Adenosine Receptor Antagonist

ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM.

8-(p-Sulfophenyl)theophylline (8-SPT) (compound 2) is an adenosine A2B receptor antagonist, with a K_i of 1330 nM for A2B human recombinant.

INCB106385 is an orally active A₂A/A₂B adenosine receptor antagonist, with an IC₅₀ value of 4.4 nM for cAMP inhibition at the A₂A adenosine receptor and an IC₅₀ value of 6.4 nM for cAMP inhibition at the A₂B adenosine receptor. INCB106385 inhibits the pCREB signaling pathway in immune cells, blocks adenosine-mediated immunosuppression in the tumor microenvironment, and induces tumor regression. INCB106385 exhibits efficacy as a monotherapy or in combination with anti-PD-1 antibodies in colon cancer models. INCB106385 can be used for the research of colon cancer.

SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC₅₀ of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.

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

DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a K_i of 0.46 nM in ³H-CHA binding to A1 receptors in rat whole brain membranes.

PSB-603 is a potent and highly selective A_2B adenosine receptor antagonist exhibiting a K_i value of 0.553 nM and virtually no affinity for the human and rat A₁ and A_2A and the human A₃ receptors up to a concentration of 10 μM.

Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.

Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities.

MRS 1754 is a selective antagonist radioligand for A_2B adenosine receptor with very low affinity for A₁ and A₃ receptors of both humans and rats.

CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its K_i for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a K_i of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.

MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i values of 18.9 nM and 113 nM for human and rat A₃ receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A₁ and A_2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.

Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research.

Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator agent and has the potential for chronic bronchitis and emphysema.

SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A_2A receptor (A_2AR), with K_is of 0.048 and 0.5 nM for human and rat A_2AR respectively. SCH442416 displays more than 23000-fold selectivity over A₁R, A_2BR, and A₃R (K_i=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A_2A receptors in rat and primate brain.

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).

7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity.

Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a K_i of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.

Derenofylline (SLV 320) is a potent, selective and orally active adenosine A₁ receptor antagonist, with K_i values of 1 nM, 200 nM and 398 nM for human A₁, A₃ and A_2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.