Structure Activity Relationships for Adenosine Antagonists

Autor: R. F. Bruns
Rok vydání: 1990
Předmět:
Zdroj: Purines in Cellular Signaling ISBN: 9781461279969
DOI: 10.1007/978-1-4612-3400-5_21
Popis: An important milestone in adenosine research was the discovery by Sattin and Rall in 1970 that theophylline and other methylxanthines could block responses to adenosine. With the availability of competitive adenosine antagonists, it was possible for the first time to investigate the role of endogenous adenosine by blocking adenosine receptors under various physiological and pathological conditions. However, although theophylline was an effective adenosine antagonist in vivo, its use as a tool was hampered by its relatively low affinity for adenosine receptors and by effects that were unrelated to adenosine, such as phosphodiesterase inhibition and release of intracellular calcium (Rall, 1982).
Databáze: OpenAIRE