay. The Ca2+ signal was completely eliminated by pertussis toxin treatment suggesting that it is mediated via betagamma release from a heterotrimeric G protein of the G(i/o) family. These results show that cAMP and Ca2+ signaling characteristics of the A(3) adenosine receptor are comparable to the ones found for the A(1) subtype. (C) 2002 Elsevier Science Inc. All rights reserved.

引用

页码：61 / 65

页数：5

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