Adenosine Receptor Antagonist

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.

ASP5854 is an orally active, blood-brain barrier permeable adenosine A1/A2a dual receptor antagonist. ASP5854 blocks receptor activity and agonist-induced intracellular calcium elevation, and exhibits the characteristic of slow dissociation from striatal A2a receptors in primates. ASP5854 reverses catalepsy, enhances cognitive ability, improves motor function and exerts neuroprotective effects, while also alleviating dyskinesia and increasing contralateral turning behavior. ASP5854 is mainly used in studies related to ischemic stroke and Parkinson's disease.

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.

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.

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.

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.

MRS1220, a highly potent and selective human A3 adenosine receptor (hA3AR) antagonist with a K_i of 0.59 nM, has therapeutic potential for the research of diseases of the central nervous system. MRS1220 reduces glioblastoma tumor size and blood vessel formation in vivo.

Inupadenant is an orally active, highly selective A_2A receptor antagonist. Inupadenant can not cross BBB. Inupadenant can enhance the humoral immune response and has anti-tumor activity.

Alloxazine is a selective A_2b antagonist. Alloxazine 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.

GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (K_i=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.

Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.

Tozadenant is an adenosine A_2A receptor antagonist, with K_i of 11.5 nM on human A_2A and 6 nM on rhesus A_2A.

Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice.