维格列汀

维格列汀(英语:Vildagliptin),商品名为高糖优适,是一种二肽基肽酶-4抑制剂类口服抗糖尿病药,用来治疗第2型糖尿病[2][3][3][2]

维格列汀
Skeletal formula
Ball-and-stick model
临床资料
商品名英语Drug nomenclatureGalvus
其他名称(2S)-1-{2-[(3-hydroxy-1-adamantyl)amino]acetyl}pyrrolidine-2-carbonitrile
AHFS/Drugs.com国际药品名称
核准状况
怀孕分级
  • Not recommended
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
生物利用度85%
血浆蛋白结合率9.3%
药物代谢主要水解为非活性代谢物; CYP450没有明显参与
生物半衰期2-3小时
排泄途径肾脏
识别信息
  • (S)-1-[N-(3-hydroxy-1-adamantyl)glycyl]pyrrolidine-2-carbonitrile
CAS号274901-16-5  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.158.712 编辑维基数据链接
化学信息
化学式C17H25N3O2
摩尔质量303.399 g/mol
3D模型(JSmol英语JSmol
  • N#C[C@H]4N(C(=O)CNC13CC2CC(C1)CC(O)(C2)C3)CCC4
  • InChI=1S/C17H25N3O2/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16/h12-14,19,22H,1-8,10-11H2/t12?,13?,14-,16?,17?/m0/s1 checkY
  • Key:SYOKIDBDQMKNDQ-XWTIBIIYSA-N checkY

维格列汀是唯一一种无论在高血糖或低血糖时都可以抑制胰高血糖素的物质。

引用

  1. ^ WHO International Working Group for Drug Statistics Methodology. ATC/DDD Classification (FINAL): New ATC 5th level codes. WHO Collaborating Centre for Drug Statistics Methodology. August 27, 2008 [2008-09-05]. (原始内容存档于2008年5月6日). 
  2. ^ 2.0 2.1 Ahrén, B; Landin-Olsson, M; Jansson, PA; Svensson, M; Holmes, D; Schweizer, A. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes. The Journal of Clinical Endocrinology and Metabolism. 2004, 89 (5): 2078–84 [2015-08-30]. PMID 15126524. doi:10.1210/jc.2003-031907. (原始内容存档于2011-05-16). 
  3. ^ 3.0 3.1 Mentlein, R; Gallwitz, B; Schmidt, WE. Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum. European journal of biochemistry / FEBS. 1993, 214 (3): 829–35. PMID 8100523. doi:10.1111/j.1432-1033.1993.tb17986.x.