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

Famous quotes containing the words comparison of and/or comparison:

    “When we reflect on our past sentiments and affections, our thought is a faithful mirror, and copies its objects truly; but the colours which it employs are faint and dull, in comparison of those in which our original perceptions were clothed.”
    —David Hume (1711–1776)

    “Most parents aren’t even aware of how often they compare their children. . . . Comparisons carry the suggestion that specific conditions exist for parental love and acceptance. Thus, even when one child comes out on top in a comparison she is left feeling uneasy about the tenuousness of her position and the possibility of faring less well in the next comparison.”
    —Marianne E. Neifert (20th century)