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Adenosine Receptors

Adenosine is an endogenous nucleoside that is present in all body fluids where it predominantly exhibits a cytoprotective function. Four adenosine receptors (P1 purinergic receptors) have been cloned from several mammalian species and have been classified as A1, A2A, A2B and A3.

Targets
Literature (1)
Receptor Data

Adenosine Receptor Target Files

Related Targets

Adenosine receptors are all G-protein-coupled and exhibit distinct pharmacological profiles. Due to their widespread distribution on nearly every cell type, adenosine receptors are an attractive target for pharmacological intervention.

Literature for Adenosine Receptors

Tocris offers the following scientific literature for Adenosine Receptors to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

P2X and P2Y Receptors Scientific Review

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.

Adenosine Receptor Data

Receptor Subtype A1 A2A A2B A3
Transduction Mechanism ↓Adenylyl Cyclase (Gi/o) and ↑ PLC ↑Adenylyl Cyclase (Gs) ↑Adenylyl Cyclase (Gs) and ↑ PLC (Gq) ↓Adenylyl Cyclase (Gi/o) and ↑ PLC
Primary Distribution Brain (cortex, cerebellum, hippocampus), spinal cord, eye, adrenal gland, atria Spleen, thymus, leukocytes, platelets, striatopallidal GABAergic neurons, olfactory bulb Cecum, colon, bladder Testis, mast cells
Tissue Function Antinociception, hypothermia, sedation, sleep, inhibition of lipolysis, cardio- and neuroprotection Reflex tachycardia, vasodilation, inhibition of platelet aggregation, sleep, protection against ischemia Relaxation of vascular and intestinal smooth muscle, cytokine production, inhibition of cell proliferation Mast cell degranulation, coronary vasodilation and protection from reperfusion
Key Compounds Ki Values (nM)
Agonists CGS 21680 (1063)
2-Chloro-N6-cyclopentyladenosine (1705)
2-Cl-IB-MECA (1104)
N6-Cyclopentyladenosine (1702)
HEMADO (1579)
IB-MECA (1066)
2'-MeCCPA (2281)
NECA (1691)
SDZ WAG 994 (2465)
 290
0.8
820 (rat)
2.3
327
3.7
3.3
14
23 		27
2300
470 (rat)
790
1230
2500
9580
20 - 		88800*
18800*
-
18600*
100000*
11000*
37600
2400*
25000 		67
42
0.33 (rat)
43
1.1
1.2
1150
6.2
-
Antagonists CGS 15943 (1699)
DPCPX (0439)
MRS 1220 (1217)
MRS 1334 (1385)
MRS 1706 (1584)
MRS 1754 (2752)
MRS 3777 (2403)
PSB 36 (2019)
SCH 442416 (2463)
VUF 5574 (1359)
ZM 241385 (1036)
8-(3-Chlorostyryl)caffeine (3306)
PSB 1115 (2009)
PSB 603 (3198) 		3.5
3.9
305 (rat)
> 100000 (rat)
157
403
> 10000
0.12 (rat)
1111
~ 10000 (rat)
540
28200
> 10000
> 10000 		4.2
130
52 (rat)
> 100000 (rat)
112
503
> 10000
552 (rat)
0.048
> 10000 (rat)
1.4
54
24000
> 10000 		16
50
-
-
1.39
1.97
> 10000
187
> 10000
-
31
-
53.4
0.568 		51
4000
0.7
5.69
230
570
47
2300
> 10000
4
270
-
> 10000
> 10000

* EC50 values

References

Klotz et al (2000) Naunyn-Schmied.Arch.Pharmacol. 362 382.Kim et al (1994) J.Med.Chem. 37 3614. van Muijlwijk-Koezen et al (2000) J.Med.Chem. 43 2227. Kim et al (2000) J.Med.Chem. 43 1165. Volpini et al (2002) J.Med.Chem. 45 3271. Li et al (1998) J.Med.Chem. 41 3186. Cappellacci et al (2005) J.Med.Chem. 48 1550. Osama et al (2004) J.Pharmacol.Exp.Ther. 308 358. Toddle et al (2000) J.Med.Chem. 43 4359. Jacobson and Gao (2000) Nat.Rev.Drug Discov. 5 247.