Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry

D Camp; J M Green; S M Kaiser; R W Moni; A Townsend-Nicholson; P R Schofield; R J Quinn

doi:10.1016/s0960-894x(98)00102-4

Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry

Bioorg Med Chem Lett. 1998 Mar 17;8(6):691-4. doi: 10.1016/s0960-894x(98)00102-4.

Authors

D Camp¹, J M Green, S M Kaiser, R W Moni, A Townsend-Nicholson, P R Schofield, R J Quinn

Affiliation

¹ Queensland Pharmaceutical Research Institute, Griffith University, Brisbane, Australia.

PMID: 9871584
DOI: 10.1016/s0960-894x(98)00102-4

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Brain / metabolism
Cells, Cultured
Corpus Striatum / metabolism
Humans
Microchemistry / methods
Models, Chemical
Phenylisopropyladenosine / analogs & derivatives*
Phenylisopropyladenosine / metabolism
Purinergic P1 Receptor Agonists*
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology*
Rats
Receptors, Purinergic P1 / metabolism*
Silicon

Substances

Purinergic P1 Receptor Agonists
Pyrimidines
Receptors, Purinergic P1
Phenylisopropyladenosine
Silicon