AB21 hydrochloride is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 hydrochloride has the effect of reducing mechanical hypersensitivity.
AB21 hydrochloride shows Kis of 12 nM and 14 nM with or without Phenytoin in the S1R Radioligand Binding Assay[1].
AB21 hydrochloride (20 mg/kg, s.c., administered 30 min before the injection of Capsaicin ) reverses mechanical allodyniain in Capsaicin -induced pain model, and exhibits higher potency than BD1063 dhydrochloride [1].
References:
[1]. Dichiara M, et al. Synthesis, Computational Insights, and Evaluation of Novel Sigma Receptors Ligands. ACS Chem Neurosci. 2023 May 17;14(10):1845-1858.