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
Receptor Data

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

Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
P2X and P2Y Receptors

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.

Asthma

Asthma Poster

Asthma is one of the most common chronic diseases in the world, affecting over 300 million people. This poster highlights key pathways and new therapies used to treat the condition, including those currently in clinical development.

Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

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.