格列丁唑

格列丁唑用途

格列苯唑(去糖基苯唑)是一种口服活性降糖药,具有抗糖尿病作用[1]。

格列丁唑名称

[ CAS 号 ]:
1492-02-0

[ 中文名 ]:
格列丁唑

[ 英文名 ]:
Glybuzole

[中文别名 ]:

[英文别名 ]:

格列丁唑生物活性

[ 描述 ]:

格列苯唑(去糖基苯唑)是一种口服活性降糖药,具有抗糖尿病作用[1]。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他
研究领域 >> 代谢疾病

[体内研究]

格列苯唑(100 mg/kg,p.o.)很快被吸收,在狗和大鼠的血清中发现浓度为100-250 mg/L[1]。动物模型：狗或大鼠[1]剂量：100 mg/kg给药：口服(p.o.)结果：快速吸收,在血清中浓度为100-250 mg/L。在最初的几个小时内,48小时内的尿液排泄量为给药剂量的15-30%。

[参考文献]

[1]. Populaire P, Terlain B, Lebreton G, et al. Absorption, excretion and biotransformation of benzene sulfonamido-2-tertiobutyl-5-thiadiazole-1, 3, 4 (desaglybuzole= 7 891 RP). Therapie, 1969, 24(2): 313-326.

格列丁唑物理化学性质

[ 密度 ]:
1.344g/cm3

[ 沸点 ]:
449.4ºC at 760mmHg

[ 分子式 ]:
C12H15N3O2S2

[ 分子量 ]:
297.39600

[ 闪点 ]:
225.6ºC

[ 精确质量 ]:
297.06100

[ PSA ]:
108.57000

[ LogP ]:
3.79020

[ 蒸汽压 ]:
2.88E-08mmHg at 25°C

[ 折射率 ]:
1.605

格列丁唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DB1290000
CHEMICAL NAME :
Benzenesulfonamide, N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)-
CAS REGISTRY NUMBER :
1492-02-0
LAST UPDATED :
199612
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C12-H15-N3-O2-S2
MOLECULAR WEIGHT :
297.42
WISWESSER LINE NOTATION :
T5NN DSJ CX1&1&1 EMSWR

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 :
500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
219 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
310 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
550 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - dyspnea Endocrine - hypoglycemia
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,131,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
235 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
248 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
193 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
967 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
118 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2100 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2100 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1050 mg/kg
SEX/DURATION :
female 7-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
YIKUAO Yamaguchi Igaku. Yamaguchi Medicine. (Yamaguchi Daigaku Igakkai, Kogushi Ube, Yamaguchi- Ken, Japan) V.1- 1953- Volume(issue)/page/year: 18,21,1969

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