A 1 adenosine receptor agonists, antagonists, and allosteric modulators

Zhan Guo Gao, Dilip K. Tosh, Shanu Jain, Jinha Yu, Rama R. Suresh, Kenneth A. Jacobson

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


One of the four G protein-coupled receptors for adenosine, the A 1 adenosine receptors (A 1 AR), is widely distributed in the body and modulates numerous normal and pathological processes, through signaling pathways including those downstream from its coupled G i protein. It is an attractive drug target for heart failure, arrhythmias, angina, asthma, stroke, seizure, pain, depression, and diabetes. In this chapter, we describe the A 1 AR structure, function, signaling pathways, and therapeutic applications. We detail numerous structure-activity features of A 1 AR agonists, antagonists, and allosteric modulators, introduced as pharmacological tools and molecules for clinical development.

Original languageEnglish
Pages (from-to)59-89
Number of pages31
StatePublished - 2018

Bibliographical note

Publisher Copyright:
© Springer Nature Switzerland AG 2018.


  • A adenosine receptors
  • A AR agonists and antagonists
  • A AR allosteric modulators
  • A AR structural characterization
  • Structure-activity relationships


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