化學(xué)名

4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine

簡稱

S1RA

別名

E-52862, E52862, E 52862

中文名

N/A

化學(xué)式

C₂₀H₂₃N₃O₂

分子量

337.42

CAS號

878141-96-9

純度

98%

溶劑/溶解度

Water<1mg/ml; DMSO40mg/ml; Ethanol<1mg/ml

溶液配制

5mg加入1.48ml DMSO，或者每3.37mg加入1ml DMSO，配制成10mM溶液。SD2393-10mM用DMSO配制。

產(chǎn)品描述

S1RA (E-52862) is a potent and selective sigma-1 receptor (σ1R, Ki=17nM) antagonist, showed good selectivity against σ2R (Ki>1000nM).

信號通路

GPCR & G Protein

靶點(diǎn)

σ1R

σ2R

－

－

－

IC50

17nM (Ki)

>1000nM (Ki)

－

－

－

體外研究

S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki=17nM) and guinea pig (Ki=23.5nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki>1000nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki=328nM) and antagonistic activity, with very low potency (IC50=4700nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki>1μM or % inhibition at 1μM <50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes).

體內(nèi)研究

Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25mg·kg/L, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior.

臨床實(shí)驗(yàn)

N/A

特征

N/A

酶活性檢測實(shí)驗(yàn)

方法

N/A

細(xì)胞實(shí)驗(yàn)

細(xì)胞系

N/A

濃度

N/A

處理時(shí)間

N/A

方法

N/A

動(dòng)物實(shí)驗(yàn)

動(dòng)物模型

N/A

配制

N/A

劑量

N/A

給藥方式

N/A

產(chǎn)品編號

產(chǎn)品名稱

包裝

SD2393-10mM

S1RA (Sigma Receptor拮抗劑)

10mM×0.2ml

SD2393-5mg

S1RA (Sigma Receptor拮抗劑)

5mg

SD2393-25mg

S1RA (Sigma Receptor拮抗劑)

25mg

—

說明書

1份