Adenosine Receptor - Comparison of Subtypes

Comparison of Subtypes

Adenosine receptors
Receptor Gene Mechanism Effects Agonists Antagonists
A1 ADORA1 Gi/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
A2A ADORA2A Gs → 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
A2B ADORA2B Gs → cAMP↑

Also recently discovered A2B 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 Gi/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

Read more about this topic:  Adenosine Receptor

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