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Merck
모든 사진(1)

문서

SML3970

Sigma-Aldrich

S1RA

new

≥98% (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C20H23N3O2
CAS Number:
Molecular Weight:
337.42
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

, White to light Brown

solubility

DMSO: 2 mg/mL, clear

저장 온도

room temp

생화학적/생리학적 작용

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.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

José Luis Díaz et al.
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
L Romero et al.
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
Francisco Rafael Nieto et al.
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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