中文名称:

盐酸阿地芬宁

中文同义词:

解痉素;盐酸二苯胺乙酯;盐酸屈生丁;二苯乙酸 2-(二乙胺基)乙酯;解痉素 盐酸盐;盐酸阿地芬宁(标准品);盐酸阿的芬宁;盐酸阿地芬尼

英文名称:

Adiphenine hydrochloride

英文同义词:

2-(Diethylamino)ethyl a-phenylbenzeneacetate hydrochloride;Disodium (6E)-4-amino-3-(4-nitrophenyl)diazenyl-5-oxo-6-(phenylhydrazinylidene)naphthalene-2,7-disulfonate;Oil Black S;Orient Water Black R 455;Spasnil;Spasmolytin;2,2-diphenylacetic acid 2-diethylaminoethyl ester hydrochloride;2-diethylaminoethyl 2,2-diphenylacetate hydrochloride

CAS号:

50-42-0

分子式:

C20H25NO2.ClH

分子量:

347.88

EINECS号:

200-036-9

相关类别:

医药原料药;小分子抑制剂;医药原料;医药 解痉药;医药产品;原料药;医药与生物化工;ETHYOL;其他科研原料药;医药中间体;其他原料;医药、农药及染料中间体;医药化工类

Mol文件:

50-42-0.mol

熔点 

113-114°

密度 

1.0555 (rough estimate)

折射率 

1.5400 (estimate)

形态

neat

Merck 

14,161

InChIKey

LKPINBXAWIMZCG-UHFFFAOYSA-N

CAS 数据库

50-42-0(CAS DataBase Reference)

生物活性

Adiphenine HCl 是一种烟碱受体抑制剂，用作解痉药。

靶点

Target Value α3β4 nAChR (Cell-free assay) 1.8 μM α1 nAChR (Cell-free assay) 1.9 μM α4β2 nAChR (Cell-free assay) 3.7 μM α4β4 nAChR (Cell-free assay) 6.3 μM

Target

Value

α3β4 nAChR (Cell-free assay)

1.8 μM

α1 nAChR (Cell-free assay)

1.9 μM

α4β2 nAChR (Cell-free assay)

3.7 μM

α4β4 nAChR (Cell-free assay)

6.3 μM

体外研究

Adiphenine (10 nM-1 mM; 3 min) blocks the function of α1*-nAChR in a dose-dependent manner in TE671/RD cells, with an IC 50 of 1.9 µM. Adiphenine (10 nM-1 mM; 3 min) blocks the function of α3α4*-nAChR in a dose-dependent manner in SH-SY5Y cells, with an IC 50 of 1.8 µM. Adiphenine (10 nM-1 mM; 3 min) blocks the function of α4β2- and α4β4-nAChR in a dose-dependent manner in SH-EP1 cells, with IC 50 s of 3.7 and 6.3 µM, respectively. Adiphenine (50-200 µM; 30-60 s) decreases the frequency of ACh-induced single-channel currents in HEK 293 cells.

体内研究

Adiphenine (i.p.) prevents the hindleg tonic-extensor component of maximal electroshock seizures (MES), with an ED 50 of 62 mg/kg in mice.

危险品标志 

Xn

危险类别码 

20/21/22

安全说明 

36

WGK Germany 

3

RTECS号

AH2625000

毒性

LD50 i.p. in mice: 0.24 g/kg (Burtner, Cusic)