Cutamesine (SA-4503; AGY-94806) is a selective and potent sigma-1 (σ1) receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes, 100-fold less selective for the sigma 2 receptor.

Vesamicol hydrochloride, (+/-)- [(±)-AH-5183] is a novel and potent inhibitor of acetylcholine transport with a Ki of 2 nM.

E-52862, also known as S1RA, is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. In preclinical studies, S1RA has demonstrated efficacy in relieving neuropathic pain and pain in […]

BD-1063 HCl (BD1063 hydrochloride) is a novel, potent and selective sigma receptor antagonist with the potential for treating alcoholism.

Formerly known as Lu-28-179, siramesine HCl is a potent and selective sigma-2 receptor agonist with anticancer effects.

4-IBP is a novel and selective σ1 (sigma1) agonist with high affinity for the σ1 receptor with Ki of 1.7 nM and a moderate affinity for the σ2 receptor (Ki = 25.2 nM).