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. 2015 Dec 9;172(24):5744–5869. doi: 10.1111/bph.13348
Nomenclature A1 receptor A2A receptor A2B receptor A3 receptor
HGNC, UniProt ADORA1, P30542 ADORA2A, P29274 ADORA2B, P29275 ADORA3, P0DMS8
Agonists cyclopentyladenosine (pK i 6.5–9.4) [388, 570, 736, 839, 870, 1592, 2141] – – –
(Sub)family‐selective agonists NECA (pK i 5.3–8.2) [570, 870, 1592, 1903, 2077] NECA (pK i 6.9–8.7) [189, 427, 570, 943, 1021, 2077] NECA (pK i 5.7–6.9) [146, 189, 862, 1113, 1798, 1945, 2077] NECA (pK i 7.5–8.4) [189, 570, 840, 1634, 1946, 2077]
Selective agonists 5‐Cl‐5‐deoxy‐(±)‐ENBA (pK i 9.3) [536], GR79236 (pK i 8.5) [839] – Rat, CCPA (pK i 7.7–8.1) [839, 1419] apadenoson (pK i 9.3) [1481], UK‐432,097 (pK i 8.3) [2065], CGS 21680 (pK i 6.7–8.1) [189, 427, 570, 839, 943, 968, 1021, 1419], regadenoson (pK i 6.5) [839] BAY 60‐6583 (pK i 8–8.5) [460] IB‐MECA (pK i 8.7–9.2) [511, 561, 968, 1946], Cl‐IB‐MECA (pK i 8–8.9) [202, 840, 941], MRS5698 (pK i 8.5) [1898]
Antagonists caffeine (pK i 4.3–5) [6, 409, 838] SCH 58261 (pK i 8.3–9.2) [427, 1021, 1445], theophylline (pK i 5.2–5.8) [427, 838, 968, 1945], caffeine (pK i 4.6–5.6) [6, 838, 1021] theophylline (pK i 4.1–5) [141, 511, 944, 1945], caffeine (pK i 4.5–5) [141, 188, 944] caffeine (pK i 4.9) [838]
(Sub)family‐selective antagonists CGS 15943 (pK i 8.5) [1445], xanthine amine congener (pK d 7.5) [536] CGS 15943 (pK i 7.7–9.4) [427, 943, 968, 1445], xanthine amine congener (pK i 8.4–9) [427, 968] xanthine amine congener (pK i 6.9–8.8) [146, 862, 863, 968, 1113, 1798], CGS 15943 (pK i 6–8.1) [65, 862, 863, 968, 1445, 1798] CGS 15943 (pK i 7–7.9) [949, 968, 1445, 1946], xanthine amine congener (pK i 7–7.4) [968, 1634, 1946]
Selective antagonists PSB36 (pK i 9.9) [6] – Rat, DPCPX (pK i 7.4–9.2) [826, 1419, 1592, 2015, 2141], derenofylline (pK i 9) [897], WRC‐0571 (pK i 8.8) [1210] SCH442416 (pK i 8.4–10.3) [1728, 1891], ZM‐241385 (pK i 8.8–9.1) [1445] PSB‐0788 (pK i 9.4) [188], PSB603 (pK i 9.3) [188], MRS1754 (pK i 8.8) [862, 948], PSB1115 (pK i 7.3) [723] MRS1220 (pK i 8.2–9.2) [840, 949, 1818, 2090], VUF5574 (pK i 8.4) [2143], MRS1523 (pK i 7.7) [1092], MRS1191 (pK i 7.5) [840, 866, 1097]
Labelled ligands [3H]CCPA (Agonist) (pK d 9.2) [968, 1592], [3H]DPCPX (Antagonist) (pK d 8.4–9.2) [388, 511, 968, 1445, 1592, 1903] [3H]ZM 241385 (Antagonist) (pK d 8.7–9.1) [36, 569], [3H]CGS 21680 (Agonist) (pK d 7.7–7.8) [852, 1976] [3H]MRS1754 (Antagonist) (pK d 8.8) [862] [125I]AB‐MECA (Agonist) (pK d 9–9.1) [1445, 1946]