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多索茶碱

多索茶碱用途

Doxofylline 是腺苷 A1 受体 (adenosine A1 receptor) 的拮抗剂,且能抑制磷酸二酯酶 IV (phosphodiesterase IV)。
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多索茶碱名称

[ CAS 号 ]:
69975-86-6

[ 中文名 ]:
多索茶碱

[ 英文名 ]:
Doxofylline

[中文别名 ]:

[英文别名 ]:

多索茶碱生物活性

多索茶碱物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
505.2±53.0 °C at 760 mmHg

[ 熔点 ]:
144-146ºC

[ 分子式 ]:
C11H14N4O4

[ 分子量 ]:
266.253

[ 闪点 ]:
259.3±30.9 °C

[ 精确质量 ]:
266.101501

[ PSA ]:
80.28000

[ LogP ]:
-0.70

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.700

[ 储存条件 ]:
室温

[ 水溶解性 ]:
Soluble

多索茶碱MSDS

多索茶碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XH5135000
CHEMICAL NAME :
Theophylline, 7-(1,3-dioxolan-2-ylmethyl)-
CAS REGISTRY NUMBER :
69975-86-6
BEILSTEIN REFERENCE NO. :
0561195
LAST UPDATED :
199806
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C11-H14-N4-O4
MOLECULAR WEIGHT :
266.29
WISWESSER LINE NOTATION :
T56 BN DN FNVNVJ F1 H1 B1- BT5O COTJ

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 :
965 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4868186
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
426 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4187308
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
315 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4187308
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
841 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 36,201,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
396 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4187308
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
216 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 36,201,1981
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多索茶碱安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37

[ 危险品运输编码 ]:
NONH for all modes of transport

多索茶碱制备

【方法一】
茶碱溶于沸水,加入氢氧化钠和3-氯-1,2-丙二醇,回流。蒸去水后用乙醇重结晶,得化合物(I),收率95%。
化合物(I)溶于水,搅拌下加入等摩尔的HIO4?2H2O,搅拌。滤集固体,乙醇重结晶,得茶碱乙醛,收率70%。
茶碱乙醛、乙二醇和对甲苯磺酸在苯中回流脱水,得多索茶碱,收率70%。
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多索茶碱文献

Doxofylline, an antiasthmatic drug lacking affinity for adenosine receptors.

Arch. Int. Pharmacodyn. Ther. 295 , 221-37, (1988)

In the present study the interaction of doxofylline, a new antiasthmatic drug, with A1- and A2-adenosine receptors of the guinea-pig brain and rat striatum was investigated in comparison with known me...

Doxofylline in rat brain in relation to locomotor activity.

Drug Metab. Dispos. 17(4) , 437-40, (1989)

Doxofylline is a new xanthine derivative with significant bronchodilatatory activity. We have studied in HPLC the distribution of doxofylline in various areas of rat brain (cortex, cerebellum, limbic ...

The effect of intravenous doxofylline or aminophylline on gastric secretion in duodenal ulcer patients.

Aliment. Pharmacol. Ther. 4(6) , 643-9, (1990)

The aim of this study was to compare the effects upon gastric secretion of therapeutic doses of aminophylline, with doxofylline, a new xanthine derivative proposed for the treatment of chronic asthma....


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公司名:上海脉铂医药科技有限公司

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相关化合物

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