苯托沙敏

苯托沙敏用途

苯甲苯胺(Bistrimin)是一种具有镇静和镇痛作用的抗组胺药。苯基甲苯胺还具有强大的Sigma-1受体结合亲和力(Ki:160nM)[1][2][3]。
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苯托沙敏名称

[ CAS 号 ]:
92-12-6

[ 中文名 ]:
苯托沙敏

[ 英文名 ]:
phenyltoloxamine

[英文别名 ]:

苯托沙敏生物活性

[ 描述 ]:

苯甲苯胺(Bistrimin)是一种具有镇静和镇痛作用的抗组胺药。苯基甲苯胺还具有强大的Sigma-1受体结合亲和力(Ki:160nM)[1][2][3]。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体
信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450
研究领域 >> 炎症/免疫
研究领域 >> 神经疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

Sigma 1 Receptor:160 nM (Ki)


[体外研究]

苯基甲苯胺(10-50μM,24小时)在EVSA-T细胞中显示出细胞毒性[2]。苯基甲苯胺表现出强大的Sigma 1受体(S1R)结合亲和力,Ki值为160nM[3]。苯甲苯胺(100μM)抑制人肝巨细胞CYP2D6酶99.0%[4]。

苯托沙敏物理化学性质

[ 密度 ]:
1.022g/cm3

[ 沸点 ]:
359.2ºC at 760 mmHg

[ 分子式 ]:
C17H21NO

[ 分子量 ]:
255.35500

[ 闪点 ]:
106ºC

[ 精确质量 ]:
255.16200

[ PSA ]:
12.47000

[ LogP ]:
3.21780

[ 折射率 ]:
1.552

苯托沙敏毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
KH2376000
CHEMICAL NAME :
Ethanamine, N,N-dimethyl-2-(2-(phenylmethyl)phenoxy)-
CAS REGISTRY NUMBER :
92-12-6
BEILSTEIN REFERENCE NO. :
1986598
LAST UPDATED :
199701
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C17-H21-N-O
MOLECULAR WEIGHT :
255.39

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1127 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
246 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
55 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PSCBAY Psychopharmacology Service Center, Bulletin. (Bethesda, MD) V.1-3, 1961-65. For publisher information, see PSYBB9. Volume(issue)/page/year: 2,17,1963 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 83250 No. of Facilities: 19 (estimated) No. of Industries: 1 No. of Occupations: 9 No. of Employees: 934 (estimated) No. of Female Employees: 506 (estimated)
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