Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.
Silicon-based microphysiometry, measuring extracellular acidification rate of cells in culture, demonstrated that a series of diimidazo[1,2-c:4',5'-e]pyrimidines were agonists at the human adenosine A1 receptor. 5-amino-7,8-dihydro-3-ribofuranose-8-(R)-(phenyl)-3H-diimidazo [1,2-c:4',5'-e]pyrimidine (2a) had an EC50 of 100 microM and reached 90% of the Emax produced by R-PIA.
Camp
D
D
Queensland Pharmaceutical Research Institute, Griffith University, Brisbane, Australia.
Green
J M
JM
Kaiser
S M
SM
Moni
R W
RW
Townsend-Nicholson
A
A
Schofield
P R
PR
Quinn
R J
RJ
D000818:Animals; D001921:Brain / Q000378:metabolism; D002478:Cells, Cultured; D003342:Corpus Striatum / Q000378:metabolism; D006801:Humans; D008832:Microchemistry / Q000379:methods; D008956:Models, Chemical; D010660:Phenylisopropyladenosine / Q000031:analogs & derivatives* / Q000378:metabolism; D058906:Purinergic P1 Receptor Agonists; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D012825:Silicon
D058906:Purinergic P1 Receptor Agonists; D011743:Pyrimidines; D018047:Receptors, Purinergic P1; D010660:Phenylisopropyladenosine; D012825:Silicon