Adenosine A2A-R Inhibitors

Caffeine is a non-selective adenosine receptor antagonist, which includes both ADORA1 and ADORA2A receptors. It blocks the binding of adenosine to its receptors, including ADORA2A, leading to its stimulant effects.

5′-Deoxy-5′-methylthioadenosine serves as a potent modulator of the adenosine A2A receptor, characterized by its ability to induce allosteric changes in receptor conformation. This compound exhibits unique sulfur-containing moieties that facilitate specific electrostatic interactions, enhancing binding affinity. Its reaction kinetics demonstrate a rapid onset of action, with a distinctive profile of receptor desensitization, influencing intracellular signaling cascades and metabolic pathways.

Caffeine-d9 is a deuterium-labeled form of caffeine, and its mechanism of action is the same as regular caffeine. It acts as a non-selective adenosine receptor antagonist, affecting both ADORA1 and ADORA2A receptors.

PD 116,948 is a selective ADORA2A antagonist. It specifically targets and blocks the ADORA2A receptor.

ZM 241385 is a potent and selective ADORA2A receptor antagonist. It competitively binds to the ADORA2A receptor, blocking the binding of adenosine.

This compound is a non-selective adenosine receptor antagonist, including ADORA2A, similar to caffeine. It inhibits the effects of adenosine by blocking its receptors.

SCH 58261 is a highly selective A2A-R antagonist that prevents the activation of A2A receptors by adenosine.

SCH 442416 is a selective A2A-R antagonist that has shown potential in preclinical studies for various applications.

ANR 94 acts as a selective modulator of the adenosine A2A receptor, showcasing unique hydrophobic interactions that stabilize receptor-ligand complexes. Its structural features promote specific hydrogen bonding, leading to enhanced receptor activation. The compound exhibits a distinctive binding kinetics profile, characterized by a prolonged duration of action, which influences downstream signaling pathways. Additionally, its conformational flexibility allows for dynamic interactions within the receptor's active site.

XAC is a non-selective adenosine receptor antagonist, affecting both ADORA1 and ADORA2A receptors. It competitively blocks adenosine binding to its receptors.