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].

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

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.

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

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.

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.

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.

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

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.

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

adenosine A2A receptors antagonist

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

antagonist for the human adenosine A3 receptor

A1 adenosine receptor antagonist

A2B receptor antagonist 2 is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

M1069 (free base) is an orally active and selective dual antagonist for the A2A and A2B adenosine receptors, demonstrating over 100-fold selectivity compared to A1 and A3 receptors. It mitigates the immune-suppressive effects of adenosine and shows anti-tumor properties [1] [2] [3].

PSB 0777 ammonium hydrate is a potent and selective adenosine A2A receptor full agonist, with K i values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. For rat and human A1 receptors, it has significantly lower affinity, with K i values of ≥10000 nM and 541 nM, respectively. The compound exhibits poor brain penetration and is not orally absorbable. It is of interest in research related to inflammatory bowel disease (IBD) [1] [2] [3].

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor), exhibiting dual affinity towards A1 A2A ARs with higher affinity for A1- than A2A AR, and Ki values of 52.2 nM for A1 AR and 167 nM for A2A AR.

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

Potent non-nucleoside adenosine kinase inhibitor (IC50 = 1.7 nM), selective over other sites of adenosine interaction (A1, A2A and A3 receptors, adenosine transporter and adenosine deaminase). Displays oral activity in animal models of pain and inflammation.

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