SML3970
S1RA
≥98% (HPLC)
Synonym(s):
4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine, E 52862, E-52862, E52862, MR 309, MR-309, MR309
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About This Item
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
, White to light Brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
Biochem/physiol Actions
Selective, high-affinity sigma-1 receptor antagonist with antinociceptive efficacy in vivo.
S1RA (E-52862) is a selective, high-affinity sigma-1 receptor antagonist (human/guinea pig σ1 Ki = 17/23.5 nM; σ2 Ki = 9.3 μM/rat, >1 μM/guinea pig). S1RA exerts dose-dependent antinociceptive effects in several neuropathic pain models in mice in vivo (16 - 64 mg/kg i.p.).
S1RA (E-52862) is a selective, high-affinity sigma-1 receptor antagonist (human/guinea pig σ1 Ki = 17/23.5 nM; σ2 Ki = 9.3 μM/rat, >1 μM/guinea pig). S1RA exerts dose-dependent antinociceptive effects in several neuropathic pain models in mice in vivo (16 - 64 mg/kg i.p.).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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British journal of pharmacology, 166(8), 2289-2306 (2012-03-13)
The sigma-1 (σ(1) ) receptor is a ligand-regulated molecular chaperone that has been involved in pain, but there is limited understanding of the actions associated with its pharmacological modulation. Indeed, the selectivity and pharmacological properties of σ(1) receptor ligands used
Journal of medicinal chemistry, 55(19), 8211-8224 (2012-07-13)
The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ(1) receptor (σ(1)R) antagonists are reported. The new compounds were evaluated in vitro in human σ(1)R and guinea pig σ(2) receptor (σ(2)R) binding assays. The nature of
The journal of pain, 13(11), 1107-1121 (2012-10-16)
Sigma-1 (σ(1)) receptors play a role in different types of pain and in central sensitization mechanisms; however, it is unknown whether they are involved in chemotherapy-induced neuropathic pain. We compared the ability of paclitaxel to induce cold (acetone test) and
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