a2a/a1

A2A A1 AR antagonist-1 (compound 1a) is a potent dual antagonist with Ki values of 5.58 nM and 24.2 nM for A2A and A1 AR, respectively, demonstrating potential for ischemic stroke research [1].

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.

LAS38096 is an A2B adenosine receptor antagonist (Ki : 17 nM) that is potent, selective and efficient .

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.

2-Chloroadenosine (CADO) is a metabolically stable analog of adenosine that binds to adenosine A1, A2A, and A3 receptors( Ki:300, 80, and 1,900 nM, respectively)

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.

8-Bromotheophylline (Bromotheophylline) is the active moiety of pamabrom, a mixture of 2-amino-2-methyl-propanol and bromotheophylline. From this mixture, 8-Bromotheophylline acts as a weak diuretic that has been used along with some analgesics to relieve the symptoms of premenstrual syndrome

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.

CGS 15943 is an orally bioavailable non-xanthine antagonist of the Adenosine Receptor. In transfected CHO cells, its Ki values for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM, respectively.

MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n

MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.

N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor, mimicking its action with Ki values of 2.3 nM, 790 nM, and 43 nM for human A1, A2A, and A3 receptors, respectively. CPA is used to modulate cellular signaling, neurotransmission, and other biological processes.

ATL444 is an adenosine receptor antagonist with affinity (Ki values) for rA1AR, rA2AAR, rA2BAR, and rA3AR of 7.0, 2.5, 61.8, and >1000 nM, respectively.

antagonist for the human adenosine A3 receptor

A1 adenosine receptor antagonist

adenosine A2A receptors antagonist

Vipadenant (CEB-4520)(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

JNJ-40255293 is an antagonist of adenosine A2A/A1.

Regadenoson (CVT-3146) is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.

MRS5698 is a high affinity and selective agonist of A3 adenosine receptor (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors