Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Sigma receptor ligands bind sigma-1 and sigma-2 receptors, two unrelated proteins that are not G protein-coupled. The sigma-1 receptor was cloned in 1996 and resembles a yeast sterol isomerase more than any known mammalian receptor. It resides mainly in the endoplasmic reticulum, and its 2016 crystal structure showed a trimer with one transmembrane helix per protomer. The gene for the sigma-2 receptor was identified in 2017 as transmembrane protein 97 (TMEM97). Cutamesine (SA4503) dihydrochloride, 4-IBP and pentoxyverine citrate are sigma-1 agonists, whereas S1RA and BD-1047 2HBr are sigma-1 antagonists. Siramesine is a sigma-2 agonist, and UMB24 a sigma-2 antagonist.
Synonyms: E52862; MR390
S1RA is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.
Synonyms: BD 1047 dihydrobromide
BD-1047 2HBr is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
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 2 is a potent and selective sigma 1 receptor (??1 R) antagonist with Kis of 3.88 and 1288 nM for ??1 and ??2 receptor, respectively.
Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.
Synonyms: CYR-101; MIN-101; MT-210
Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia.
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.
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.
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.
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.
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.
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.
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.
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.
Out of stock
All 3 sizes
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.
IPAG is a potent antagonist of the sigma-1 receptor, exhibiting a pKi of 4.3. It has been shown to induce apoptosis in various cell types, making it a valuable tool for research in cancer biology and neuroprotection. Applications include the study of sigma-1 receptor signaling pathways and potential therapeutic strategies targeting these mechanisms.
DuP 734 is a selective sigma receptor antagonist that also targets the 5-HT2 receptor with high potency. It exhibits weak affinity for D2 receptors, suggesting a profile that may offer antipsychotic effects while minimizing motor side effects commonly associated with traditional neuroleptics. This compound is valuable for research in neuropharmacology and may aid in the exploration of novel treatments for psychiatric disorders.
EST64454 hydrochloride is a selective antagonist of the sigma-1 receptor, exhibiting a Ki value of 22 nM. This compound shows promise in the investigation of pain mechanisms and may facilitate new research into pain management therapies. Its oral bioavailability allows for convenient applications in preclinical studies.
Synonyms: R 2498
Trifluperidol hydrochloride is a potent Sigma-1 receptor antagonist, exhibiting a Ki value of 3.3 nM. This compound is primarily utilized in research focused on psychotic disorders, facilitating investigations into neuropharmacological mechanisms and potential therapeutic strategies. Its inhibitory action on the Sigma-1 receptor supports studies related to mood and psychotic disorders.
Sigma-1 Receptor Antagonist 1 (compound 137) is a selective antagonist of the sigma-1 receptor (σ1R), demonstrating a high binding affinity with a Ki value of 1.06 nM. This compound exhibits notable antineuropathic pain activity, making it a promising candidate for research into therapeutic interventions for neuropathic pain. Its specificity for σ1R positions it as a valuable tool in understanding the biological functions and potential clinical applications of sigma-1 receptor modulation.
BD-1008 is a potent nonselective σ receptor antagonist, exhibiting Ki values of 2 nM and 8 nM for σ1 and σ2 receptors, respectively. With minimal affinity for the D2 receptor (Ki = 1112 nM) and negligible binding to the dopamine transporter (Ki > 10,000 nM), BD-1008 effectively antagonizes dopamine release in the nucleus accumbens shell region through σ₂ receptor blockade. This compound serves as a valuable tool for investigating addiction therapies targeting σ receptors.
AB21 hydrochloride is a potent and selective antagonist of the sigma-1 receptor (S1R), exhibiting a Ki of 13 nM for S1R and 102 nM for S2R. This compound effectively reduces mechanical hypersensitivity, making it a valuable tool for research in pain mechanisms and neuropharmacology. Its application in studying the sigma receptor's role in various biological processes highlights its significance in addressing pain-related conditions and therapeutic interventions.
BD-1008 dihydrobromide is a nonselective σ receptor antagonist, exhibiting Ki values of 2 nM for the σ1 receptor and 8 nM for the σ2 receptor. It demonstrates minimal affinity for the D2 receptor (Ki = 1112 nM) and very low affinity for the dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide effectively antagonizes dopamine release in the shell region of the nucleus accumbens via σ₂ receptor inhibition and interferes with the self-administration of σ agonists. This compound is valuable for research in addiction therapy targeting σ receptors.
EST64454 is a selective sigma-1 receptor antagonist with a Ki value of 22 nM, demonstrating oral bioactivity. This compound is useful for investigating pain mechanisms and signaling pathways associated with sigma-1 receptor activity. Its application in research can provide insights into pain modulation and potential therapeutic interventions.
