A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
@article{Chang2005ASO, title={A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.}, author={Lisa C W Chang and Jacobien K. von Frijtag Drabbe K{\"u}nzel and Thea Mulder-Krieger and Ronald F Spanjersberg and Sophie F. Roerink and Gijs van den Hout and Margot W. Beukers and Johannes Brussee and Adriaan P. IJzerman}, journal={Journal of medicinal chemistry}, year={2005}, volume={48 6}, pages={ 2045-53 } }
Adenosine receptor agonists are usually variations of the natural ligand, adenosine. The ribose moiety in the ligand has previously been shown to be of great importance for the agonistic effects of the compound. In this paper, we present a series of nonadenosine ligands selective for the adenosine A(1) receptor with an extraordinary pharmacological profile. 2-Amino-4-benzo[1,3]dioxol-5-yl-6-(2-hydroxyethylsulfanyl)pyridine-3,5-dicarbonitrile (70, LUF 5853) shows full agonistic behavior…
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