A(1) adenosine receptor agonists: medicinal chemistry and therapeutic potential.
Adenosine receptors are widely distributed in the body and modulate numerous physiological processes. Four receptor subtypes (termed A(1), A(2A), A(2B) and A(3)) have been identified based on their pharmacological profile and cloning. Activation of the A(1) adenosine receptors produces a number of effects including a reduction in heart rate and atrial contractility, the attenuation of the stimulatory actions of catecholamines on the heart as well as a reduction of lipolysis in adipose tissue. As a result, A(1)AR agonists have been targeted as anti-arrhythmic and cardioprotective agents. This review discusses the synthesis, structure-activity relationships and therapeutic potential of A(1)AR agonists.
Department of Medicinal Chemistry, Victorian College of Pharmacy, Monash University, 381 Royal Parade, Parkville VIC 3052, Australia.
S A
SA
Hutchinson
P J
PJ
Scammells
D000241:Adenosine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D058907:Adenosine A1 Receptor Agonists; D018712:Analgesics, Non-Narcotic / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000737:chemistry / Q000494:pharmacology; D002316:Cardiotonic Agents / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D018696:Neuroprotective Agents / Q000737:chemistry / Q000494:pharmacology; D043682:Receptor, Adenosine A1 / Q000737:chemistry / Q000502:physiology; D013329:Structure-Activity Relationship
D058907:Adenosine A1 Receptor Agonists; D018712:Analgesics, Non-Narcotic; D000889:Anti-Arrhythmia Agents; D002316:Cardiotonic Agents; D018696:Neuroprotective Agents; D043682:Receptor, Adenosine A1; D000241:Adenosine