Given the relevance of AR ligands as possible therapeutic tools for cardiovascular conditions, we explored a selection of promising synthetic small-molecule agents (developed from 2000 to date), namely, RPR749 [172], LJ-1888 [173,174], IB-MECA [175], GS-9667 [176], LassBio-294 [177], cyclopentyladenosine (CPA) [178], and PSB-15826 [179] (see structures in Table 3), in order to highlight novel treatment opportunities in the context of IHD. This evidence concerns the gene AR and myocardial ischemia.