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Published in final edited form as: Pharmacol Rev. 2001 Dec;53(4):527–552.

TABLE 1.

Current adenosine receptor nomenclature

Receptor	A₁	A_2A	A_2B	A₃
Receptor Code	2.1:ADO:	2.1:ADO:	2.1:ADO:	2.1:ADO:
Previous names	R_i	A_2a, R_s	A_2b, R_s
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	DPCPX^a 8-cyclopentyl-theophylline, WRC0571	selective: SCH 58261^b,c moderately selective: ZM241385,^a KF 17387, CSC	MRS1754,^d enprofylline, alloxazine (historical)	MRS 1220,^e MRE 3008-F20,^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 plateletaggregation 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,^f cow,^g rabbit^i,j	Also cloned from e.g. dog,^h guinea pig.^k Variations in structure among humans		Alternative splicing in rat can yield product with 337 aa.^l Also cloned from sheep^m 317 aa, rabbit^j 320 aa

^a

DPCPX and ZM241385 also have nanomolar affinity for the adenosine A_2B receptor.

^b

Dionisotti et al., 1997.

^c

Ongini et al., 1999.

^d

Kim et al., 2000.

^e

Li et al., 1999; Baraldi et al., 2000b.

^f

Libert et al., 1989, 1991.

^g

Tucker et al., 1992.

^h

Maenhaut et al., 1990.

ⁱ

Bhattacharya et al., 1993.

^j

Hill et al., 1997.

^k

Meng et al., 1994.

^l

Sajjadi et al., 1996.

^m

Linden et al., 1993.