Search Result
Results for "
σ1-receptor
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-10815
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Sigma Receptor
Apoptosis
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Neurological Disease
Cancer
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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 [1].
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- HY-125820
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Sigma Receptor
Potassium Channel
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Neurological Disease
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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 [1].
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- HY-125821
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Sigma Receptor
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Neurological Disease
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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 [1].
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- HY-147560
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Sigma Receptor
Opioid Receptor
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Neurological Disease
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σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain [1].
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- HY-163065
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Opioid Receptor
Sigma Receptor
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Neurological Disease
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σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models [1].
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- HY-125819
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Sigma Receptor
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Neurological Disease
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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 [1].
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- HY-149335
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Sigma Receptor
Histamine Receptor
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Neurological Disease
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Sigma-1 receptor antagonist 5 (compound 12),a 4-pyridylpiperidine derivative with analgesic activity,is an antagonist of sigma receptor (Ki=4.5 nM (σ1R),10 nM (σ2R)) and histamine H3 (hH3R,Ki=7.7 nM,IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models [1].
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- HY-149274
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Sigma Receptor
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Neurological Disease
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Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance [1].
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- HY-B2215
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- HY-18101A
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- HY-101864
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- HY-100985
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IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3 [1]. IPAG induces apoptosis .
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- HY-13510
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SA4503 dihydrochloride; AGY94806 dihydrochloride
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Sigma Receptor
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Neurological Disease
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Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
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- HY-116463
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- HY-131914A
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Sigma Receptor
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Neurological Disease
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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 [1].
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- HY-16996A
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Sigma Receptor
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Neurological Disease
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BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia [1].
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- HY-B1733
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- HY-B1216
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- HY-116586
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Sigma Receptor
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Neurological Disease
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AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease [1].
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- HY-100155
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Sigma Receptor
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Cancer
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4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).
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- HY-105296
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Sigma Receptor
mAChR
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Cancer
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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 [1].
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- HY-14813
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SA4503; AGY 94806
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Sigma Receptor
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Neurological Disease
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Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
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- HY-100930
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Sigma Receptor
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Neurological Disease
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L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research [1].
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- HY-116463D
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Sigma Receptor
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Neurological Disease
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(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders [1].
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- HY-101043
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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] .
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- HY-111081C
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Sigma Receptor
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Neurological Disease
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(±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats [1].
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- HY-101484A
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Sigma Receptor
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Neurological Disease
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NE-100 (hydrochloride) is a potent and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 (hydrochloride) exerts antipsychotic activity in vivo[1]. NE-100 (hydrochloride) also suppresses ER stress-induced hippocampal cell death[2].
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- HY-10684
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ACR16; ASP2314; FR310826
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Dopamine Receptor
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Neurological Disease
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Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
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- HY-134189
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Opioid Receptor
Sigma Receptor
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Neurological Disease
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EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity [1].
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- HY-108512
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Sigma Receptor
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Neurological Disease
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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] .
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- HY-134189A
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Sigma Receptor
Opioid Receptor
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Neurological Disease
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EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity [1].
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- HY-B1813A
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(±)-AH5183 hydrochloride
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Sigma Receptor
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Neurological Disease
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(±)-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 [1] .
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- HY-153091
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Adrenergic Receptor
5-HT Receptor
Sigma Receptor
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Neurological Disease
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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 [1] .
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- HY-108512A
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Sigma Receptor
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Neurological Disease
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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] .
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- HY-18100A
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Sigma Receptor
Akt
NO Synthase
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Cardiovascular Disease
Neurological Disease
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PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway [1] .
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- HY-116463A
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Sigma Receptor
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Neurological Disease
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(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders [1].
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- HY-116463B
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Sigma Receptor
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Neurological Disease
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(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders [1].
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- HY-116463C
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Sigma Receptor
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Neurological Disease
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(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders [1].
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- HY-18100
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Sigma Receptor
Akt
NO Synthase
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Cardiovascular Disease
Neurological Disease
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PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway [1] .
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- HY-155484
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Sigma Receptor
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Neurological Disease
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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 [1].
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- HY-134004
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Carbetapentane
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Sigma Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
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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 [1] .
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- HY-14221
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Lu 28-179
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Sigma Receptor
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Cancer
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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 [1] .
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- HY-14221A
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Lu 28-179 hydrochloride
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Sigma Receptor
Ferroptosis
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Cancer
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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 [1] .
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- HY-B1055
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Carbetapentane citrate
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Sigma Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
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Pentoxyverine (Carbetapentane) citrate 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 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 [1] .
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- HY-14221B
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LU-28-179 fumarate
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Sigma Receptor
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Cancer
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Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate 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 fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity [1] .
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- HY-18099A
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E-52862 hydrochloride
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Sigma Receptor
5-HT Receptor
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Neurological Disease
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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 [1] .
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- HY-130344
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Dopamine Receptor
Sigma Receptor
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Neurological Disease
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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 [1] .
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- HY-103412
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Dopamine Receptor
Sigma Receptor
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Neurological Disease
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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 [1] .
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- HY-18099
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S1RA
1 Publications Verification
E-52862
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Sigma Receptor
5-HT Receptor
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Neurological Disease
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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 [1] .
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- HY-151562
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Cholinesterase (ChE)
Monoamine Oxidase
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Neurological Disease
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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 [1].
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