Sigma Receptor

Sigma Receptor

The entire mammalian body expresses a special class of binding sites known as sigma receptors (subtypes sigma-1 and sigma-2). Although the endogenous ligand for these sites has not been discovered, N,N-dimethyltryptamine, sphingolipid-derived amines, and steroid hormones—especially progesterone—can bind with a fair amount of affinity.

The sigma-1 receptor (1R) is a chaperone protein that resides in the endoplasmic reticulum (ER) and functions as a modulator of inter-organelle signaling. Numerous biological processes, such as nociception, cancer, stroke, memory, drug addiction, cardiac activity, and Alzheimer's disease, are affected by it. Numerous human tumors have an overexpression of the sigma-2 (2R) receptor. It has been proven to be a reliable biomarker for spreading tumors.

Sigma Receptor related products

Structure Cat No. Product Name CAS No. Product Description
(±)-PPCC oxalate V84311 (±)-PPCC oxalate 1781628-91-8
4-IBP V3950 4-IBP 155798-08-6 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).
AB10 V79226 AB10 AB10 is a selective S1R antagonist.
AB21 V79240 AB21 AB21 is a potent and specific S1R antagonist (inhibitor) with Ki of 13 nM and 102 nM for S1R and S2R, respectively.
AB21oxalate V78890 AB21oxalate AB21 oxalate is a potent and specific S1R antagonist (inhibitor) with Ki of 13 nM and 102 nM for S1R and S2R, respectively.
AD186 V79439 AD186 AD186 is a potent and specific S1R agonist/activator with Ki of 2.7 and 27 nM for S1R and S2R respectively.
AF710B V85383 AF710B
Antidepressant agent 3 V80042 Antidepressant agent 3 Antidepressant agent 3 is an orally bioactive antidepressant.
Antidepressant agent 4 V77994 Antidepressant agent 4 Antidepressant agent 4 is an orally bioactive antidepressant.
BD 1047 dihydrobromide V2985 BD 1047 dihydrobromide 138356-21-5 BD1047 dihydrobromide (BD-1047) is a selective functional antagonist of sigma receptors (σ receptors) with antipsychotic activity and may be used for schizophrenia.
BD1063 HCl V4741 BD1063 HCl 206996-13-6 BD-1063 HCl (BD1063 hydrochloride) is a novel, potent and selective sigma receptor antagonist with the potential for treatingalcoholism.
Broussoflavonol F V71977 Broussoflavonol F 162558-94-3 Broussoflavonol F has xanthine oxidase inhibitory activity.
CM398 V70033 CM398 1121931-70-1 CM398 is a selective, orally bioactive sigma-2 receptor ligand (Ki=0.43 nM) with a high sigma-1/sigma -2 selectivity ratio (1000-fold).
CT-1812 V3312 CT-1812 1802632-22-9 CT1812 (Elayta) is a novel, potent andorally bioavailable allosteric antagonist of the sigma-2 receptor complex (sigma-2/PGRMC1) that prevents and displaces binding of Aβ oligomers to neurons.
Cutamesine (SA 4503; AGY 94806) V0097 Cutamesine (SA 4503; AGY 94806) 165377-43-5 Cutamesine (SA-4503; AGY-94806) is a selective and potent sigma-1 (σ1) receptor agonist with an IC50of 17.4 nM in guinea pig brain membranes, 100-fold less selective for the sigma 2 receptor.
Dimemorfan phosphate V30747 Dimemorfan phosphate 36304-84-4 Dimemorfan phosphate (Astomin; AT17; Gentus; AT-17) is a morphinan-based sigma 1 receptor agonistwith potent antitussive activity.
DuP 734 V70037 DuP 734 135135-87-4 DuP 734 is a sigma receptor antagonist.
EST64454 HCl V2275 EST64454 HCl 1950569-11-5 EST64454 HCl is a selective and orally bioactive sigma-1 receptor blocker (antagonist) with Ki of 22 nM.
EST73502 monohydrochloride V69891 EST73502 monohydrochloride 2535970-65-9 EST73502 mono HCl is a selective, orally bioactive, BBB (blood-brain barrier) permeable (penetrable) μ-opioid receptor (μ-opioid receptor/MOR) agonist and σ1 receptor (σ1R) antagonist, targeting MOR and σ1R The Kis of the effects are 64 nM and 118 nM respectively.
Eupatoriochromene V71980 Eupatoriochromene 19013-03-7 Eupatoriochromene is a benzopyran compound with inhibitory activity against xanthine oxidase (XO).
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