格列吡嗪

格列吡嗪用途

Glipizide可作用于钾离子通道,可用于2型糖尿病。

格列吡嗪作用

格列吡嗪为第二代磺脲类口服降血糖药。主要是促进胰岛β细胞分泌胰岛素，尤其是促进葡萄糖刺激的胰岛素β细胞分泌；还有增强胰岛素作用，从而有效地降低血糖浓度和糖基化血红蛋白；并可改善高脂血症，降低甘油三酯和胆固醇水平，提高高密度脂蛋白胆固醇在总胆固醇中比率；还可抑制血小板聚集和促进纤维蛋白溶解，因而对血管病变可能有一定的防治作用。①促进胰腺胰岛β细胞分泌胰岛素，先决条件是胰岛β细胞还有一定的合成和分泌胰岛素的功能；②通过增加门静脉胰岛素水平或对肝脏直接作用，抑制肝糖原分解和糖原异生作用，肝生成和输出葡萄糖减少；③也可能增加胰外组织对胰岛素的敏感性和糖的利用（可能主要通过受体后作用），因此，总的作用是药动学吸收快，口服后1～2.5小时血药浓度达峰值，作用持续时间可达24小时，T1/2为2.5～4小时。主要经肝代谢失去活性，第l天97%排出体外，第2天100%排出体外。

格列吡嗪名称

[ CAS 号 ]:
29094-61-9

[ 中文名 ]:
格列吡嗪

[ 英文名 ]:
Glipizide

[中文别名 ]:

格列甲嗪

[英文别名 ]:

EINECS 249-427-6
Glican
Ozidia
Glipid
k4024
exylurea
Glucotrol
Glipizide
MFCD00072159
Mindiab

格列吡嗪生物活性

[ 描述 ]:

Glipizide可作用于钾离子通道,可用于2型糖尿病。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 代谢疾病

[参考文献]

[1]. Chowdary, K.P. and Y.S. Rao, Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: a technical note. AAPS PharmSciTech, 2003. 4(3): p. E39.

[2]. Rao, N.G., et al., Suicide by combined insulin and glipizide overdose in a non-insulin dependent diabetes mellitus physician: a case report. Med Sci Law, 2006. 46(3): p. 263-9.

[相关活性小分子]

格列吡嗪物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
676.0±65.0 °C at 760 mmHg

[ 熔点 ]:
208-209°C

[ 分子式 ]:
C₂₁H₂₇N₅O₄S

[ 分子量 ]:
445.535

[ 闪点 ]:
362.6±34.3 °C

[ 精确质量 ]:
445.178375

[ PSA ]:
138.53000

[ LogP ]:
3.37

[ 外观性状 ]:
白色或灰白色结晶粉末

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.654

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
methanol: 1.9 mg/mL

格列吡嗪MSDS

详细MSDS(安全技术说明书)

格列吡嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YS7640000

CHEMICAL NAME :: Urea, 1-cyclohexyl-3-((p-(2-(5-methylpyrazinecarboxamido)et hyl)phenyl)sulfonyl)-

CAS REGISTRY NUMBER :: 29094-61-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C21-H27-N5-O4-S

MOLECULAR WEIGHT :: 445.59

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 2400 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,208,1971

格列吡嗪安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;Xn: Harmful;

[ 风险声明 (欧洲) ]:
R21

[ 安全声明 (欧洲) ]:
S24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
YS7640000

[ 海关编码 ]:
2935009090

格列吡嗪海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

格列吡嗪文献

Identification of CYP3A7 for glyburide metabolism in human fetal livers.

Biochem. Pharmacol. 92(4) , 690-700, (2014)

Glyburide is commonly prescribed for the treatment of gestational diabetes mellitus; however, fetal exposure to glyburide is not well understood and may have short- and long-term consequences for the ...

Maternal-fetal disposition of glyburide in pregnant mice is dependent on gestational age.

J. Pharmacol. Exp. Ther. 350(2) , 425-34, (2014)

Gestational diabetes mellitus is a major complication of human pregnancy. The oral clearance (CL) of glyburide, an oral antidiabetic drug, increases 2-fold in pregnant women during late gestation vers...

Quantitative determination of metformin, glyburide and its metabolites in plasma and urine of pregnant patients by LC-MS/MS.

Biomed. Chromatogr. 29(4) , 560-9, (2015)

This report describes the development and validation of an LC-MS/MS method for the quantitative determination of glyburide (GLB), its five metabolites (M1, M2a, M2b, M3 and M4) and metformin (MET) in ...

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