Sigma Receptor

Cat. No.

A25969

CAS No.

75136-54-8

PRE-084 hydrochloride

PRE-084 hydrochloride is a highly selective agonist for the sigma-1 receptor (S1R), exhibiting an IC50 value of 44 nM. This compound demonstrates significant neuroprotective effects, enhancing motor function and promoting motor neuron survival in murine models. Additionally, PRE-084 hydrochloride mitigates myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS signaling pathway, making it a valuable tool for research in neurodegenerative diseases and cardiac protection.

Cat. No.

A30351

CAS No.

172907-03-8

PB28 dihydrochloride

PB28 dihydrochloride is a potent σ2 receptor agonist, exhibiting high affinity with a Ki of 0.68 nM, and also acts as a σ1 antagonist with a Ki of 0.38 nM. This compound demonstrates significant biological activity by inhibiting electrically evoked twitch responses in guinea pig bladder and ileum, with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride has been shown to modulate SARS-CoV-2-human protein-protein interactions, induce caspase-independent apoptosis, and display antitumor effects, making it a valuable tool for research in neuropharmacology and cancer biology.

Cat. No.

A30683

CAS No.

1204401-49-9

σ1 Receptor antagonist-1

σ1 Receptor antagonist-1 is a selective antagonist of the sigma 1 receptor, exhibiting a high binding affinity (pKi = 10.28). It effectively inhibits cell proliferation by inducing cell cycle arrest at the G0/G1 phase and promoting apoptosis in MCF-7/ADR cells. This compound is valuable for research applications focused on cancer biology and the mechanisms underlying resistance to chemotherapeutic agents.

Cat. No.

A32025

CAS No.

2162116-09-6

BS148

BS148 is a selective agonist for the sigma-2 receptor (S2R) with a binding affinity (Ki) of 20 nM and shows over 80-fold selectivity for S2R compared to S1R. This compound activates the endoplasmic reticulum stress response by upregulating key genes such as protein kinase R-like ER kinase (PERK), activating transcription factor 4 (ATF4), and C/EBP homologous protein (CHOP), leading to apoptosis in melanoma cells. Additionally, BS148 downregulates cholesterol-related genes and activates the MAPK signaling pathway, making it a valuable tool for melanoma research.

Cat. No.

A32189

CAS No.

172906-90-0

PB28

PB28 is a selective sigma 2 (σ2) receptor agonist, exhibiting a high affinity with a Ki value of 0.68 nM, and also acts as a σ1 antagonist (Ki = 0.38 nM). This compound demonstrates significant biological activity by inhibiting electrically evoked contractions in guinea pig bladder and ileum, with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 is also noted for its ability to modulate SARS-CoV-2-human protein interactions and induces caspase-independent apoptosis, showcasing its potential in antitumor research applications.

Cat. No.

A32580

CAS No.

157752-20-0

CB-64D

CB-64D is a dual agonist of sigma receptor 1 and sigma receptor 2, exhibiting Ki values of 16.5 nM and 3063 nM, respectively. It has been shown to induce apoptosis in SK-N-SH cancer cells, highlighting its potential role in cancer research. This compound can serve as a valuable tool for investigating the biological functions of sigma receptors and their implications in various pathologies.

Cat. No.

A33099

CAS No.

913816-12-3

SV119 hydrochloride

SV119 hydrochloride is a sigma-2 ligand with a Ki value of 5.2 nM that enhances the translocation of therapeutic agents across the plasma membrane of cancer cells. It has shown the ability to overcome the internalization barrier in pancreatic cancer, effectively maintaining the anti-tumor properties of conjugated dm-Erastin. Furthermore, SV119 hydrochloride exhibits cytotoxic effects on triple-negative breast cancer (TNBC) cells and promotes apoptosis, making it a valuable compound for cancer research and therapeutic development.

Cat. No.

A34034

CAS No.

2566715-93-1

KSK67

KSK67 is a high-affinity dual antagonist of the sigma-2 and histamine H3 receptors, exhibiting Ki values of 3.2 nM for the H3 receptor and 101 nM for the sigma-2 receptor. This compound demonstrates significant potential in the study of nociceptive and neuropathic pain pathways. KSK67's unique receptor profile makes it a valuable tool for investigating the modulation of pain-related mechanisms in various research applications.

Cat. No.

A45839

CAS No.

1265917-14-3

S1RA hydrochloride

Synonyms: E-52862 hydrochloride

S1RA hydrochloride is a selective antagonist of the sigma-1 receptor (σ1R), exhibiting a Ki value of 17 nM and demonstrating high selectivity against the σ2 receptor (Ki >1000 nM). In addition, it acts as a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride has been shown to inhibit neuropathic pain and modulate activity-induced spinal sensitization, making it a valuable tool for research in pain mechanisms and pharmacological interventions.

Cat. No.

A45989

CAS No.

105565-56-8

BMY 14802

BMY 14802 is a selective sigma-1 receptor (σ1R) antagonist that also exhibits agonistic activity at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. This compound has demonstrated the capability to inhibit abnormal involuntary movements (AIM) in rat models of Parkinson's disease, suggesting its potential in modulating motor symptoms associated with this condition. BMY 14802 serves as a valuable tool for research in neuropharmacology and the study of movement disorders.

Cat. No.

A46003

CAS No.

105565-55-7

BMY-14802 hydrochloride

Synonyms: BMY-14802-1; BMS 181100 hydrochloride

BMY-14802 hydrochloride is a selective antagonist of the sigma receptor, exhibiting an IC50 of 112 nM. It also functions as an agonist for the 5-HT1A and adrenergic α1 receptors. BMY-14802 hydrochloride demonstrates antipsychotic activity, making it a valuable tool for research in neuropharmacology and the investigation of psychiatric disorders.

Cat. No.

A54071

CAS No.

149409-57-4

NE-100 hydrochloride

NE-100 hydrochloride is a selective antagonist of the sigma-1 receptor, exhibiting an IC50 value of 4.16 nM. This compound demonstrates significant neuroprotective effects and has been shown to improve cognitive impairment, making it valuable in studies related to neurodegenerative disorders and psychiatric conditions. NE-100 hydrochloride is a useful tool for investigating the role of sigma receptors in the nervous system.

Cat. No.

A59880

CAS No.

75859-03-9

Rimcazole dihydrochloride

Synonyms: BW 234U dihydrochloride

Rimcazole dihydrochloride is a sigma (σ) receptor antagonist that plays a significant role in modulating neurotransmitter systems. This carbazole derivative also interacts with the dopamine transporter, inhibiting dopamine uptake and consequently reducing locomotor activity and sensitization. Due to its pharmacological profile, Rimcazole dihydrochloride is a valuable reagent for research applications related to neuropharmacology and cancer studies.

Cat. No.

A66171

CAS No.

1644629-60-6

SAS-0132

SAS-0132 is a selective antagonist of the Sigma 2 receptor (Sig2R) with a Ki of 90 nM, demonstrating the ability to penetrate the blood-brain barrier. This compound effectively regulates intracellular Ca2+ levels and modulates pathways related to PGRMC1. SAS-0132 exhibits neuroprotective properties and has shown promise in improving cognitive function in models of Alzheimer's disease. It serves as a valuable research tool for investigating neurocognitive disorders, particularly Alzheimer's disease.

Cat. No.

A67297

CAS No.

1312991-83-5

threo-Ifenprodil hemitartrate

threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research.

Cat. No.

A67381

CAS No.

206862-30-8

MS-377

MS-377 is a selective sigma-1 receptor ligand with an affinity (Ki = 73 nM) that demonstrates minimal interaction with the sigma-2 receptor (Ki = 6900 nM) and no significant binding to other receptors, including those for dopamine and serotonin. This compound indirectly modulates the NMDA receptor ion-channel complex, exhibiting antipsychotic activity by inhibiting PCP-induced behaviors and reducing dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 is suitable for research applications related to schizophrenia.

Cat. No.

A78406

CAS No.

4952-56-1

Caprospinol

Synonyms: SP-233

Caprospinol is a potent σ-1 receptor ligand that exhibits neuroprotective properties through multiple mechanisms. It effectively binds to β-amyloid protein (Aβ(42)), interacts with the mitochondrial respiratory chain, and facilitates the clearance of Aβ(42) monomers. Caprospinol is capable of crossing the blood-brain barrier, thereby showing promise in restoring cognitive function and inhibiting the progression of Alzheimer's disease. Its diverse biological activities make it a valuable tool for research in neurodegenerative disorders.

Cat. No.

A79262

CAS No.

401501-66-4

S1R agonist 3

S1R Agonist 3 is a highly selective sigma-1 receptor (S1R) agonist with a binding affinity (Ki) of 1.5 nM. It demonstrates the capability to reduce hyperlocomotion in wfs1abKO zebrafish larvae while leaving locomotion unaltered in wildtype wfs1abWT zebrafish. Additionally, S1R Agonist 3 effectively reverses learning and memory deficits induced by the Aβ25-35 peptide, highlighting its potential utility in Alzheimer’s disease research.

Cat. No.

A79263

CAS No.

120447-62-3

(±)-Vesamicol hydrochloride

Synonyms: (±)-AH5183 hydrochloride

(±)-Vesamicol hydrochloride is a potent inhibitor of vesicular acetylcholine transport, exhibiting a Ki value of 2 nM. Additionally, it demonstrates a high affinity for σ1 and σ2 receptors, with Ki values of 26 nM and 34 nM, respectively. This compound is valuable for research into cholinergic signaling and receptor interactions, facilitating studies on neurological disorders and synaptic transmission mechanisms.

Cat. No.

A79264

CAS No.

206996-13-6

BD1063 dhydrochloride

BD1063 dihydrochloride is a potent and selective antagonist of the sigma 1 receptor. This compound plays a significant role in modulating various neurological processes and exhibits potential neuroprotective effects. BD1063 is valuable in studies investigating neurodegenerative diseases, pain management, and the modulation of mood disorders.

Cat. No.

A79265

CAS No.

1121931-70-1

CM398

CM398 is a selective sigma-2 receptor ligand that demonstrates a high binding affinity (Ki = 0.43 nM) while maintaining a 1000-fold selectivity over the sigma-1 receptor. In addition to its primary target, CM398 exhibits appreciable affinity for dopamine (Ki = 32.90 nM) and serotonin (Ki = 244.2 nM) transporters. This compound has shown promising anti-inflammatory and analgesic properties in preclinical studies, specifically within the formalin model of inflammatory pain in mice, making it a valuable tool for research in pain management and neuropharmacology.

Cat. No.

A79266

CAS No.

154130-99-1

PD 144418

PD 144418 is a potent and selective sigma 1 (σ1) receptor ligand, exhibiting a high affinity with a Ki value of 0.08 nM for σ1 and significantly lower affinity of 1377 nM for σ2 receptors. This compound demonstrates minimal interaction with other receptors, ion channels, and enzymes, ensuring specificity in its action. PD 144418 has shown potential antipsychotic properties, making it a valuable tool for research into psychiatric disorders and sigma receptor biology.

Cat. No.

A79267

CAS No.

2849471-75-4

WLB-89462

WLB-89462 is a selective σ2 receptor ligand, exhibiting an affinity (Ki) of 13 nM. This compound demonstrates neuroprotective activity, effectively improving short-term memory impairment caused by Aβ peptide in rodent models. Additionally, WLB-89462 possesses a favorable ADMET profile, characterized by good solubility, lack of CYP inhibition, metabolic stability, high permeability, and significant brain penetration, making it a valuable tool for research in neurodegenerative diseases.

Cat. No.

A79268

CAS No.

132173-07-0

SR-31747

SR-31747 is a sigma receptor ligand that exhibits immunosuppressive and anti-inflammatory effects. This compound inhibits sterol isomerase, thereby blocking cell proliferation. SR-31747 can be utilized in research focused on immune regulation and inflammatory disorders.

Cat. No.

A79269

CAS No.

315-72-0

Opipramol

Synonyms: Ensidon; G-33040

Opipramol is a sigma (σ) receptor agonist that exhibits potent interaction with sigma recognition sites, demonstrating a Ki value of 50 nM. This atypical tricyclic antidepressant (TCA) is primarily utilized in research focused on generalized anxiety disorder (GAD). Its mechanism of action may contribute to modulating anxiety-related behaviors, making it a valuable compound for studies investigating novel therapeutic approaches in anxiety disorders.