S1RA hydrochloride has shown efficacy in various pain models, significantly inhibiting formalin-induced nociception, capsaicin-induced mechanical hypersensitivity, and sciatic nerve injury-induced mechanical and thermal hypersensitivity in mice, across a wide dose range through both intraperitoneal and oral administration^[1].

S1RA hydrochloride distinguishes itself as a highly selective antagonist for the sigma-1 receptor (σ1R), with strong affinity indicated by Ki values of 17 nM and 23.5 nM for human and guinea pig σ1Rs, respectively. Its affinity extends to the human σ2R, albeit at a much higher Ki value of 9.3 μM, demonstrating its selectivity towards σ1R. Additionally, S1RA hydrochloride targets the human 5-HT2B receptor, with a Ki value of 328 nM and an IC50 value of 4.7 μM, indicating a moderate antagonistic activity^[1].