SML2181
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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关于此项目
经验公式（希尔记法）:
C23H32N2O2 · 2HCl
化学文摘社编号:
分子量:
441.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
SA4503, ≥98% (HPLC)
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
SMILES string
COC1=CC=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1OC
InChI key
XWOXAKBQEMQMFH-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
2-8°C
相关类别
Biochem/physiol Actions
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）。
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，在实验小鼠和大鼠中具有体内功效。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Possible involvement of the Sigma-1 receptor chaperone in chemotherapeutic-induced neuropathic pain.
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
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
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
K Matsuno et al.
European journal of pharmacology, 306(1-3), 271-279 (1996-06-13)
The binding profiles of SA4503 (1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride), a novel sigma receptor ligand, to sigma 1 and sigma 2 receptor subtypes in guinea pig and rat brain membranes were evaluated. SA4503 showed a high affinity for the sigma 1 receptor subtype
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.
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