格列美脲

格列美脲用途

Glimepiride(Amaryl)是中长效的磺酰脲类抗糖尿病化合物,ED50为182 μg/k。

格列美脲作用

本品为第三代磺酰脲类长效抗糖尿病药，其作用机制是通过与胰腺β-细胞表面的磺酰脲受体结合，此受体与ATP敏感的K+（KATP）通道相耦连，促使KATP通道关闭，引起细胞膜的去极化，使电压依赖性钙通道开放，Ca2+内流而促使胰岛素的释放，并抑制肝葡萄糖的合成。此外，格列美脲还可以通过非胰岛素依赖的途径增加心脏葡萄糖的摄取，这可能是葡萄糖转运因子1,4两种蛋白质表达作用增加所致。由于格列美脲对心血管KATP通道的作用较弱，故心血管的不良反应亦很少。

格列美脲名称

[ CAS 号 ]:
93479-97-1

[ 中文名 ]:
格列美脲

[ 英文名 ]:
Glimepiride

[中文别名 ]:

[英文别名 ]:

Glimpiride
Glimepiride
Grimepride
amary
AMARYL
GliMepiride COS
CLIMEPIRIDE
MFCD00878417
glimepirid
GliMperide

格列美脲生物活性

[ 描述 ]:

Glimepiride(Amaryl)是中长效的磺酰脲类抗糖尿病化合物,ED50为182 μg/k。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 代谢疾病

[参考文献]

[1]. Geisen, K., Special pharmacology of the new sulfonylurea glimepiride. Arzneimittelforschung, 1988. 38(8): p. 1120-30.

[2]. Liu, F., et al., Glimepiride attenuates Abeta production via suppressing BACE1 activity in cortical neurons. Neurosci Lett, 2013. 557 Pt B: p. 90-4.

[3]. Basit, A., M. Riaz, and A. Fawwad, Glimepiride: evidence-based facts, trends, and observations (GIFTS). [corrected]. Vasc Health Risk Manag, 2012. 8: p. 463-72.

[相关活性小分子]

格列美脲物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
677.0±65.0 °C at 760 mmHg

[ 熔点 ]:
212.2-214.5 °C

[ 分子式 ]:
C₂₄H₃₄N₄O₅S

[ 分子量 ]:
490.616

[ 闪点 ]:
363.2±34.3 °C

[ 精确质量 ]:
490.224976

[ PSA ]:
133.06000

[ LogP ]:
4.17

[ 外观性状 ]:
白色水晶般的固体

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.628

[ 储存条件 ]:
Room temp

[ 水溶解性 ]:
DMSO: >10 mg/mL

格列美脲MSDS

详细MSDS(安全技术说明书)

格列美脲毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UX9363950

CHEMICAL NAME :: 1H-Pyrrole-1-carboxamide, 2,5-dihydro-3-ethyl-4-methyl-N-(2-(4-(((((4-methylcyc lohexyl)amino) carbonyl)amino)sulfonyl)phenyl)ethyl)-2-oxo-, trans-

CAS REGISTRY NUMBER :: 93479-97-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C24-H34-N4-O5-S

MOLECULAR WEIGHT :: 490.68

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,547,1993

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3950 mg/kg

TOXIC EFFECTS :: Liver - other changes

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,547,1993

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: DIFREZ Diabetes Frontier. (Medikaru Rebyusha, Yoshida Bldg., 1-7-3 Hirano-machi, Chuo-ku, Osaka, 541, Japan) V.1- 1990- Volume(issue)/page/year: 3,565,1992

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: DIFREZ Diabetes Frontier. (Medikaru Rebyusha, Yoshida Bldg., 1-7-3 Hirano-machi, Chuo-ku, Osaka, 541, Japan) V.1- 1990- Volume(issue)/page/year: 3,565,1992 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 254 ug/kg

SEX/DURATION :: female 7-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - abortion Reproductive - Fertility - other measures of fertility

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 27,1477,1993

格列美脲安全信息

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

[ 危害码 (欧洲) ]:
Xn,Xi

[ 风险声明 (欧洲) ]:
R21

[ 安全声明 (欧洲) ]:
S25-S26-S36/37-S53

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UX9363950

[ 海关编码 ]:
2935009090

格列美脲合成路线

详细合成路线

格列美脲上下游产品

格列美脲上游产品

格列美脲下游产品

格列美脲制备

3-乙基-2.-,5-二氢-4-甲基-2-氧1H-吡咯和异氰酸苯乙酯反应，再用氯磺酸进行氯磺化，氨解为磺酰胺，最后和异氰酸对甲环己基酯缩合，即得产品。

格列美脲海关

[ 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%

格列美脲文献

Drug-drug interaction of losartan and glimepiride metabolism by recombinant microsome CYP2C9*1, 2C9*3, 2C9*13, and 2C9*16 in vitro.

Int. J. Clin. Pharmacol. Ther. 52(9) , 732-8, (2014)

Co-administration of anti-hypertension and anti-diabetic drugs is common in clinical settings.In this study, we characterized the drug-drug interactions of losartan (LOS) and glimepiride (GLP) using r...

Role of wetland organic matters as photosensitizer for degradation of micropollutants and metabolites.

J. Hazard. Mater. 276 , 1-9, (2014)

Overall photodegradation of pharmaceuticals, personal care products (PPCPs) and pharmaceutical metabolites were investigated in order to evaluate their photochemical fate in aquatic environments in va...

Analysis of multi-site drug-protein interactions by high-performance affinity chromatography: Binding by glimepiride to normal or glycated human serum albumin.

J. Chromatogr. A. 1408 , 133-44, (2015)

High-performance affinity chromatography (HPAC) was used in a variety of formats to examine multi-site interactions between glimepiride, a third-generation sulfonylurea drug, and normal or in vitro gl...

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