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托非索泮

托非索泮用途

托福西泮是一种2,3-苯二氮卓化合物,是一种口服活性抗焦虑剂[1]。
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托非索泮名称

[ CAS 号 ]:
22345-47-7

[ 中文名 ]:
托非索泮

[ 英文名 ]:
Tofisopam

[中文别名 ]:

[英文别名 ]:

托非索泮生物活性

[ 描述 ]:

托福西泮是一种2,3-苯二氮卓化合物,是一种口服活性抗焦虑剂[1]。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他
研究领域 >> 神经疾病

[体外研究]

以50 mg/kg的剂量给药七天,可改善受损的认知能力,增强海马中减弱的突触传递,增加颗粒下区的增殖,并改善健忘症大鼠星形胶质细胞的减少[1]。

[参考文献]

[1]. Umut İrfan Üçel, et al. Antiamnesic effects of tofisopam against scopolamine-induced cognitive impairments in rats. Pharmacol Biochem Behav. 2020 Mar;190:172858.

托非索泮物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
479.0±45.0 °C at 760 mmHg

[ 熔点 ]:
155-159ºC

[ 分子式 ]:
C18H39N5O13S

[ 分子量 ]:
565.593

[ 闪点 ]:
195.2±21.2 °C

[ 精确质量 ]:
565.226501

[ PSA ]:
61.64000

[ LogP ]:
2.39

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.558

[ 储存条件 ]:
室温，密封

托非索泮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DE9540000
CHEMICAL NAME :
5H-2,3-Benzodiazepine, 1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methy l-
CAS REGISTRY NUMBER :
22345-47-7
LAST UPDATED :
199506
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C22-H26-N2-O4
MOLECULAR WEIGHT :
382.50
WISWESSER LINE NOTATION :
T67 HNN KHJ CO1 DO1 GR CO1 DO1& J1 K2

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 :
825 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1270 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
103 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3800 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1950 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
415 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9 gm/kg/30D-I
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in thymus weight Blood - changes in leukocyte (WBC) count
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
36400 mg/kg/26W-I
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - changes in lung weight Liver - changes in liver weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
110 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - sex ratio
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,565,1981
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
270 mg/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - behavioral
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,565,1981
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
12 gm/kg
SEX/DURATION :
male 30 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 12,547,1981
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托非索泮安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H400

[ 警示性声明 ]:
P273

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;N: Dangerous for the environment;

[ 风险声明 (欧洲) ]:
R22;R50

[ 安全声明 (欧洲) ]:
60-61

[ 危险品运输编码 ]:
UN 3077

[ WGK德国 ]:
2

[ RTECS号 ]:
DE9540000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

托非索泮合成路线

详细合成路线

托非索泮制备
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托非索泮文献

The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis.

J. Neural Transm. Gen. Sect. 117(11) , 1319-25, (2010)

Tofisopam is a member of the 2,3-benzodiazepine compound family which is marketed for the treatment of anxiety in some European countries. In contrast to classical 1,4-benzodiazepines, the compound do...

[Pineal hormone melatonin in low doses potentiates psychotropic and chronotropic activity of tofisopam in rats].

Eksp. Klin. Farmakol. 76(4) , 15-7, (2013)

Combination with a low dose of pineal hormone melatonin increased the anxiolytic effect of tofisopam (subthreshold dose) in open-field and cross-maze tests, as well as its chronotropic activity in tim...

Clinical trial: dextofisopam in the treatment of patients with diarrhoea-predominant or alternating irritable bowel syndrome.

Aliment. Pharmacol. Ther. 27(2) , 197-206, (2008)

Dextofisopam modulates stimulated activity in animal models of stress, altered bowel motility, and visceral hypersensitivity.To evaluate the effects of dextofisopam in men and women with diarrhoea-pre...


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公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：托非索洋

公司名：上海吉至生化科技有限公司

区域：上海市奉贤区

价格：
￥1148.0/10mg ￥4568.0/50mg

联系人：刘佳

产品详情：托非索洋

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Tofisopam

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥999.9/250mg ￥249.9/50mg ￥2799.9/1g ￥9799.9/5g

联系人：阿拉丁

产品详情：托非索泮

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