Adenosine Receptor - Comparison of Subtypes

Comparison of Subtypes

Adenosine receptors
Receptor	Gene	Mechanism	Effects	Agonists	Antagonists
A₁	ADORA1	G_i/o → cAMP↑/↓ Inhibition ↓ vesicle release Bronchoconstriction	decrease heart rate	N6-Cyclopentyladenosine Adenosine CCPA 2'-MeCCPA GR 79236 SDZ WAG 994	Caffeine theophylline 8-Cyclopentyl-1,3-dimethylxanthine (CPX) 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) 8-Phenyl-1,3-dipropylxanthine PSB 36
A_2A	ADORA2A	G_s → cAMP↑	coronary artery vasodilatation Decreased dopaminergic activity in CNS	ATL-146e CGS-21680 Regadenoson Adenosine	Caffeine theophylline istradefylline SCH-58261 SCH-442,416 ZM-241,385
A_2B	ADORA2B	G_s → cAMP↑ Also recently discovered A_2B has Gq → DAG and IP3 → Release calcium → activate calmodulin → activate myosin light chain kinase → phosphrylate myosin light chain → myosin light chain plus actin → bronchoconstriction	bronchospasm	5'-N-ethylcarboxamidoadenosine BAY 60–6583 Adenosine LUF-5835 LUF-5845	theophylline Caffeine CVT-6883 MRS-1706 MRS-1754 PSB-603 PSB-0788 PSB-1115
A₃	ADORA3	G_i/o → ↓cAMP	Cardiac muscle relaxation Smooth muscle contraction cardioprotective in cardiac ischemia inhibition of neutrophil degranulation	2-(1-Hexynyl)-N-methyladenosine CF-101 (IB-MECA) Adenosine 2-Cl-IB-MECA CP-532,903 MRS-3558	theophylline Caffeine MRS-1191 MRS-1220 MRS-1334 MRS-1523 MRS-3777 MRE3008F20 PSB-10 PSB-11 VUF-5574

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