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σ1 receptor ligand

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 [1] .
    PD 144418
  • HY-168562
    σ1 Receptor ligand 1

    		Sigma Receptor Neurological Disease Cancer
    σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research [1].
    σ1 Receptor ligand 1
  • HY-101043
    4-PPBP maleate

    		Sigma Receptor iGluR Neurological Disease
    4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection [1] .
    4-PPBP maleate
  • 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 [1] .
    PD 144418 oxalate
  • HY-108515
    (+)-Igmesine hydrochloride

    JO1784

    		 Sigma Receptor NO Synthase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    (+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ1 receptor ligand with an IC50 of 39 nM. (+)-Igmesine hydrochloride binds σ1 receptors to activate G-proteins and modulate Ca 2+ uptake. (+)-Igmesine (hydrochloride) attenuates ischaemia-induced nitric oxide synthase activity and hyperactivity. (+)-Igmesine hydrochloride can be used for the research of duodenal ulcers, gastric ulcers, and cerebral ischaemia [1] .
    (+)-Igmesine hydrochloride
  • HY-106153B
    E-5842 citrate

    		Sigma Receptor Neurological Disease
    E-5842 citrate is a σ receptor ligand (Ki: 4 nM for σ1 receptor). E-5842 citrate increases levels of Fos in the medial prefrontal cortex and the nucleus accumbens, without affecting the levels of the protein in the striatum. E-5842 citrate can be used in the research of psychiatric disorders [1].
    E-5842 citrate
  • HY-120008
    SAS-1121

    		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 [1].
    SAS-1121
  • HY-120155
    MS-377

    		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 [1] .
    MS-377
  • HY-119196
    Caprospinol

    SP-233

    		 Amyloid-β Sigma Receptor Others
    Caprospinol (SP-233) is a steroid compound candidate based on the structure of 22R-hydroxycholesterol. It has multiple mechanisms of neuroprotection, including binding to β-amyloid protein (Aβ(42)), interacting with the mitochondrial respiratory chain, clearing Aβ(42) monomers, and acting as a σ-1 receptor ligand. It can cross the blood-brain barrier in vivo and restore cognitive impairment, and has the potential to inhibit Alzheimer's disease.
    Caprospinol
  • HY-118279
    KSCM-1

    		Sigma Receptor Neurological Disease
    KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors [1].
    KSCM-1
  • HY-120236
    KSCM-5

    		Sigma Receptor Neurological Disease
    KSCM-5 is a sigma receptor ligand with high affinity activity on sigma-1 receptor. The Ki value of KSCM-5 is about 34nM, showing significant selectivity. KSCM-5 has potential application value in compound development, especially for diseases related to sigma receptors [1].
    KSCM-5
  • HY-159997
    AD353

    		Sigma Receptor Neurological Disease
    AD353 is a selective sigma-1 receptor ligand with antiallodynic activity. AD353 exhibits high potency both in a model of Capsaicin (HY-10448)-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile [1].
    AD353
  • HY-181649
    S1R agonist 3

    		Sigma Receptor Neurological Disease
    S1R agonist 3 is a potent, selective and brain-penetrant sigma-1 receptor (S1R) agonist with a Ki of 1.5 nM. S1R agonist 3 reduces hyperlocomotion in wfs1abKO zebrafish larvae without affecting locomotion in wildtype wfs1abWT zebrafish larvae. S1R agonist 3 reverses Aβ25-35 (HY-P0128)-induced learning and memory impairments. S1R ligand 1 can be used for the research of Alzheimer’s disease [1].
    S1R agonist 3

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