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.

Adenosine Receptor Target Files

Related Categories

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.

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-cyclopentyl-
adenosine (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

All Ki values quoted are at human receptors unless otherwise stated. For full experimental details, including species and biological system used, please refer to the cited publications.

Quick Order

Find multiple products by catalog number

divider line

Cardiovascular Research Product Guide

Cardiovascular Research Product Guide

Our Cardiovascular Guide highlights over 250 products for cardiovascular research. Request copy or view PDF today.

divider line

Pain Research Product Guide

Pain Research Product Guide

Our Pain guide highlights over 280 products for Pain research. Request copy or view PDF today.

divider line

GPCR Product Listing

GPCR Product Listing

Highlights over 450 products for GPCRs Request copy or view PDF today.

divider line

P2 Receptors Review

Written by Kenneth Jacobson

P2X and P2Y Receptors Scientific Review

Our Purine Receptor review gives an overview of the subtypes and structures of the P2 receptor family, and the pharmacological ligands used to study them. Request copy or view PDF today.

divider line

New Therapies and Challenges in Asthma

Written by Peter J. Barnes

Asthma Life Science Poster

Our Asthma poster highlights key pathways and new therapies used to treat asthma, including those currently in clinical development. Request copy today.

divider line

Regulation of Vascular Reactivity by GPCRs

Written by J.J. Maguire and A.P. Davenport

Cardiovascular Life Science Poster

Our Cardiovascular poster highlights the key G protein-coupled receptors involved in the regulation of vascular reactivity. Request copy today.

divider line

Bio-Techne Events

IVBM 2016

IVBM 2016

October 30 - November 3, 2016

Boston, MA, USA

Booth: 2