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多西拉敏

多西拉敏用途

Doxylamine是第一代抗组胺药,是一种组胺(H1)受体拮抗剂。多西拉明也是一种局部镇痛剂和有效的催眠剂[1][2][3]。

多西拉敏名称

[ CAS 号 ]:
469-21-6

[ 中文名 ]:
多西拉敏

[ 英文名 ]:
doxylamine

[中文别名 ]:

[英文别名 ]:

多西拉敏生物活性

[ 描述 ]:

Doxylamine是第一代抗组胺药,是一种组胺(H1)受体拮抗剂。多西拉明也是一种局部镇痛剂和有效的催眠剂[1][2][3]。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体
研究领域 >> 炎症/免疫
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H1 Receptor


[参考文献]

[1]. Sjöqvist F, Lasagna L. The hypnotic efficacy of doxylamine. Clin Pharmacol Ther. 1967;8(1):48-54.

[2]. Hung CH, et al. Subcutaneous infiltration of doxylamine on cutaneous analgesia in rats. Pharmacol Rep. 2018;70(3):565-569.

[3]. Jackson CD, Blackwell BN. Subchronic studies of doxylamine in B6C3F1 mice. Fundam Appl Toxicol. 1988;10(2):254-261.

多西拉敏物理化学性质

[ 密度 ]:
1.043 g/cm3

[ 沸点 ]:
364.9ºC at 760 mmHg

[ 熔点 ]:
25°C

[ 分子式 ]:
C17H22N2O

[ 分子量 ]:
270.37

[ 闪点 ]:
174.5ºC

[ 精确质量 ]:
270.17300

[ PSA ]:
25.36000

[ LogP ]:
2.92330

[ 折射率 ]:
1.5486 (estimate)

[ 储存条件 ]:
-20°C

多西拉敏毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
US9250000
CHEMICAL NAME :
Pyridine, 2-(alpha-(2-(dimethylamino)ethoxy)-alpha-methylbenzyl )-
CAS REGISTRY NUMBER :
469-21-6
BEILSTEIN REFERENCE NO. :
0230379
LAST UPDATED :
199612
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C17-H22-N2-O
MOLECULAR WEIGHT :
270.41
WISWESSER LINE NOTATION :
T6NJ BX1&R&O2N1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
440 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(5),17,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
470 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(5),17,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
460 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(5),17,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
62 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(5),17,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
250 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - rigidity (including catalepsy)
REFERENCE :
DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(5),17,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
49 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - rigidity (including catalepsy)
REFERENCE :
DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(5),17,1982

多西拉敏合成路线

详细合成路线

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