S1RA (E-52862)(AB286948)

MW 337.4 Da, Purity >=98%. A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.