格列齐特

化合物

格列齐特(英语:Gliclazide),商品名为达美康。是一种磺酰脲类口服抗糖尿病药[1][2]. 格列齐特可以防止因高血糖引起的细胞凋亡,保护人体的胰岛β细胞[3] 格列齐特还可以防止因2型糖尿病导致的动脉粥样硬化(防止动脉脂肪堆积)。[4]格列齐特在中国作为一线药物使用,应用极为广泛,而在其他国家却并不常用。Diamicron ( Gliclazide)

格列齐特
临床资料
商品名英语Drug nomenclature达美康
AHFS/Drugs.comMicromedex详细消费者药物信息
怀孕分级
  • : C
给药途径口服
ATC码
法律规范状态
法律规范
药物动力学数据
生物半衰期10.4小时
识别信息
  • N-(hexahydrocyclopenta[c]pyrrol-2(1H)-ylcarbamoyl)-4-methylbenzenesulfonamide
CAS号21187-98-4  checkY
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.040.221 编辑维基数据链接
化学信息
化学式C15H21N3O3S
摩尔质量323.412 g/mol
3D模型(JSmol英语JSmol
  • O=S(=O)(c1ccc(cc1)C)NC(=O)NN3CC2CCCC2C3
  • InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19) checkY
  • Key:BOVGTQGAOIONJV-UHFFFAOYSA-N checkY

药理

编辑

格列齐特为胰岛素增泌剂,通过抑制胰岛β细胞ATP-sensitive potassium channel英语ATP-sensitive potassium channel,从而促进胰岛素的释放。

引用

编辑
  1. ^ Ballagi-Pordány, György; Köszeghy, Anna; Koltai, Mária-Zsófia; Aranyi, Zoltán; Pogátsa, Gábor. Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compounds. Diabetes Research and Clinical Practice. 1990, 8 (2): 109–14. PMID 2106423. doi:10.1016/0168-8227(90)90020-T. 
  2. ^ Shimoyama, Tatsuhiro; Yamaguchi, Shinya; Takahashi, Kazuto; Katsuta, Hidenori; Ito, Eisuke; Seki, Hiroyuki; Ushikawa, Kenji; Katahira, Hiroshi; et al. Gliclazide protects 3T3L1 adipocytes against insulin resistance induced by hydrogen peroxide with restoration of GLUT4 translocation. Metabolism. 2006, 55 (6): 722–30. PMID 16713429. doi:10.1016/j.metabol.2006.01.019. 
  3. ^ Del Guerra, S; Grupillo, M; Masini, M; Lupi, R; Bugliani, M; Torri, S; Boggi, U; Del Chiaro, M; et al. Gliclazide protects human islet beta-cells from apoptosis induced by intermittent high glucose. Diabetes/Metabolism Research and Reviews. 2007, 23 (3): 234–8. PMID 16952202. doi:10.1002/dmrr.680. 
  4. ^ Katakami, N.; Yamasaki, Y.; Hayaishi-Okano, R.; Ohtoshi, K.; Kaneto, H.; Matsuhisa, M.; Kosugi, K.; Hori, M. Metformin or gliclazide, rather than glibenclamide, attenuate progression of carotid intima-media thickness in subjects with type 2 diabetes. Diabetologia. 2004, 47 (11): 1906–13. PMID 15565373. doi:10.1007/s00125-004-1547-8.