Article
ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor.
The Journal of pharmacology and experimental therapeutics - 1 Feb 2007
Li Qilan, Ye Kai, Blad Clara C, den Dulk Hans, Brouwer Jaap, Ijzerman Ad P, Beukers Margot W
Abstract excerpt
The human adenosine A(2B) receptor belongs to class A G protein-coupled receptors (GPCRs). In our previous work, constitutively active mutant (CAM) human adenosine A(2B) receptors were identified from a random mutation bank. In the current study, three known A(2B) receptor antagonists, 4-{2-[7-amino-2-(2-furyl)[1,2,4]triazolo-[2,3-a][1,3,5]triazin-5-yl-amino]ethyl}phenol (ZM241385),...
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