Abstract
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 language | English |
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Pages (from-to) | 59-89 |
Number of pages | 31 |
Journal | Receptors |
Volume | 34 |
DOIs | |
State | Published - 2018 |
Bibliographical note
Publisher Copyright:© Springer Nature Switzerland AG 2018.
Keywords
- A adenosine receptors
- A AR agonists and antagonists
- A AR allosteric modulators
- A AR structural characterization
- Structure-activity relationships