The human GPCR family is classified into subclasses A (rhodopsin-like), B (secretin and adhesion), C (glutamate), and F (Frizzled) based on their amino acid sequences.
Class A GPCRs, a family of rhodopsin-like receptors consisting of 719 members, are further divided into several subclasses: amines, peptides, proteins, lipids, melatonin, nucleotides, steroids, saccharocarboxylic acids, sensory receptors, and orphan receptors. Indications for Class A GPCRs include pain relief, allergies, cardiovascular diseases, hypertension, and cancer.
The left curve shows Imaradenant-mediated dose-dependent inhibition of NECA-induced cAMP response with IC50 = 37.4 nM. The right curve shows Ciforadenant-mediated dose-dependent inhibition with IC50 = 23.9 nM. The data demonstrate potent antagonist activity of both compounds at ADORA2A receptor, suitable for HTS and functional testing.
The left curve shows NECA induced a dose-dependent response with EC50 = 11 nM. The right curve shows Adenosine induced a dose-dependent response with EC50 = 250 nM. The data confirm functional ADORA2A receptor activity, supporting compound screening and receptor functional characterization.
