Sigma receptor

NE-100 hydrochloride (NE-100 HCl) is a potent and selective antagonist of σ1 (IC50 = 4.16 nM) with antipsychotic activity. NE100 HCl also suppresses ER stress-induced hippocampal cell death.

Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of Y cells and to exhibit a potent anticancer activity in vivo.

AF-710B is a specific variant of M1 muscarinic and Sigma-1 receptor agonist used in the study of neurological disorders such as Alzheimer's disease dementia and schizophrenia.

Blarcamesine hydrochloride (AVex-73 hydrochloride) is a Sigma-1 Receptor agonist (IC50: 860 nM).

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

Sigma-1 receptor antagonist 1 is an effective and selective antagonist of sigma-1 receptor. Sigma-1 receptor antagonist 1 exhibits antineuropathic pain activity and can be used in the treatment of neuropathic pain studies.

BD-1047 dihydrobromide (BD1047.2HBr) , a selective functional antagonist of sigma receptors, has antipsychotic activity in animal models predictive of efficacy in schizophrenia.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Cutamesine dihydrochloride (SA4503 dihydrochloride) is a selective σ1 receptor agonist (IC50: 17.4 nM). It shows selectivity for σ1 over σ2 receptors, and inhibits angiotensin II-induced cardiomyocyte hypertrophy in vitro and attenuates myocardial hypertrophy in vivo. In a rat model of experimental stroke, it enhances brain plasticity and sensorimotor function.

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.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.

Glycerol phenylbutyrate (HPN-100) (GPB) is a new generation ammonia scavenger drug and it also is a sigma-2 (σ2) receptor ligand (pKi: 8.02).

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

Opipramol (Ensidon) is a compound with antidepressant activity that attenuates cocaine-seeking behavior in a rat model of self-administration.Opipramol is a sigma (σ) receptor agonist with anxiolytic activity and may be used in the study of neurological disorders.

AB21 HCl is a selective antagonist of the σ1 receptor, with Kis of 13 nM for σ1 receptor and 102 nM for σ2 receptor. AB21 HCl is known for its ability to reduce mechanical hypersensitivity.

S1RA hydrochloride (E-52862 hydrochloride) is an effective and specific sigma-1 receptor(σ1R, Ki: 17 nM) antagonist, and has good selectivity against σ2R (Ki > 1000 nM).

PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand with a Ki value of 0.08 nM for σ1 and 1377 nM for σ2, exhibiting negligible affinity for other receptors, ion channels, and enzymes, and demonstrating potential antipsychotic activity.

Pentoxyverine (Carbetapentan) is an orally available cough suppressant, an antagonist of muscarinic receptor M1 and an agonist of the σ1 receptor, which causes alveolar relaxation and thus symptomatic relief.

Sigma-LIGAND-1 is a selective Sigma Receptor ligand with IC50 values of 16 nM and 19 nM at the DTG site and the PPP site, respectively, and a Ki of 4000 nM at the dopamine D2 receptor.

BD1063 dihydrochloride is a potent and selective sigma 1 (σ1) receptor antagonist (Ki = 9 nM).

Ditolylguanidine (Di-o-tolylguanidine) is an agonist of sigma receptor (σ1 σ2 receptor).

BMY-14802 (alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine butanol) is a selective and orally active sigma-1 antagonist with an IC50 of 112 nM.