International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update

PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity

“…Thawed membranes containing 30 μg CHO-hA 1 IC 50 values of PQ-69 or DPCPX were determined using the method described by Cheng and Prusoff [13]. K i values were calculated using the equation…”

“…Upon activation, A 1 and A 3 AR may inhibit adenylyl cyclase, which results in a decrease in cyclic AMP level and stimulates phospholipase C and phospholipase D via G i/o protein, whereas the A 2A and A 2B ARs are stimulatory to adenylyl cyclase via G s protein. Adenosine A1 receptor (A 1 AR) activation can also activate several types of K + channels and mitogen-activated protein kinases (MAPK) via β,γ-subunits released from G i/o proteins, and also inhibits N-type Ca 2+ currents via PTX-sensitive pathways [1]. A 1 ARs are expressed in large numbers in the brain, as well as in peripheral tissues including kidney, heart and liver [2].…”

Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

“…The A 3 AR is one of four subtypes among a G protein-coupled receptor (GPCR) family (A 1 , A 2A , A 2B and A 3 ) that responds to extracellular adenosine [15]. Adenosine levels are significantly increased during ischemic stress, thereby activating ARs near the site of injury [16-18].…”

Purinergic signalling-evoked intracellular Ca2+ concentration changes in the regulation of chondrogenesis and skeletal muscle formation

“…The former are now referred to as adenosine receptors, with four members of the family (A 1 , A 2A , A 2B , and A 3 ) [7,8] identified and characterised. All adenosine receptors belong to the large superfamily of G-protein coupled receptors (GPCRs) and affect the intracellular production of cyclic AMP (cAMP) or inositol 1,4,5-trisphosphate (IP 3 ).…”