Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular oxidative stress, which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
Cell Cycle/DNA Damage >
Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK
Epigenetics >
AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase JAK MicroRNA PARP PKC Sirtuin Protein Arginine Deiminase
GPCR/G Protein >
5-HT Receptor Adenosine Receptor Adenylate Cyclase Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR Dopamine Receptor EBI2/GPR183 Endothelin Receptor GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR MCHR1 (GPR24) Melatonin Receptor mGluR Motilin Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor Prostaglandin Receptor Protease-Activated Receptor (PAR) Ras RGS Protein Sigma Receptor Somatostatin Receptor TSH Receptor Urotensin Receptor Vasopressin Receptor Melanocortin Receptor
Immunology/Inflammation >
Aryl Hydrocarbon Receptor CCR Complement System COX CXCR FLAP Histamine Receptor IFNAR Interleukin Related IRAK MyD88 NO Synthase NOD-like Receptor (NLR) PD-1/PD-L1 PGE synthase Salt-inducible Kinase (SIK) SPHK STING Thrombopoietin Receptor Toll-like Receptor (TLR) Arginase
JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

Tozadenant

Tozadenant is an adenosine A2A receptor antagonist, with Ki of 11.5 nM on human A2A and 6 nM on rhesus A2A.

  • CAS Number: 870070-55-6
  • MF: C19H26N4O4S
  • MW: 406.499
  • Catalog: Adenosine Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

8-(3-Chlorostyryl)caffeine

(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research[1].

  • CAS Number: 147700-11-6
  • MF: C16H15ClN4O2
  • MW: 330.76900
  • Catalog: Adenosine Receptor
  • Density: 1.36g/cm3
  • Boiling Point: 559.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 292.1ºC

Preladenant-d3

Preladenant-d3 (SCH-420814-d3) is the deuterium labeled Preladenant. Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors[1][2].

  • CAS Number: 1346599-84-5
  • MF: C25H26D3N9O3
  • MW: 506.57
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LUF6096

LUF6096, a potent allosteric enhancer of the adenosine A3 receptor, is able to allosterically enhance agonist binding. LUF6096 shows low orthosteric affinity for any of the adenosine receptors. LUF6096 shows protective effects in myocardial ischemia/reperfusion injury[1][2].

  • CAS Number: 1116652-18-6
  • MF: C22H21Cl2N3O
  • MW: 414.32800
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VCP171

VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain[1].

  • CAS Number: 1018830-99-3
  • MF: C18H12F3NOS
  • MW: 347.354
  • Catalog: Adenosine Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 507.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 260.4±30.1 °C

8-Cyclopentyl-1,3-dimethylxanthine

8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) is a selective adenosine A1 receptor antagonist with Kis of 10.9 nM and 1440 nM for A1 receptor and A2 receptor, respectively[1].

  • CAS Number: 35873-49-5
  • MF: C12H16N4O2
  • MW: 248.28100
  • Catalog: Adenosine Receptor
  • Density: 1.332g/cm3
  • Boiling Point: 513.1ºC at 760mmHg
  • Melting Point: 250-252ºC
  • Flash Point: 264.1ºC

Neladenoson dalanate

Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases[1].

  • CAS Number: 1239309-58-0
  • MF: C35H34ClN7O4S2
  • MW: 716.272
  • Catalog: Adenosine Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A2AAR/HDAC-IN-1

A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].

  • CAS Number: 2767560-51-8
  • MF: C24H21N7O2
  • MW: 439.47
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Danshenol B

Danshenol B is a diterpenoid. Danshenol B has strong aldose reductase (AR) inhibitory activity with IC50 value of 0.042μM. Danshenol B can be used for the research of diabetic related complication resulted by metabolic abnormality, such as cataracts, retinopathy, neuropathy, and nephropathy[1].

  • CAS Number: 189308-09-6
  • MF: C22H26O4
  • MW: 354.43900
  • Catalog: Adenosine Receptor
  • Density: 1.24±0.1 g/cm3
  • Boiling Point: 501.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A

Acefylline

Acefylline is an adenosine receptor antagonist.

  • CAS Number: 652-37-9
  • MF: C9H10N4O4
  • MW: 238.200
  • Catalog: Adenosine Receptor
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 555.7±56.0 °C at 760 mmHg
  • Melting Point: 270-272 °C
  • Flash Point: 289.9±31.8 °C

2-Ethyl-5,7-Dimethyl-3H-Imidazo[4,5-B]Pyridine

Adenosine receptor antagonist 4 (compound 2) is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor[1].

  • CAS Number: 133240-06-9
  • MF: C10H13N3
  • MW: 175.23
  • Catalog: Adenosine Receptor
  • Density: 1.14g/cm3
  • Boiling Point: 370.502ºC at 760 mmHg
  • Melting Point: 142-146 °C
  • Flash Point: 174.175ºC

Adenosine receptor antagonist 1

Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aRthan A2bR.

  • CAS Number: 2682930-40-9
  • MF: C22H15ClFN7O
  • MW: 447.85
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PSB11 hydrochloride

PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM)[1].

  • CAS Number: 453591-58-7
  • MF: C16H18ClN5O
  • MW: 331.800
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine receptor inhibitor 2

Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR[1].

  • CAS Number: 2550401-76-6
  • MF: C17H20BrN5O2
  • MW: 406.28
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PSB 1115

PSB-1115 is a selective A2B Adenosine Receptor antagonist. PSB-1115 inhibits the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced contraction inhibition of acetylcholine (ACh)[1].

  • CAS Number: 152529-79-8
  • MF: C14H14N4O5S
  • MW: 350.35000
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2'-MeCCPA

2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs)[1][2].

  • CAS Number: 205171-12-6
  • MF: C16H22ClN5O4
  • MW: 383.83000
  • Catalog: Adenosine Receptor
  • Density: 1.76g/cm3
  • Boiling Point: 643.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 342.9ºC

PSB-1901

PSB-1901 is a potent A2B adenosine receptor (A2BAR) antagonist with Kis of 0.0835 nM and 0.131 nM for human and mouse A2BARs respectively. PSB-1901 can be used for the research of cancer[1].

  • CAS Number: 2332835-02-4
  • MF: C24H25BrN6O4S
  • MW: 573.46
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Capadenoson

Capadenoson is a selective agonist of adenosine-A1 receptor.

  • CAS Number: 544417-40-5
  • MF: C25H18ClN5O2S2
  • MW: 520.026
  • Catalog: Adenosine Receptor
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 787.9±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 430.3±35.7 °C

Tonapofylline

Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure[1][2].

  • CAS Number: 340021-17-2
  • MF: C22H32N4O4
  • MW: 416.51400
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY 60-6583

BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model[1][5].

  • CAS Number: 910487-58-0
  • MF: C19H17N5O2S
  • MW: 379.43600
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CGS 15943

CGS 15943 is an adenosine A2 receptor antagonist and reduces stroke injury in the Mongolian gerbil[1]. CGS 15943 is a selectively p110γ inhibitor with an IC50 of 1.1 μM, shows inhibitory effect on p110δ (IC50=8.47 μM), has an anti-carcinogenic effect on HCC and PDAC cells[2].

  • CAS Number: 104615-18-1
  • MF: C13H8ClN5O
  • MW: 285.68900
  • Catalog: Adenosine Receptor
  • Density: 1.72 g/cm3
  • Boiling Point: 566.6ºC at 760 mmHg
  • Melting Point: 278-279 °C
  • Flash Point: 296.5ºC

Alloxazine;Isoalloxazine

Alloxazine is a selective A2b antagonist. Alloxazine can completely block 5’N-Ethylcarboxamido adenosine (NECA)-mediated cyclic AMP accumulation with an IC50 of 2.9 μM. Alloxazine can be used for the research of cancer[1][2].

  • CAS Number: 490-59-5
  • MF: C10H6N4O2
  • MW: 214.18000
  • Catalog: Adenosine Receptor
  • Density: 1.509g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD-4635

AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM.

  • CAS Number: 1321514-06-0
  • MF: C15H11ClFN5
  • MW: 315.73300
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

hA2A/hCA XII modulator 1

hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research[1].

  • CAS Number: 2548963-55-7
  • MF: C24H19N7O4S
  • MW: 501.52
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]pyrimidin-5-one

JNJ-40255293 is a high-affinity human A 2A receptor antagonist with a KiKi of 7.5 nM. JNJ-40255293 can be used in the research of neurodegenerative diseases such as Parkinson's disease[1].

  • CAS Number: 1147271-25-7
  • MF: C23H22N4O3
  • MW: 402.45
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-(2-((3-(tert-Butylamino)-2-hydroxypropyl)thio)thiazol-4-yl)thiophene-2-carboxamide

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases[1].

  • CAS Number: 68377-92-4
  • MF: C15H21N3O2S3
  • MW: 371.541
  • Catalog: Adenosine Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 599.8±60.0 °C at 760 mmHg
  • Melting Point: 148-149ºC
  • Flash Point: 316.6±32.9 °C

Taminadenant

Taminadenant is an antagonist of adenosine receptor[1].

  • CAS Number: 1337962-47-6
  • MF: C10H8BrN7
  • MW: 306.121
  • Catalog: Adenosine Receptor
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 574.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 301.5±32.9 °C

PD 117519

PD 117519 is an adenosine agonist.Target: Adenosine ReceptorPD 117519 is an adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.

  • CAS Number: 96392-15-3
  • MF: C19H21N5O4
  • MW: 383.40100
  • Catalog: Adenosine Receptor
  • Density: 1.71g/cm3
  • Boiling Point: 723.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 391.2ºC

Proxyphylline

Proxyphylline is a methylxanthine derivative clinical used as cardiac stimulant, vasodilator and bronchodilator.

  • CAS Number: 603-00-9
  • MF: C10H14N4O3
  • MW: 238.24300
  • Catalog: Adenosine Receptor
  • Density: 1.46 g/cm3
  • Boiling Point: 487.2ºC
  • Melting Point: 134-136ºC
  • Flash Point: 248.5ºC

Adenosine receptor inhibitor 1

Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].

  • CAS Number: 2550400-52-5
  • MF: C17H19ClFN5O3
  • MW: 395.82
  • Catalog: Adenosine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A