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。

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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。

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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

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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。

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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...

更多文献

格列美脲

格列美脲用途

格列美脲作用

格列美脲名称

格列美脲生物活性

格列美脲物理化学性质

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

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

格列美脲安全信息

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

格列美脲海关

格列美脲文献

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