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5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers by Luigi Aurelio; Heidi Figler; Bernard L. Flynn; Joel Linden; Peter J. Scammells is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers about?

Two series of 5-substituted 2-amino-4-(3-trifluoromethylphenyl)thiophenes were prepared and evaluated as allosteric enhancers at the A 1 adenosine receptor (A 1 AR). In the 3-benzoyl series, a 5-phenyl group was found to confer the greatest potency (9a: ED 50 = 2.1 lM, AE score = 18%). However, the analogue with no 5-substituent (6b: ED 50 = 15.8 lM, AE score = 77%) proved to be the most efficacious. In the 3-ethoxycarbonyl series, the 5-(4-chlorophenyl) analogue was clearly the most potent and efficacious (9l: ED 50 = 6.6 lM, AE score = 57%). The antagonist activity of all compounds was measured using a [ 3 H]CPX competitive binding assay.

Who reads 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers?

Author

Luigi Aurelio; Heidi Figler; Bernard L. Flynn; Joel Linden; Peter J. Scammells

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2008

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)