adenosine a2a receptor

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively.

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

RWJ-51204 is a selective adenosine A2A receptor antagonist and a partial agonist of GABA(A) receptor (IC50: 0.2-2 nM). It has neuroprotective and movement-improving effects and can be used in research related to Parkinson's disease.

Apadenoson TFA is a potent adenosine A2A receptor (A2AR) agonist that can be used to improve survival in patients infected with SARS.

ST 1535 is a potent and orally active antagonist of the A2A adenosine receptor, exhibiting antiparkinsonian activity and antitremorigenic effects, with potential for Parkinson's disease research.

Evodenoson (ATL313) is a potent and selective adenosine A2a receptor (A2aR) agonist for the treatment of eye diseases, tumors, and immune system disorders, and may be used in studies of open-angle glaucoma and blood tumors.

Sonedenoson (MRE0094) is an adenosine A(2A) receptor agonist and potential inhibitor potentially targeting SARS-CoV-2 coronavirus 2;-O-ribose methyltransferase, and may be used in the study of diabetic foot ulcers.

A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.

Amp579 TFA is a novel adenosine A1 A2a receptor agonist that induces acute and delayed preconditioning against myocardial shock in vivo.

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1 A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

Istradefylline (KW-6002)(Ki of 2.2 nM) is a selective adenosine A2A receptor (A2AR) antagonist, which is under development in Phase 3 trails. It has been used in trials studying the treatment and basic science of Drug Abuse, Sleep Disorder, Hepatic Impairment, Parkinson's Disease, and Restless Legs Syndrome, among others.

Regadenoson is an A2A adenosine receptor agonist, a coronary vasodilator commonly used in pharmacologic stress testing.

AZD4635 (HTL1071) is a new-type adenosine 2A receptor (A2AR) inhibitor(Ki=1.7 nM).

CGS 21680 is a chemical compound that acts as a selective agonist for both adenosine and its A2A receptor, demonstrating a binding affinity (K i) of 27 nM.

SCH 58261 is a potent and selective A2a adenosine receptor antagonist.The Ki =2.3 nM for rat A2a and 2 nM is for bovine A2a.

ZM-241385 is a high-affinity antagonist ligand selective for the adenosine A2A receptor.

N6-Ethyladenosine, an adenosine derivative, acts as an agonist of Adenosine receptors (hA1AR and hA3AR) with Ki values of 4.9 nM and 4.7 nM, respectively.

ANR94 is a potent, selective antagonist of the adenosine A2A receptor (AA2AR), exhibiting a K_i value of 46 nM for the human AA2AR (hAA2AR). This compound shows promise for research into Parkinson's disease. [1] [2]

Tozadenant (SYN115) is an adenosine A2A receptor antagonist(Ki of 11.5 nM and 6 nM on human and rhesus,respectively)

4-Desmethyl Istradefylline is a Istradefylline metabolite. Istradefylline is a very potent, selective, and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

Sch412348 is a potent competitive the human adenosine A2A receptor antagonist with Ki of 0.6 nM and has >1000-fold selectivity over all other adenosine receptors.

ST3932 is a ST1535 metabolite, is a adenosine A2A receptor antagonist(Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively).

ST4206 is an antagonist of adenosine A2A. For adenosine A2A receptor and adenosine A1 receptor, the Kis values are 12 nM and 197 nM , respectively.