Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

Compound 8b hydrochloride, a selective S1R agonist, exhibits affinity with K i s of 1.1 nM for S1R and 88 nM for S2R. It demonstrates neuroprotective effects against ROS and NMDA-induced neurotoxicity [1].

AB21 oxalate, a potent and selective S1R antagonist, exhibits binding affinities (Kis) of 13 nM and 102 nM for S1R and S2R, respectively. It effectively reduces mechanical hypersensitivity [1].

WLB-89462 (Compound 20c) is a selective σ2 receptor ligand with a K i of 13 nM, exhibiting neuroprotective properties and the ability to ameliorate Aβ peptide-induced short-term memory impairment in rats. It possesses a favorable ADMET profile characterized by good solubility, absence of CYP inhibition, robust metabolic stability, high permeability, effective brain penetration, and substantial oral exposure in rodent models [1].

KB-5492 free base is an orally available and selective antiulcer agent that inhibits sigma receptors, inhibits [3H]1,3-di(2-tolyl)guanidine (DTG) binding to sigma receptors, and may be useful in the study of gastric lesions and gastric secretion.