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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.
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.
Synonyms: EMD 57445
Panamesine is a selective sigma receptor ligand with a high affinity of IC50 6 nM for sigma binding sites. This compound exhibits potential as an atypical neuroleptic agent, making it of interest in neuropharmacological research. Its unique binding properties may provide insights into the therapeutic mechanisms of sigma receptor modulation in various neurological disorders.
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.
KB-5492 free base is a selective inhibitor of sigma receptors, demonstrating potent activity by inhibiting specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding with an IC50 of 3.15 μM. This compound exhibits anti-ulcer properties, making it valuable for research in gastrointestinal disorders and related therapeutic applications. Its mechanism of action also suggests potential implications in neuropharmacology and pain management studies.
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.
PD 144418 oxalate is a selective and potent ligand for the sigma 1 (σ1) receptor, demonstrating a high binding affinity with a Ki value of 0.08 nM. Its selectivity is underscored by minimal affinity for sigma 2 (σ2) and other biological targets, including receptors, ion channels, and enzymes. This compound has potential applications in studying antipsychotic mechanisms and could serve as a valuable tool in neuropharmacological research.
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.
S1R Agonist 1 is a selective sigma-1 receptor (S1R) agonist, demonstrating a binding affinity (Ki) of 0.93 nM for S1R and 72 nM for S2R. This compound exhibits neuroprotective effects against reactive oxygen species (ROS) and N-methyl-D-aspartate (NMDA)-induced neurotoxicity. It is useful in research applications aimed at understanding neurodegenerative diseases and neuroprotection mechanisms.
S1R agonist 1 hydrochloride is a selective agonist of the sigma-1 receptor (S1R), demonstrating a binding affinity with a Ki of 0.93 nM for S1R and 72 nM for the sigma-2 receptor (S2R). This compound displays neuroprotective properties against reactive oxygen species (ROS) and NMDA-induced neurotoxicity. S1R agonist 1 hydrochloride is applicable in research focused on neurodegenerative conditions and the modulation of cellular stress responses.
KB-5492 anhydrous is a selective inhibitor of the sigma receptor, demonstrating inhibition of specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding with an IC50 of 3.15 μM. This compound has been identified for its potential application as an anti-ulcer agent, making it relevant for research in gastrointestinal disorders and sigma receptor pharmacology. Its activity underscores the significance of sigma receptors in various biological processes, providing valuable insights for therapeutic exploration.
Synonyms: JO 1784 hydrochloride
Igmesine hydrochloride is a potent σ-receptor ligand that exhibits the ability to inhibit colonic electromechanical activity stimulated by emotional stress. This compound effectively counteracts the enhancement of colonic motility induced by dopamine and centrally injected D1 or D2 receptor agonists. Additionally, Igmesine hydrochloride disrupts the colonic motility responses prompted by corticotropin-releasing factor (CRF), likely through mechanisms involving central cholecystokinin (CCK) release or activation of supraspinal CCK pathways, making it a valuable tool for studying gastrointestinal responses to stress and neurotransmitter signaling.
UKH-1114 is a selective agonist for the sigma-2 receptor, specifically targeting TMEM97, with affinities of 1279 nM and 46 nM for σ1R and σ2R/TMEM97, respectively. This compound demonstrates remarkable selectivity, displaying minimal affinity for over 50 other receptors and ion channels. UKH-1114 has been shown to effectively alleviate mechanical hypersensitivity induced by spared nerve injury (SNI) while minimizing the risk of motor impairment. It serves as a valuable tool for investigating mechanisms of neuropathic pain.
S1R Agonist 2 is a selective sigma-1 receptor (S1R) agonist, demonstrating a binding affinity of 1.1 nM for S1R and 88 nM for sigma-2 receptor (S2R). This compound exhibits significant neuroprotective effects against reactive oxygen species (ROS) and N-methyl-D-aspartate (NMDA)-induced neurotoxicity. Due to its targeted action on the S1R, S1R Agonist 2 is valuable for research focusing on neurodegenerative diseases and neuronal protection mechanisms.
Convolamine is a sigma-1 receptor modulator derived from Convolvulus pluricaulis. It demonstrates positive modulation of the sigma-1 receptor with an IC50 of 289 nM. This compound exhibits notable cognitive-enhancing and neuroprotective activities, making it a valuable tool for research into neurological disorders and cognitive function enhancement.
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.
Synonyms: KC 9172
Umespirone is an investigational compound that functions primarily as an antipsychotic and antianxiety agent. It selectively targets serotonin receptors, contributing to its anxiolytic and neuroleptic effects. Umespirone is being explored for its potential to alleviate symptoms associated with anxiety disorders and schizophrenia, providing insights into neuropharmacological mechanisms. Its unique profile supports research in the development of new therapeutic strategies for mental health conditions.
Synonyms: LU-28-179 fumarate
Siramesine fumarate is a potent sigma-2 receptor agonist with a subnanomolar affinity for sigma-2 receptors (IC50 = 0.12 nM) and a 140-fold selectivity over sigma-1 receptors (IC50 = 17 nM). This compound induces cell death through the destabilization of mitochondria without affecting lysosomes. Siramesine fumarate has demonstrated significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and the study of sigma receptor biology.
SYB4 is a positron emission tomography (PET) tracer that selectively targets the Sigma-2 receptor. Its primary application lies in neuroimaging, allowing for the visualization of Sigma-2 receptor distribution in the brains of nonhuman primates. This compound is valuable for studying neurobiological processes and may assist in understanding various neurological disorders.
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Synonyms: FTC-146 hydrochloride
CM304 is a potent sigma-1 receptor (S1R) inhibitor. It demonstrates significant neuroprotective effects by mitigating drug-induced convulsions in rat models. This compound is valuable for research focused on neurological disorders and the modulation of synaptic functions associated with S1R activity.
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.
KSCM-11 is a selective ligand for the sigma receptor, functioning as a modulator of sigma receptor activity. This compound exhibits significant potential in neuroscience research, contributing to studies on neuroprotection, pain management, and the modulation of psychotropic effects. Its targeted action on sigma receptors makes it a valuable tool for exploring therapeutic avenues in neurological disorders.
L-693403 maleate is a highly selective sigma receptor ligand with strong binding affinity. This compound serves as an important tool for investigating sigma receptor-mediated pathways and their potential implications in various physiological diseases. It is suitable for research applications focused on understanding the role of sigma receptors in neurobiology and pharmacology.
