Sigma Receptor

Cat. No.

A79295

CAS No.

1424832-57-4

(2S,3S)-E1R

(2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) that enhances cognitive and memory functions. This enantiomer of E1R is designed for research applications exploring the modulation of sigma-1 receptor activity, which has implications in treating cognition and memory disorders. Its selectivity and mechanism of action make it a valuable reagent in neuroscience studies.

Cat. No.

A79296

CAS No.

2088272-67-5

EST64454 maleate

EST64454 maleate is a potent σ1 receptor antagonist, effectively demonstrating antinociceptive properties suitable for pain management research. With excellent metabolic stability in various species and a favorable pharmacokinetic profile in rodent models, EST64454 maleate stands out as a promising candidate for clinical applications. Its high aqueous solubility and suitable permeability through Caco-2 cell membranes further support its potential in drug development studies.

Cat. No.

A79297

CAS No.

1415247-18-5

KSCM-5

KSCM-5 is a high-affinity ligand for the sigma-1 receptor, exhibiting a Ki value of approximately 34 nM, which indicates significant selectivity. Its unique interaction with the sigma receptor makes KSCM-5 valuable for research applications in compound development targeting diseases related to sigma receptor dysregulation. This compound can provide insights into the therapeutic potential and mechanisms of sigma receptors in various biological processes.

Cat. No.

A79298

CAS No.

1335032-28-4

Sigma-1 receptor antagonist 6

Sigma-1 receptor antagonist 6 is a selective antagonist of the Sigma-1 receptor (σ1R), exhibiting significant antiallodynic properties. This compound effectively reduces mechanical allodynia in neuropathic pain models, particularly in response to paclitaxel treatment. Its application in research settings enables the exploration of σ1R modulation in pain pathways and the development of novel analgesic therapies.

Cat. No.

A79299

CAS No.

468-61-1

Oxeladin

Oxeladin is an orally active cough suppressant that functions as a selective sigma 1 receptor agonist with a Ki of 25 nM. This compound demonstrates significant potential in modulating cough reflex and can be utilized in research related to pulmonary diseases and stroke. Its ability to penetrate the blood-brain barrier further enhances its relevance in neuropharmacological studies.

Cat. No.

A79300

CAS No.

932736-91-9

(±)-PPCC hemioxalate

(±)-PPCC hemioxalate is a selective modulator of the sigma-1 receptor, which plays a critical role in regulating intracellular calcium signaling between the endoplasmic reticulum and mitochondria. This compound promotes the dissociation of the sigma-1 receptor from the BIP complex, influencing cellular bioenergetics and survival. (±)-PPCC hemioxalate is suitable for research applications related to cocaine addiction, memory processes, pain modulation, depression, Alzheimer's disease, stroke, and cancer studies.

Cat. No.

A79301

CAS No.

139652-86-1

Sigma-LIGAND-1 hydrochloride

Sigma-LIGAND-1 hydrochloride is a selective ligand for sigma receptors, exhibiting IC50 values of 16 nM and 19 nM at the DTG and PPP sites, respectively. This compound demonstrates a Ki of 4000 nM at the dopamine D2 receptor, indicating its selectivity for sigma binding. It is valuable for research in neuropharmacology, particularly in studies exploring sigma receptor-mediated signaling pathways and their implications in various neurological disorders.

Cat. No.

A79303

CAS No.

787623-60-3

(Rac)-E1R

(Rac)-E1R is a racemic mixture that functions as a positive allosteric modulator of the sigma-1 receptor (Sig1R PAM). This compound has been investigated for its potential role in enhancing cognitive functions and memory processes. Research applications include the study of cognitive and memory disorders, making it a valuable tool in neuroscientific investigations.

Cat. No.

A79304

CAS No.

1424832-60-9

(2R,3S)-E1R

(2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) that enhances receptor activity. This compound has demonstrated potential in the treatment of cognition and memory disorders by modulating signaling pathways associated with neuroprotection and cognitive enhancement. Its unique mechanism of action makes it a valuable tool for research in neurobiology and the development of therapies for neurodegenerative diseases.

Cat. No.

A79305

CAS No.

2573850-59-4

PW507

PW507 is a selective antagonist of the sigma 1 receptor (S1R) with a binding affinity of Ki 7.5 nM for the human variant. With minimal interactions with the sigma 2 receptor (S2R) and hERG channel, PW507 is well-suited for studies requiring brain penetration. This compound is particularly relevant for investigating painful diabetic neuropathy (PDN) and other related conditions.

Cat. No.

A79306

CAS No.

1350296-29-5

CM764

CM764 is a sigma receptor activator, exhibiting Ki values of 86.6 nM for the sigma-1 receptor and 3.5 nM for the sigma-2 receptor. This compound increases cytoplasmic calcium levels, enhances NAD+/NADH and ATP production, and reduces reactive oxygen species (ROS) concentration. CM764 is relevant for studies exploring sigma receptor pathways and their implications in cellular metabolism and oxidative stress.

Cat. No.

A79307

CAS No.

2095551-67-8

SAS-1121

SAS-1121 is a selective ligand for the sigma 2 receptor and PGRMC1, exhibiting a Ki of 16.2 nM. It demonstrates a remarkable 574-fold selectivity for the sigma 2 receptor compared to the sigma 1 receptor. As a tertiary amine, SAS-1121 is valuable for studying mechanisms related to neurological conditions and offers potential insights into sigma receptor-related pathways in pharmacological research.

Cat. No.

A79308

CAS No.

1400888-63-2

(2R,3R)-E1R

(2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM), specifically designed for enhancing cognitive function and memory. This enantiomer of E1R exhibits significant biological activity in modulating Sig1R, which is implicated in various neurological processes. Research applications include the investigation of cognitive and memory disorders, offering potential therapeutic insights for related conditions.

Cat. No.

A79309

CAS No.

909-39-7

Opipramol dihydrochloride

Synonyms: Ensidon dihydrochloride; G-33040 dihydrochloride

Opipramol dihydrochloride is a sigma (σ) receptor agonist that exhibits notable binding affinity, with a Ki value of 50 nM for sigma recognition sites. This atypical tricyclic antidepressant is primarily utilized in research related to generalized anxiety disorder (GAD). Opipramol's mechanism of action involves modulation of sigma receptor activity, highlighting its potential in elucidating the pathophysiology of anxiety disorders and evaluating novel therapeutic approaches.

Cat. No.

A79310

CAS No.

220120-14-9

E-5842 citrate

E-5842 citrate is a selective σ receptor ligand with a Ki value of 4 nM for the σ1 receptor. This compound has been shown to enhance Fos protein levels in the medial prefrontal cortex and nucleus accumbens, while having no effect on protein levels in the striatum. E-5842 citrate is valuable for investigating the neurobiological mechanisms underlying psychiatric disorders.

Cat. No.

A79311

CAS No.

3026677-23-3

AB21

AB21 is a potent and selective antagonist of the sigma-1 receptor (S1R), exhibiting an IC50 value of 13 nM for S1R with minimal activity against the sigma-2 receptor (S2R) at 102 nM. This compound is effective in reducing mechanical hypersensitivity, making it a valuable tool for research into pain modulation and related neurological disorders. Additionally, AB21 may facilitate studies into the role of S1R in various physiological and pathological processes.

Cat. No.

A79312

CAS No.

2839205-09-1

WLB-87848

WLB-87848 is a selective σ1 receptor agonist with a Ki value of 9 nM, demonstrating high oral bioavailability and the ability to penetrate the blood-brain barrier. This compound has been shown to effectively rescue recognition memory impairment, making it a valuable tool for research in neurodegenerative diseases and memory-related disorders. Its specific targeting of the σ1 receptor positions WLB-87848 as a promising candidate for further investigation in cognitive enhancement studies.

Cat. No.

A79313

CAS No.

1781628-91-8

(±)-PPCC oxalate

(±)-PPCC oxalate is a potent sigma-1 agonist, exhibiting high affinity for sigma-1 receptors with a Ki of 1.5 nM. It demonstrates significant anti-amnesic effects in rodent models of cognitive impairment, effectively enhancing cognitive function in both mild and severe cases. This compound is useful for research in neuropharmacology and the exploration of cognitive disorders.

Cat. No.

A79314

CAS No.

2860554-32-9

Sigma-2 Radioligand 1

Sigma-2 Radioligand 1 is a selective ligand targeting the sigma-2 receptor. This radioligand demonstrates favorable biodistribution in murine models and exhibits significant in vivo activity in rat studies. Modified with [18F], Sigma-2 Radioligand 1 is suitable for micro-PET/CT imaging, displaying high tumor uptake and an optimal tumor-to-background ratio, particularly in U87MG glioma xenografts. Its specificity makes it a valuable tool for tumor visualization and research into sigma receptor biology.

Cat. No.

A79315

CAS No.

138356-20-4

BD-1047

BD-1047 is a selective functional antagonist targeting sigma receptors. It demonstrates significant activity in modulating behaviors associated with dopamine signaling, reducing apomorphine-induced climbing and phencyclidine-induced head twitches. This compound is valuable for research applications in neuropharmacology and the study of sigma receptor biology.

Cat. No.

A79316

CAS No.

1121932-91-9

CM572

CM572 is a selective irreversible partial agonist of the sigma-2 receptor. It demonstrates significant antitumor activity, inducing dose-dependent cell death in SK-N-SH neuroblastoma cells, with an EC50 of 7.6 μM. This compound is valuable for researching various malignancies, including neuroblastoma and breast cancer.

Cat. No.

A79318

CAS No.

932736-90-8

(±)-PPCC

(±)-PPCC is a potent sigma-1 receptor agonist, exhibiting a binding affinity with a Ki value of 1.5 nM. This compound demonstrates significant anti-amnesic effects in both mild and severe cognitive impairment models in rats, leading to marked improvements in cognitive function. Its utility in neurological research makes it a valuable tool for studying the mechanisms underlying cognitive disorders and potential therapeutic interventions.

Cat. No.

A79319

CAS No.

1415247-17-4

KSCM-1

KSCM-1 is a selective ligand for the sigma-1 receptor, exhibiting a Ki value of 27.5 nM. This compound demonstrates a marked selectivity for the sigma-1 receptor over sigma-2 receptors and exhibits minimal affinity for non-sigma receptor targets. KSCM-1 is valuable for studies investigating the role of sigma-1 receptors in various biological processes and neurological disorders.

Cat. No.

A79321

CAS No.

511-13-7

Chlophedianol hydrochloride

Synonyms: Clofedanol hydrochloride; Calmotusin hydrochloride; NSC 113595 hydrochloride

Chlophedianol hydrochloride is a potent antitussive agent that acts primarily by suppressing the cough reflex in the central nervous system. This compound is useful in research focused on acute cough, particularly in the context of upper respiratory tract infections (URIs). Its efficacy in alleviating cough symptoms makes it a valuable tool for studies aimed at understanding cough mechanisms and developing new therapeutic strategies.

Cat. No.

A79322

CAS No.

1422251-09-9

SOMCL-668

SOMCL-668 is a selective and potent allosteric modulator of the sigma-1 receptor. It has been demonstrated to enhance social interaction and alleviate cognitive impairments induced by the sigma-1 agonist PRE084. Additionally, SOMCL-668 exhibits anti-seizure properties, making it a valuable tool for research into psychotic illnesses and related neurological disorders.