Table 1

Current adenosine receptor nomenclature

ReceptorA1A2AA2BA3
Receptor Code2.1:ADO:2.1:ADO:2.1:ADO:2.1:ADO:
Previous namesRi A2a, Rs A2b, Rs
Structural information7TM; human 326 aa, P30542, chr 1q32.1, rat 326 aa,P25099, mouse 326 aa7TM; human 410 aa, P29274, chr 22g11.2, rat 409 aa, P30543, mouse 409 aa, UO56727TM; human 328 aa, P29275, chr 17p11.2–12; rat 332 aa, P29276 mouse 332 aa, UO56737TM; human 318 aa, P33765, chr 1p21–13, rat 320 aa P28647 (see comments), mouse 320 aa, AF069778
Selective agonistsCPA, CCPA, CHACGS 21680, HENECA, CV-1808, CV-1674, ATL146eNoneCl-IB-MECA
Selective antagonistsDPCPX1-a8-cyclopentyl-theophylline, WRC0571selective: SCH 582611-b 1-c moderately selective: ZM241385,1-a KF 17387, CSCMRS1754,1-d enprofylline, alloxazine (historical)MRS 1220,1-eMRE 3008-F20,1-e MRS 1191; MRS 1523
Tissue functionsBradycardia; inhibition of lipolysis; reduced glomerular filtration; tubero-glomerular feedback, antinociception; reduction of sympathetic and parasympathetic activity; presynaptic inhibition; neuronal hyperpolarization; ischemic preconditioningRegulation of sensorimotor integration in basal ganglia; inhibition of platelet aggregation and polymorphonuclear leukocytes; vasodilatation, protection against ischemic damage, stimulation of sensory nerve activityRelaxation of smooth muscle in vasculature and intestine; inhibition of monocyte and macrophage function, stimulation of mast cell mediator release (some species)Enhancement of mediator release from mast cells (some species). Preconditioning (some species)
PhenotypesTissue functions above confirmed in knockout mouseTissue functions above confirmed in knockout mouseTissue functions above confirmed in knockout mouse
CommentsAlso cloned from dog,1-fcow,1-grabbit1-i 1-j Also cloned from e.g. dog,1-h guinea pig.1-k Variations in structure among humansAlternative splicing in rat can yield product with 337 aa.1-l Also cloned from sheep1-m 317 aa, rabbit1-j 320 aa

  • ↵1-a  DPCPX and ZM241385 also have nanomolar affinity for the adenosine A2B receptor.

  • ↵1-b  Dionisotti et al., 1997.

  • ↵1-c  Ongini et al., 1999.

  • ↵1-d  Kim et al., 2000.

  • ↵1-e   Li et al., 1999;Baraldi et al., 2000b.

  • ↵1-f   Libert et al., 1989,1991.

  • ↵1-g  Tucker et al., 1992.

  • ↵1-h  Maenhaut et al., 1990.

  • ↵1-i   Bhattacharya et al., 1993.

  • ↵1-j   Hill et al., 1997.

  • ↵1-k  Meng et al., 1994.

  • ↵1-l   Sajjadi et al., 1996.

  • ↵1-m Linden et al., 1993.