2. Signaling Pathways
  3. Neuronal Signaling
  4. Sigma Receptor
  5. Sigma Receptor Antagonist

Sigma Receptor Antagonist

Sigma Receptor Isoform Comparison

Sigma Receptor Antagonists (40):

Cat. No. Product Name Effect Purity
  • HY-16996A
    BD-1047 dihydrobromide
    		Antagonist 98.14%
    BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
  • HY-131914
    EST64454
    		Antagonist
    EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain.
  • HY-111669
    CT1812
    		Antagonist
    CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease.
  • HY-18099A
    S1RA hydrochloride
    		Antagonist 99.94%
    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.
  • HY-13575
    Blonanserin
    		Antagonist 99.62%
    Blonanserin (AD-5423) is a potent?and orally active 5-HT2A?(Ki=0.812 nM) and?dopamine D2?receptor?(Ki =0.142?nM)?antagonist. Blonanserin is usually acts as an atypical antipsychotic?agent and can be used for the research of extrapyramidal symptoms, excessive?sedation, or?hypotension.
  • HY-18101A
    BD1063 dhydrochloride
    		Antagonist ≥98.0%
    BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.
  • HY-10815
    σ1 Receptor antagonist-1
    		Antagonist 99.70%
    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.
  • HY-101484A
    NE-100 hydrochloride
    		Antagonist ≥98.0%
    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].
  • HY-18099
    S1RA
    		Antagonist 99.43%
    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.
  • HY-108510
    Rimcazole dihydrochloride
    		Antagonist 99.96%
    Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.
  • HY-100985
    IPAG
    		Antagonist 99.84%
    IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3. IPAG induces apoptosis.
  • HY-108509
    BMY-14802 hydrochloride
    		Antagonist 98.02%
    BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.
  • HY-118901
    Opipramol
    		Antagonist 99.91%
    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).
  • HY-136281
    DuP 734
    		Antagonist 98.82%
    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.
  • HY-125821
    Sigma-1 receptor antagonist 1
    		Antagonist 98.64%
    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.
  • HY-134189A
    EST73502 monohydrochloride
    		Antagonist 99.58%
    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.
  • HY-124462
    Trifluperidol hydrochloride
    		Antagonist 99.4%
    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.
  • HY-125820
    Sigma-1 receptor antagonist 3
    		Antagonist 99.47%
    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.
  • HY-125819
    Sigma-1 receptor antagonist 2
    		Antagonist 99.14%
    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.
  • HY-153091
    BMY 14802
    		Antagonist 98.96%
    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.