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Sigma Receptor

" in MedChemExpress (MCE) Product Catalog:

180

Inhibitors & Agonists

2

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1

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8

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1

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6

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1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-111669
    Zervimesine
    1 Publications Verification

    CT1812; Sigma-2 Receptor antagonist 1

    Sigma Receptor Neurological Disease
    Zervimesine (CT1812) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. Zervimesine can be used for the research of Alzheimer’s disease .
    Zervimesine
  • HY-101864
    Blarcamesine hydrochloride
    3 Publications Verification

    Anavex 2-73

    Sigma Receptor Neurological Disease Cancer
    Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
    Blarcamesine hydrochloride
  • HY-105296
    Blarcamesine
    3 Publications Verification

    Sigma Receptor mAChR Cancer
    Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
    Blarcamesine
  • HY-118901

    Ensidon; G-33040

    Sigma Receptor Neurological Disease
    Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
    Opipramol
  • HY-14221A
    Siramesine hydrochloride
    5 Publications Verification

    Lu 28-179 hydrochloride

    Sigma Receptor Ferroptosis Cancer
    Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
    Siramesine hydrochloride
  • HY-B2087
    Glycerol phenylbutyrate
    1 Publications Verification

    HPN-100

    Sigma Receptor Cardiovascular Disease
    Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent .
    Glycerol phenylbutyrate
  • HY-18099
    S1RA
    3 Publications Verification

    E-52862

    Sigma Receptor 5-HT Receptor Neurological Disease
    S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
    S1RA
  • HY-135608

    Sigma Receptor Neurological Disease
    BD-1008 is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σreceptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor .
    BD-1008
  • HY-B1216

    Sigma Receptor Cardiovascular Disease Others Neurological Disease
    Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research .
    Oxeladin citrate
  • HY-14221
    Siramesine
    5 Publications Verification

    Lu 28-179

    Sigma Receptor Cancer
    Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
    Siramesine
  • HY-19469
    Roluperidone
    1 Publications Verification

    CYR-101; MIN-101; MT-210

    5-HT Receptor Sigma Receptor Neurological Disease
    Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
    Roluperidone
  • HY-B2215
    Dimemorfan phosphate
    3 Publications Verification

    Sigma Receptor Neurological Disease Inflammation/Immunology
    Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
    Dimemorfan phosphate
  • HY-134004

    Carbetapentane

    Sigma Receptor mAChR Neurological Disease Inflammation/Immunology
    Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
    Pentoxyverine
  • HY-18099A
    S1RA hydrochloride
    3 Publications Verification

    E-52862 hydrochloride

    Sigma Receptor 5-HT Receptor Neurological Disease
    S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
    S1RA hydrochloride
  • HY-13510
    Cutamesine dihydrochloride
    5+ Cited Publications

    SA4503 dihydrochloride; AGY94806 dihydrochloride

    Sigma Receptor Neurological Disease
    Cutamesine (SA4503) dihydrochloride is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine dihydrochloride shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine dihydrochloride has antidepressant effects .
    Cutamesine dihydrochloride
  • HY-B1813A
    (±)-Vesamicol hydrochloride
    1 Publications Verification

    (±)-AH5183 hydrochloride

    Sigma Receptor Neurological Disease
    (±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively .
    (±)-Vesamicol hydrochloride
  • HY-B1055

    Carbetapentane citrate

    Sigma Receptor mAChR Neurological Disease Inflammation/Immunology
    Pentoxyverine (Carbetapentane) citrate is an orally active and blood-brain barrier permeability sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
    Pentoxyverine citrate
  • HY-100155

    Sigma Receptor Apoptosis Autophagy Cancer
    4-IBP is a selective σreceptor agonist with high affinity for the σreceptor (Ki =1.7 nM) and moderate affinity for the σreceptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research .
    4-IBP
  • HY-14218
    Ditolylguanidine
    2 Publications Verification

    1,3-Di-o-tolylguanidine; DTG

    Sigma Receptor Neurological Disease
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer .
    Ditolylguanidine
  • HY-90002

    Sigma Receptor Neurological Disease
    4-Phenylpiperidine is a σ receptor ligand with a Ki value of 1980 nM for guinea pig σ receptors. 4-Phenylpiperidine binds to σ receptors. 4-Phenylpiperidine is used in psychiatric disease research .
    4-Phenylpiperidine
  • HY-14813
    Cutamesine
    5+ Cited Publications

    SA4503; AGY 94806

    Sigma Receptor Neurological Disease
    Cutamesine (SA4503) is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine has antidepressant effects .
    Cutamesine
  • HY-101376

    (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride

    Opioid Receptor Neurological Disease
    (+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease .
    (+)-N-Allylnormetazocine hydrochloride
  • HY-130344
    SKF 83959
    1 Publications Verification

    Dopamine Receptor Sigma Receptor Neurological Disease
    SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression .
    SKF 83959
  • HY-125821

    Sigma Receptor Neurological Disease
    Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .
    Sigma-1 receptor antagonist 1
  • HY-10815
    σ1 Receptor antagonist-1
    1 Publications Verification

    Sigma Receptor Apoptosis Neurological Disease Cancer
    σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
    σ1 Receptor antagonist-1
  • HY-108512
    PD 144418
    1 Publications Verification

    Sigma Receptor Neurological Disease
    PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity .
    PD 144418
  • HY-100985

    Sigma Receptor Cancer
    IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3 . IPAG induces apoptosis .
    IPAG
  • HY-117731

    Sigma Receptor Neurological Disease
    UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a Ki values of 1279 and 46 nM for σ1R and σ2R/TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research .
    UKH-1114
  • HY-125819

    Sigma Receptor Neurological Disease
    Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively .
    Sigma-1 receptor antagonist 2
  • HY-125820

    Sigma Receptor Potassium Channel Neurological Disease
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 has the potential for the neuropathic pain .
    Sigma-1 receptor antagonist 3
  • HY-108512A
    PD 144418 oxalate
    1 Publications Verification

    Sigma Receptor Neurological Disease
    PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity .
    PD 144418 oxalate
  • HY-124462

    R 2498

    Sigma Receptor Neurological Disease
    Trifluperidol hydrochloride is a Sigma-1 receptor antagonist with a Ki value of 3.3 nM. Trifluperidol hydrochloride is used in the study of psychosis .
    Trifluperidol hydrochloride
  • HY-116594A

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .
    OPC-14523 hydrochloride
  • HY-116463

    Sigma Receptor Neurological Disease
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity .
    E1R
  • HY-136280

    EMD 57445

    Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-N15339

    Sigma Receptor Neurological Disease
    Convolamine is an alkaloid found in Convolvulus pluricaulis and an effective positive modulator of the sigma-1 receptor (IC50 = 289 nM), exhibiting cognitive and neuroprotective properties .
    Convolamine
  • HY-B1733

    Bistrimin; Histionex

    Histamine Receptor Sigma Receptor Cytochrome P450 Neurological Disease Inflammation/Immunology
    Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM) .
    Phenyltoloxamine
  • HY-103412
    SKF 83959 hydrobromide
    1 Publications Verification

    Dopamine Receptor Sigma Receptor Neurological Disease
    SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression .
    SKF 83959 hydrobromide
  • HY-136281

    Sigma Receptor Neurological Disease
    DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics .
    DuP 734
  • HY-151562

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits high affinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research .
    AChE/BuChE/MAO-B-IN-1
  • HY-100966

    Sigma Receptor Neurological Disease
    BD-1008 dihydrobromide is a nonselective σ receptor antagonist with Kis against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (Ki = 1112 nM) and dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σreceptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .
    BD-1008 dihydrobromide
  • HY-177345

    Sigma Receptor Apoptosis Caspase Cancer
    SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer .
    SV119
  • HY-A0172

    Captodiamine

    5-HT Receptor Dopamine Receptor Sigma Receptor Neurological Disease
    Captodiame (Captodiamine) is a 5-HT2c receptor antagonist and sigma-1 and D3 dopamine receptor agonist. Captodiame shows antidepressant effect .
    Captodiame
  • HY-131914A

    Sigma Receptor Neurological Disease
    EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain .
    EST64454 hydrochloride
  • HY-153091

    Adrenergic Receptor 5-HT Receptor Sigma Receptor Neurological Disease
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .
    BMY 14802
  • HY-120155

    Sigma Receptor iGluR Neurological Disease
    MS-377 is a selective and orally active sigma-1 receptor ligand (Ki=73 nM) with weak affinity for sigma-2 receptor (Ki=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (Ki: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia .
    MS-377
  • HY-155484

    Sigma Receptor Neurological Disease
    SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research .
    SOMCL-668
  • HY-120008

    Sigma Receptor Neurological Disease
    SAS-1121 is a subtype-selective sigma 2 receptor/PGRMC1 ligand with a Ki of 16.2 nM. SAS-1121 is 574-fold selective for the signma 2 receptor over the sigma 1 receptor. SAS-1121 is a tertiary amine. SAS-1121 can be studied in neurology-related research .
    SAS-1121
  • HY-47228

    Sigma Receptor Inflammation/Immunology
    KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent .
    KB-5492 free base
  • HY-162759

    Sigma Receptor Neurological Disease
    Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing σ1R. Sigma-1 receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015) .
    Sigma-1 receptor antagonist 6

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