Date published: 2025-10-8

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Sigma Receptor Inhibitors

Sigma receptor inhibitors constitute a specialized class of chemicals meticulously crafted to finely tune the intricate activity of sigma receptors. Sigma receptors, pervasive in diverse tissues and cell types, particularly within the central nervous system, are central players in a spectrum of cellular processes. Their involvement spans neurotransmission, ion channel regulation, and cell survival, highlighting their significance in maintaining cellular homeostasis. This intricate web of functions is further delineated through the differentiation of sigma receptors into two subtypes: sigma-1 and sigma-2, each characterized by unique structural and functional attributes. The development of sigma receptor inhibitors is a targeted endeavor, aiming to selectively interact with either the sigma-1 or sigma-2 subtype. By doing so, these inhibitors seek to intricately modulate the function of the respective sigma receptor subtype, thereby influencing downstream cellular responses. Sigma receptors, being implicated in a myriad of physiological and pathological processes, become intriguing targets for intervention through these inhibitors. Sigma-1 receptor inhibitors, for instance, may influence cellular processes through their selective interaction with sigma-1 receptors primarily located in the endoplasmic reticulum. This organelle, involved in protein and lipid synthesis, becomes a focal point for sigma-1-mediated modulation. Similarly, sigma-2 receptor inhibitors target cellular processes associated with the cell membrane, where sigma-2 receptors play a role in phenomena like cell proliferation. The specificity of these inhibitors allows for the nuanced investigation of sigma receptor subtypes, unraveling their roles in diverse cellular functions. The development and study of sigma receptor inhibitors contribute significantly to advancing our understanding of sigma receptor biology. Through precise modulation, these inhibitors offer insights into the intricacies of cellular signaling pathways governed by sigma receptors. Sigma receptor inhibitors, with their targeted approach, provide invaluable tools for researchers to dissect the molecular nuances of sigma receptor-mediated signaling, paving the way for innovative interventions and a deeper comprehension of cellular physiology and pathology.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Naloxone hydrochloride

357-08-4sc-203153
sc-203153A
sc-203153B
sc-203153C
50 mg
100 mg
1 g
10 g
$85.00
$166.00
$335.00
$1827.00
2
(1)

Naloxone hydrochloride may inhibits Sigma Receptor by binding to its active site or interacting with its binding site, disrupting the receptor's normal function. This interference can impact downstream signaling and cellular processes regulated by the Sigma Receptor.

BD 1047 dihydrobromide

138356-21-5sc-203837
sc-203837A
10 mg
50 mg
$142.00
$597.00
4
(0)

This compound may bind to the sigma-1 receptor's active site or its binding pocket. By doing so, it competitively blocks the binding of endogenous ligands or other molecules that would normally interact with the receptor.

NE 100 hydrochloride

149409-57-4sc-204121
sc-204121A
sc-204121B
sc-204121C
sc-204121D
10 mg
50 mg
500 mg
1 g
10 g
$162.00
$683.00
$4080.00
$7140.00
$64566.00
21
(1)

NE 100 hydrochloride exhibits a remarkable affinity for sigma receptors, characterized by its unique ability to stabilize receptor conformations through specific electrostatic interactions. This compound demonstrates distinct kinetic properties, allowing for rapid binding and unbinding, which may influence receptor activation states. Its molecular architecture promotes effective hydrophobic interactions, enhancing membrane permeability and facilitating nuanced modulation of intracellular signaling cascades.

BD 1063 dihydrochloride

206996-13-6sc-203838
sc-203838A
sc-203838B
sc-203838C
sc-203838D
10 mg
50 mg
1.5 g
2 g
3 g
$145.00
$500.00
$5000.00
$5700.00
$6533.00
1
(0)

BD 1063 dihydrochloride is notable for its selective engagement with sigma receptors, showcasing a unique binding profile that alters receptor dynamics. Its structure enables specific hydrogen bonding and hydrophobic interactions, which contribute to its stability in biological environments. The compound's kinetic behavior is marked by a slow dissociation rate, allowing for prolonged receptor occupancy. This characteristic may lead to intricate modulation of downstream signaling pathways, influencing cellular responses.

SM-21 maleate

155058-71-2sc-204289
sc-204289A
10 mg
50 mg
$154.00
$638.00
1
(0)

SM-21 maleate exhibits a distinctive affinity for sigma receptors, characterized by its ability to induce conformational changes in receptor structure upon binding. This compound facilitates unique electrostatic interactions that enhance receptor-ligand stability. Its reaction kinetics reveal a rapid association phase, followed by a gradual equilibrium, which may influence the receptor's regulatory mechanisms. Additionally, SM-21 maleate's solubility properties allow for effective distribution in various environments, impacting its interaction dynamics.

BD 1008 Dihydrobromide

138356-09-9sc-207316
10 mg
$140.00
(0)

BD 1008 Dihydrobromide demonstrates a notable selectivity for sigma receptors, engaging in specific hydrogen bonding and hydrophobic interactions that stabilize its binding. This compound exhibits a unique allosteric modulation effect, altering receptor activity through conformational shifts. Its kinetic profile indicates a biphasic binding mechanism, with an initial fast phase followed by a slower dissociation, suggesting potential for prolonged receptor engagement. The compound's solubility characteristics further enhance its interaction potential across diverse biological systems.

BD 1008

138356-08-8sc-203426
sc-203426A
10 mg
50 mg
$200.00
$525.00
(0)

BD 1008 is characterized by its distinctive affinity for sigma receptors, where it engages in intricate electrostatic interactions that facilitate receptor activation. This compound exhibits a unique dual-binding mode, allowing it to influence receptor dynamics through both competitive and non-competitive pathways. Its reaction kinetics reveal a rapid association phase, followed by a gradual stabilization, indicating a complex interplay with receptor conformations. Additionally, BD 1008's lipophilicity enhances its membrane permeability, promoting effective receptor engagement.

Metaphit methanesulfonate salt

99287-12-4sc-253003
25 mg
$186.00
(0)

Metaphit methanesulfonate salt demonstrates a remarkable selectivity for sigma receptors, engaging in specific hydrogen bonding and hydrophobic interactions that modulate receptor activity. Its unique structural features enable it to adopt multiple conformations, influencing receptor signaling pathways. The compound exhibits a notable rate of dissociation, suggesting a dynamic equilibrium with receptor states. Furthermore, its solubility profile enhances its interaction potential within biological membranes, facilitating nuanced receptor modulation.