Current adenosine receptor nomenclature
Receptor | A1 | A2A | A2B | A3 |
---|---|---|---|---|
Receptor Code | 2.1:ADO: | 2.1:ADO: | 2.1:ADO: | 2.1:ADO: |
Previous names | Ri | A2a, Rs | A2b, Rs | |
Structural information | 7TM; human 326 aa, P30542, chr 1q32.1, rat 326 aa,P25099, mouse 326 aa | 7TM; human 410 aa, P29274, chr 22g11.2, rat 409 aa, P30543, mouse 409 aa, UO5672 | 7TM; human 328 aa, P29275, chr 17p11.2–12; rat 332 aa, P29276 mouse 332 aa, UO5673 | 7TM; human 318 aa, P33765, chr 1p21–13, rat 320 aa P28647 (see comments), mouse 320 aa, AF069778 |
Selective agonists | CPA, CCPA, CHA | CGS 21680, HENECA, CV-1808, CV-1674, ATL146e | None | Cl-IB-MECA |
Selective antagonists | DPCPX1-a8-cyclopentyl-theophylline, WRC0571 | selective: SCH 582611-b 1-c moderately selective: ZM241385,1-a KF 17387, CSC | MRS1754,1-d enprofylline, alloxazine (historical) | MRS 1220,1-eMRE 3008-F20,1-e MRS 1191; MRS 1523 |
Tissue functions | Bradycardia; inhibition of lipolysis; reduced glomerular filtration; tubero-glomerular feedback, antinociception; reduction of sympathetic and parasympathetic activity; presynaptic inhibition; neuronal hyperpolarization; ischemic preconditioning | Regulation of sensorimotor integration in basal ganglia; inhibition of platelet aggregation and polymorphonuclear leukocytes; vasodilatation, protection against ischemic damage, stimulation of sensory nerve activity | Relaxation 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) |
Phenotypes | Tissue functions above confirmed in knockout mouse | Tissue functions above confirmed in knockout mouse | Tissue functions above confirmed in knockout mouse | |
Comments | Also 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 humans | Alternative 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.