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Sigma-receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Sigma Receptor (30) 5-HT Receptor (4) Adrenergic Receptor (2) Antibiotic (1) Apoptosis (2) Bacterial (1) Dopamine Receptor (2) Dopamine Transporter (1) Drug Intermediate (1) Endogenous Metabolite (1) Fungal (1) Histamine Receptor (2) iGluR (1) mAChR (2) Potassium Channel (1) Proteasome (1) SARS-CoV (1)
By Research Areas:	Cancer (4) Infection (2) Inflammation/Immunology (2) Neurological Disease (23)

Targets Recommended: Sigma Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100966

BD-1008 dihydrobromide	Sigma Receptor	Neurological Disease
BD-1008 dihydrobromide is an antagonist of *sigma Receptor* .

HY-108515

(+)-Igmesine hydrochloride JO1784	Sigma Receptor	Neurological Disease
(+)-Igmesine hydrochloride (JO1784) is an orally active and selective *σ receptor* ligand with neuroprotective and anti-amnesic activities .

HY-19120

KB-5492 anhydrous	Sigma Receptor	Inflammation/Immunology
KB-5492 anhydrous 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 anhydrous is an anti-ulcer agent .

HY-47228

KB-5492 free base	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 .

HY-136280

Panamesine 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 .

HY-173475

CM699	Sigma Receptor Dopamine Transporter	Neurological Disease
CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC₅₀s of 311 and 14.1 nM, respectively .

HY-120360

CB-64D	Sigma Receptor Apoptosis	Cancer
CB-64D is the agonist for sigma receptor 2 and sigma receptor 1 with K_i of 16.5 and 3063 nM. CB-64D induces apoptosis in cancer cell SK-N-SH .

HY-130179

RC-33 hydrochloride	Apoptosis	Neurological Disease
RC-33 hydrochloride is a selective and metabolically stable σ receptor agonist with activity in enhancing nerve growth factor (NGF)-induced neurite outgrowth. Both enantiomers of RC-33 hydrochloride bind to the σ receptor with similar affinity and show almost equal effectiveness as σ receptor agonists. The R-configured enantiomer of RC-33 hydrochloride shows higher liver metabolic stability in the presence of NADPH. RC-33 hydrochloride was selected as the best candidate for further in vivo studies in animal models of amyotrophic lateral sclerosis .

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 .

HY-121470

Vesamicol	mAChR	Others
Vesamicol is a compound used to synthesize radiolabeled derivatives that can be used as sigma receptor ligands for tumor targeting inhibition and have shown certain potential in cellular uptake, biodistribution and inhibition experiments.

HY-16996

BD-1047	Sigma Receptor	Neurological Disease
BD-1047 is a selective functional antagonist of *sigma receptors*. BD-1047 attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .

HY-16996A

BD-1047 dihydrobromide Maximum Cited Publications 7 Publications Verification	Sigma Receptor	Neurological Disease
BD-1047 dihydrobromide is a selective functional antagonist of *sigma receptors*. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .

HY-158197

RC-106	Sigma Receptor Proteasome	Cancer
RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM) .

HY-135608

BD-1008	Sigma Receptor	Others
BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.

HY-118901

Opipramol 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 K_i value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .

HY-101626A

Sigma-LIGAND-1 hydrochloride	Sigma Receptor	Neurological Disease
Sigma-LIGAND-1 hydrochloride is a selective *sigma receptor* ligand with an IC₅₀s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a K_i of 4000 nM at the dopamine D₂ receptor .

HY-118901A

Opipramol dihydrochloride Ensidon dihydrochloride; G-33040 dihydrochloride	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 K_i value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .

HY-101626

Sigma-LIGAND-1	Sigma Receptor	Neurological Disease
Sigma-LIGAND-1 is a selective *sigma receptor* ligand with an IC₅₀s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 has a K_i of 4000 nM at the dopamine D₂ receptor .

HY-117420

CM764	Sigma Receptor	Cancer
CM764 is an activator for *sigma receptor* with K_i of 86.6 and 3.5 nM for sigma-1 receptor and sigma-2 receptor. CM764 increases cytoplasmic calcium, NAD ⁺/NADH, and ATP levels, and decreases the concentration of ROS .

HY-118279

KSCM-1	Sigma Receptor	Neurological Disease
KSCM-1 is a selective **sigma-1 receptor ligand with a K_i** of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors .

HY-136281

DuP 734	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 .

HY-108510

Rimcazole dihydrochloride BW 234U dihydrochloride	Sigma Receptor Dopamine Receptor	Neurological Disease Cancer
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-108509

BMY-14802 hydrochloride BMY-14802-1; BMS 181100 hydrochloride	Sigma Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
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-118901R

Opipramol (Standard)	Sigma Receptor	Neurological Disease
Opipramol (Standard) is the analytical standard of Opipramol. This product is intended for research and analytical applications. 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-155155

SARS-CoV-2-IN-57	SARS-CoV Sigma Receptor	Infection
SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC₅₀: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively .

HY-105034

Tiospirone BMY 13859-1 free base	5-HT Receptor	Neurological Disease
Tiospirone is a 5-HT₂ receptor antagonist with affinity for D₂, 5-HT_1a, and 5-HT₇, and *sigma receptors*. Tiospirone decreases consumption of ethanol while increasing food intake of rats. Tiospirone can also reduce the reinforcing properties of Cocaine exhibited in the conditioned place preference paradigm .

HY-W714837

5-Phenyllevulinic acid 4-Oxo-5-phenylpentanoic acid; 5-Phenyl-4-oxopentanoic acid	Bacterial Fungal Antibiotic Drug Intermediate Endogenous Metabolite Sigma Receptor	Infection
5-Phenyllevulinic acid (4-Oxo-5-phenylpentanoic acid) is an endogenous fungal metabolite with inhibitory activity against the bacterium B. megaterium, the plant pathogenic fungus S. tritici, and the alga C. fusca. 5-Phenyllevulinic acid is also an intermediate in the synthesis of *σ receptor* ligands. 5-Phenyllevulinic acid holds potential for research in the field of anti-infection studies .

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 K_i* 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 .

HY-107708

threo-Ifenprodil hemitartrate	iGluR Sigma Receptor Potassium Channel	Neurological Disease
threo Ifenprodil hemitartrate is a *σ receptor* agonist, with K_is of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC₅₀=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC ₅₀ of 88 nM, showing antiarrhythmic activity .

HY-116594A

OPC-14523 hydrochloride	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 .

HY-116594

OPC-14523 free base	Sigma Receptor 5-HT Receptor	Neurological Disease
OPC-14523 free base 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 free base shows antidepressant-like activity .

HY-149335

Sigma-1 receptor antagonist 5	Sigma Receptor Histamine Receptor	Neurological Disease
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 .

HY-A0139

Thiothixene NSC 108165; Navan; Navane	Sigma Receptor mAChR Histamine Receptor Dopamine Receptor Adrenergic Receptor	Others
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

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Sigma-receptor

Inhibitors & Agonists