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 IC 50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization
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. S1RA hydrochloride (0.1-10000 nM) shows affinity to human σ2R with K i values of 9.3 μM. S1RA hydrochloride shows affinity to human 5-HT2B receptor with a K i value of 328 nM and an IC 50 value of 4.7 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD1 mice Dosage: 32, 64, 128 and 160 mg/kg Administration: Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once Result: Reduced the permanence time on the rotating rod in rotarod test. Animal Model: Male CD1 mice with formalin-evoked nociception Dosage: 20, 40 and 80 mg/kg Administration: Intraperitoneal injection; 20, 40 and 80 mg/kg, once Result: Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice. Animal Model: Male CD1 mice with capsaicin-induced mechanical hypersensitivity Dosage: 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration) Administration: Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once Result: Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
