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Sigma receptor

The sigma receptors σ1 and σ2 bind to ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine. They are named by pharmacological similarities, and are evolutionarily unrelated.

  • L-745870 trihydrochloride
    T22904866021-03-6
    L-745870 trihydrochloride is a highly potent and selective D4 dopamine receptor antagonist.
    • $68
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  • KSK67
    T775932566715-93-1
    KSK67 is a selective dual antagonist of sigma-2 and histamine H3 receptors with inhibitory effects on H3 receptors, sigma-1, and sigma-2 receptors, with Ki values of 3.2, 1531, and 101 nM, respectively.KSK67 can be used to study injury pain and neuropathic pain.
    • $68
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  • KB-5492 FA
    T62396L In house
    KB-5492 FA is a selective sigma receptor inhibitor with antiulcerogenic effects.CAS 번호128-52-56-8
    • $56
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  • AB21 HCl
    T77340L
    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.
    • $195
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  • PD 144418 oxalate
    T392111794760-28-3
    PD 144418 oxalate is a highly potent and selective sigma 1 (σ1) receptor ligand, displaying a Ki value of 0.08 nM for σ1 and 1377 nM for σ2. It exhibits negligible affinity for other receptors, ion channels, and enzymes. Additionally, PD 144418 oxalate demonstrates potential antipsychotic activity.
    • $58
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  • S1R agonist 2
    T72059150085-21-5In house
    S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.
    • $39
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  • Sigma-LIGAND-1
    T13510139652-01-0In house
    Sigma-LIGAND-1 is a selective Sigma Receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 has a Ki of 4000 nM at the dopamine D2 receptor.
    • $97
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  • AF-710B
    T236491235733-73-9In house
    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.
    • $333 TargetMol
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  • Sigma-1 receptor antagonist 3
    T129121639220-17-9In house
    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.
    • $98
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  • Sigma-1 receptor antagonist 2
    T129111639220-15-7In house
    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).
    • $97
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  • KB-5492 free base
    T62396113594-64-2In house
    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.
    • $30 TargetMol
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  • OPC-14523 hydrochloride
    T62711145969-31-9In house
    OPC-14523 hydrochloride (VPI 013 hydrochloride) is an orally active and potent sigma and 5-HT1A receptor agonist with antidepressant activity for the study of neurological disorders.
    • $117 TargetMol
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  • S1RA
    T1865878141-96-9
    S1RA (E-52862)(E-52862) is a potent, selective antagonist of the sigma-1 receptor (σ1R, Ki=17 nM), demonstrating significant selectivity over the sigma-2 receptor (σ2R, Ki > 1000 nM).
    • $39
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  • BD-1047 dihydrobromide
    T1740138356-21-5
    BD-1047 dihydrobromide (BD1047.2HBr) , a selective functional antagonist of sigma receptors, has antipsychotic activity in animal models predictive of efficacy in schizophrenia.
    • $31
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  • BD1063 dhydrochloride
    T7488206996-13-6
    BD1063 dhydrochloride is a potent and selective sigma 1(σ1) receptor antagonist(Ki = 9 nM).
    • $41
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  • Siramesine
    T4620147817-50-3
    Siramesine (Lu 28-179)(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.lysosome-destabilizing agent siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost
    • $207
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  • S1RA hydrochloride
    T42291265917-14-3
    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).
    • $32
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  • BD 1008 dihydrobromide
    T21788138356-09-9
    BD 1008 dihydrobromide is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM). BD 1008 dihydrobromide have high affinity for sigma1 receptors, moderate affinity for sigma2 receptors.
    • $183
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  • EST64454 hydrochloride
    T88341950569-11-5
    EST64454 hydrochloride (EST64454) is a highly soluble σ1 receptor antagonist (Ki : 22 nM),has the potential for Pain Management.
    • $135
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  • σ1 Receptor antagonist-1
    T92441204401-49-9
    σ1 Receptor antagonist-1 is a selective sigma 1 receptor antagonist.
    • $39
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  • Pre-084
    T3198138847-85-5
    Pre-084 is a high affinity, selective σ1 agonist.
    • $494
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  • AD186
    T78915
    AD186, a potent and selective S1R agonist, exhibits dissociation constants (Kis) of 2.7 nM for S1R and 27 nM for S2R. Notably, AD186 completely reverses the antiallodynic effect of BD-1063 [1].
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  • SARS-CoV-2-IN-57
    T793561265624-68-7
    SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 with an IC50 of 80 nM and demonstrates high affinity for the Sigma Receptor, exhibiting Kis of 13.6 nM (S1R) and 14.4 nM (S2R) [1].
    • $1,520
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  • Roluperidone
    T15034359625-79-9
    Roluperidone (CYR-101) is a novel cyclic amide derivative. It has high equipotent affinities for 5-HT2A and σ2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and σ2).
    • $30
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  • Cutamesine dihydrochloride
    T3597165377-44-6
    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.
    • $37
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  • 4-PPBP maleate
    T22513201216-39-9
    4-PPBP maleate is a potent σ1 receptor (ligand) agonist. 4-PPBP maleate can be considered a selective, non-competitive NR1a/2B NMDA receptor antagonist in the context of Xenopus oocytes expression. 4-PPBP maleate has neuroprotective properties.
    • $68
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  • BMY-14802
    T67739105565-56-8
    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.
    • $34
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  • Dimemorfan phosphate
    T502736304-84-4
    Dimemorfan phosphate (3,17-dimethylmorphinan) is a sigma 1 receptor agonist. Dimemorfan phosphate is used as a potent antitussive.
    • $39
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  • Sigma-1 receptor antagonist 1
    T129101639220-19-1
    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.
    • $97
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  • PD 144418
    T16445154130-99-1
    PD 144418 displays potential antipsychotic activity. PD 144418 is a high affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki: 0.08 nM and 1377 nM for σ1 and σ2 respectively). It shows devoid of any significant affinity for other receptors, ion channels, and enzymes.
    • $735
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  • Blarcamesine hydrochloride
    T4111195615-84-0
    Blarcamesine hydrochloride (AVex-73 hydrochloride) is a Sigma-1 Receptor agonist (IC50: 860 nM).
    • $38
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  • S1R agonist 1 hydrochloride
    T78086242487-82-7
    S1R Agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist, displaying K i values of 0.93 nM for S1R and 72 nM for S2R, and has demonstrated neuroprotective effects against ROS and NMDA-induced neurotoxicity [1].
    • $48
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  • Ditolylguanidine
    T596997-39-2
    Ditolylguanidine (Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).
    • $41
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  • Amitriptyline hydrochloride
    T0678549-18-8
    Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.
    • $45
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  • Sigma-1 receptor antagonist 4
    T74813
    Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances morphine's analgesic effects and reverses morphine-induced analgesic tolerance, potentially preventing morphine tolerance [1].
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  • NE-100 hydrochloride
    T20797149409-57-4
    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.
    • $38
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  • 4-IBP
    T4596155798-08-6
    4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .
    • $41
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  • S1R agonist 2 hydrochloride
    T78087
    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].
    • $97
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  • Sigma-1 receptor antagonist 5
    T78734
    Sigma-1 receptor antagonist 5 (compound 12), a 4-pyridylpiperidine derivative, exhibits analgesic properties through its antagonistic action on sigma receptors (Ki=4.5 nM (σ1R), 10 nM (σ2R)) and the histamine H3 receptor (hH3R, Ki=7.7 nM, IC50=215 nM). It effectively attenuates Capsaicin-induced nociception and demonstrates significant antinociceptive effects in both nociceptive and neuropathic pain models [1].
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  • AB21 oxalate
    T78916
    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].
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  • WLB-89462
    T796662849471-75-4
    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].
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  • Glycerol phenylbutyrate
    T15393611168-24-2
    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).
    • $39
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  • Siramesine hydrochloride
    T1885224177-60-0
    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.
    • $55
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  • PRE-084 hydrochloride
    T3198L75136-54-8
    PRE-084 hydrochloride is a selective agonist of σ1(IC50:44 nM, in the sigma receptor assay).
    • $37
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  • Blonanserin
    T1180132810-10-7
    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.
    • $31
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  • BMY-14802 hydrochloride
    T22612105565-55-7
    BMY-14802 hydrochloride (BMS 181100 hydrochloride) is a selective antagonist of σ receptor (IC50 = 112 nM) with antipsychotic effects. BMY-14802 hydrochloride is an agonist of the α1-adrenergic receptor and 5-HT1A.
    • $30
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  • Amitriptyline
    T2224050-48-6
    Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.
    • $39
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