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Merck

SML2181

Sigma-Aldrich

SA4503

≥98% (HPLC)

别名:

1-(3,4-二甲氧基苯乙基)-4-(3-苯丙基)哌嗪二盐酸盐, AGY 94806, AGY94806, Cutamesine, SA 4503

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About This Item

经验公式(希尔记法):
C23H32N2O2 · 2HCl
分子量:
441.43
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

H2O: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

COC1=CC=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1OC

InChI

1S/C23H32N2O2.2ClH/c1-26-22-11-10-21(19-23(22)27-2)12-14-25-17-15-24(16-18-25)13-6-9-20-7-4-3-5-8-20;;/h3-5,7-8,10-11,19H,6,9,12-18H2,1-2H3;2*1H

InChI 密鑰

XWOXAKBQEMQMFH-UHFFFAOYSA-N

生化/生理作用

SA4503 是一种高亲和力,口服活性的非阿片类细胞内受体 sigma-1(σ1R)选择性激动剂(IC50 为 17.4 nM,相比(+)镇痛新结合 1σR 为 200 nM),对 sigma 2 受体亚型(σ2R)的亲和力低约 100 倍,对其他 36 种受体、离子通道和第二信使系统几乎没有亲和力。据报道,口服给药可引起大鼠额叶皮质和海马中的脑乙酰胆碱(ACh)释放(5-20 mg/kg,口服给药),并在小鼠强迫游泳试验中减少了不动时间(静止不动时间为 214.8 s(不给药) 对比 11.1.6 s(给药),1.0 mg/kg 口服剂量)。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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K Matsuno et al.
European journal of pharmacology, 312(3), 267-271 (1996-10-03)
The immobility time in the mouse forced swimming test was dose-dependently reduced by sigma 1 receptor agonists, such as 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503) and (+)-pentazocine, and non-specific sigma receptor agonists, such as 1,3-di(2-tolyl)guanidine (DTG) and (+)-N-cyclopropyl-methyl-N-methyl-1,4-diphenyl-1-yl-but-3-en-1-ylamin e hydrochloride (JO-1784). On the
Andrew J Rennekamp et al.
Nature chemical biology, 12(7), 552-558 (2016-05-31)
Humans and many animals show 'freezing' behavior in response to threatening stimuli. In humans, inappropriate threat responses are fundamental characteristics of several mental illnesses. To identify small molecules that modulate threat responses, we developed a high-throughput behavioral assay in zebrafish
Mori Tomohisa et al.
Synapse (New York, N.Y.), 69(11), 526-532 (2015-08-04)
Previous studies have shown that ligands of the sigma-1 receptor chaperone (Sig-1R) regulate pain-related behaviors. Clinical use of chemotherapeutics is often compromised due to their adverse side effects, particularly those related to neuropathy. Previous studies have shown that repeated administration
Yasuharu Shinoda et al.
PloS one, 11(10), e0163992-e0163992 (2016-10-16)
Cardiovascular diseases are risk factors for depression in humans. We recently proposed that σ1 receptor (σ1R) stimulation rescued cardiac hypertrophy and heart failure induced by transverse aortic constriction (TAC) in mice. Importantly, σ1R stimulation reportedly ameliorates depression-like behaviors in rodents.
Dennis K Miller et al.
Pharmacology, biochemistry, and behavior, 150-151, 198-206 (2016-11-17)
This study examined the effect of the N-phenylpropyl-N'-substituted piperazine ligands SA4503 (3.4-dimethoxyphenethyl), YZ-067 (4-methoxyphenethyl), YZ-185 (3-methoxyphenethyl) and Nahas-3h (4-methoxybenzyl) on methamphetamine-induced hyperactivity in mice. In a previous study in rats, SA4503 increased methamphetamine-induced hyperactivity at a lower ligand dose and

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