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RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant antagonist of relaxin family peptide 3 (RXFP3, IC50=2.36 μM). RLX-33 also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50s of 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can inhibits the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats.