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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]。

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 ]:

MFCD00823171
Tobra Gobens
Tomycin
Dicon
Egyt 341
EINECS 244-922-3
Dartobcin
Tofisopamum [INN-Latin]
Tobracin
Tofisopam [INN:DCF:JAN]

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

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

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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