TRPM8 antagonist 4 is a compound with high functional selectivity and favorable physicochemical properties, serving as a CB2R partial agonist (EC50=54.2 µM, Ki=3.2 µM) and a TRPM8 (IC50=42.3 nM) antagonist. It possesses notable anti-inflammatory and analgesic effects, demonstrating good safety by reducing the mRNA expression of TNF-alpha, IL-6, and IL-1beta.
