S1RA (hydrochloride)

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC₅₀ value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization^[1][2]. In Vitro:S1RA hydrochloride (0.1-10000 nM) shows high affinity to human and guinea pig σ1Rs with K_i values of 17 and 23.5 nM, respectively^[1].
S1RA hydrochloride (0.1-10000 nM) shows affinity to human σ2R with K_i values of 9.3 μM^[1].
S1RA hydrochloride shows affinity to human 5-HT2B receptor with a K_i value of 328 nM and an IC₅₀ value of 4.7 μM^[1]. In Vivo:S1RA hydrochloride (i.p. 16-80 mg/kg or oral administration 32-128 mg/kg; once) dose-dependently inhibits formalin-induced nociception, capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity of mice^[1].