Ontology highlight
ABSTRACT:
SUBMITTER: Xia L
PROVIDER: S-EPMC5601358 | biostudies-literature | 2017 Sep
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20170830 17
We expanded on a series of pyrido[2,1-f]purine-2,4-dione derivatives as human adenosine A<sub>3</sub> receptor (hA<sub>3</sub>R) antagonists to determine their kinetic profiles and affinities. Many compounds showed high affinities and a diverse range of kinetic profiles. We found hA<sub>3</sub>R antagonists with very short residence time (RT) at the receptor (2.2 min for 5) and much longer RTs (e.g., 376 min for 27 or 391 min for 31). Two representative antagonists (5 and 27) were tested in [<su ...[more]