A potent

S1RA – 5 mg

Brand:
Cayman
CAS:
878141-96-9
Storage:
-20
UN-No:
Non-Hazardous - /

The sigma-1 (σ1) receptor is an intracellular, non-opioid receptor that is abundantly expressed in the central nervous system as well as peripherally. S1RA is a potent, selective antagonist of σ1 receptors (Ki = 17 nM) that weakly binds σ2 receptors (Ki = 9,300 nM).{27984} It is active in vivo, dose-dependently inhibiting neuropathic pain in several animal models, including formalin-induced nociception and capsaicin-induced mechanical hypersensitivity.{27984,27985} S1RA enhances peripheral µ-opioid analgesia without affecting opioid-induced constipation.{27986}  

 

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Description

A potent, selective antagonist of σ1 receptors (Ki = 17 nM) that weakly binds σ2 receptors (Ki = 9,300 nM); dose-dependently inhibits neuropathic pain in several animal models, including formalin-induced nociception and capsaicin-induced mechanical hypersensitivity

Formal name: 4-​[2-​[[5-​methyl-​1-​(2-​naphthalenyl)​-​1H-​pyrazol-​3-​yl]​oxy]​ethyl]​-morpholine

Synonyms:  E-52862

Molecular weight: 337.4

CAS: 878141-96-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research

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