Sigma Receptor Antagonist

Sigma Receptor Antagonists (39):

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 K_i 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 K_i 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 K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >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-18101A

BD1063 dhydrochloride	Antagonist	≥98.0%
BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.

HY-13575

Blonanserin	Antagonist	99.62%
Blonanserin (AD-5423) is a potent?and orally active 5-HT_2A?(K_i=0.812 nM) and?dopamine D2?receptor?(K_i=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-10815

σ1 Receptor antagonist-1	Antagonist	99.70%
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pK_i=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 K_is of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT_2B receptor (K_i= 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 pK_i 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 K_i 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 (K_i = 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 K_is of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity.

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 K_i 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 K_is 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.

HY-124462

Trifluperidol hydrochloride	Antagonist	99.4%
Trifluperidol hydrochloride is a Sigma-1 receptor antagonist with a K_i value of 3.3 nM. Trifluperidol hydrochloride is used in the study of psychosis.

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