Siramesine HCl is an agonist of sigma-2 receptor which can trigger cell death and exhibit anticancer activity.

BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.

BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.

S1RA HCl is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).

Pridopidine exhibits high affinity towards sigma 1 receptor (S1R) (Ki = 70-80 nM) which can counteract the effects of excessive or insufficient dopaminergic transmission and it can used as a dopamine (DA) stabilizer.

PD-144418 Oxalate is a novel selective sigma ligand.

Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor)[1].

σ1 agonist (IC50 = 860 nM); also displays affinity for muscarinic M1-M4 receptors (Ki values < 500 nM), but not for σ2 receptors. Exhibits neuroprotective effects, prevents tau hyperphosphorylation, and attenuates scopolamine- and (+)-MK 801-induced learning deficits in a mouse model of amyloid toxicity.

PRE-084 HCl is a high affinity, selective σ1 agonist, has an IC50 of 44 nM in the sigma receptor assay.

Progesterone is an agonist of the nuclear progesterone receptor (nPR)(Kd = 1 nM) and an antagonist of the σ1 receptor. It is involved in many physiological processes such as embryogenesis.

S1RA is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).