阿拉普利

化合物

阿拉普利INN:alacepril)是一种ACE抑制剂药物,可用于治疗高血压。该药物代谢为卡托普利去乙酰阿拉普利[1]阿拉普利主要用于治疗高血压,在某些情况下用于治疗肾血管性高血压。它通常与其他药物结合使用,特别是其他降血压药物,如噻嗪类利尿剂,以最大限度地发挥其功效。[2]

阿拉普利
临床资料
AHFS/Drugs.com国际药品名称
给药途径口服
ATC码
  • 未分配
法律规范状态
法律规范
  • 处方药(-only)
识别信息
  • (2S)-2-[[(2S)-1-[(2S)-3-acetylsulfanyl-2-methylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid
CAS号74258-86-9  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C20H26N2O5S
摩尔质量406.50 g·mol−1
3D模型(JSmol英语JSmol
  • C[C@H](CSC(=O)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)O
  • InChI=1S/C20H26N2O5S/c1-13(12-28-14(2)23)19(25)22-10-6-9-17(22)18(24)21-16(20(26)27)11-15-7-4-3-5-8-15/h3-5,7-8,13,16-17H,6,9-12H2,1-2H3,(H,21,24)(H,26,27)/t13-,16+,17+/m1/s1 checkY
  • Key:FHHHOYXPRDYHEZ-COXVUDFISA-N checkY

作用机制

在体内,当阿拉普利经历脱乙酰化时,它会失去类似于苯丙氨酸的分子,从而将其转化为卡托普利[3]卡托普利通过两种方式发挥降血压作用。首先,它抑制血管紧张素1(一种前体分子)转化为血管紧张素II(一种使血管变窄的血管收缩剂)的过程。其次,卡托普利可以防止缓激肽的分解,缓激肽是一种自然松弛血管的血管舒张肽。[4]

参考资料

  1. ^ Alacepril. IBM Micromedex. 24 August 2010 [23 June 2022]. 
  2. ^ Alacepril. DrugCentral online drug compendium. [13 April 2024]. It is an angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. It used for the treatment of essential or renovascular hypertension (usually administered with other drugs, particularly thiazide diuretics). 
  3. ^ Campese VM, Lakdawala RS. The Challenges of Blood Pressure Control in Dialysis Patients. Nissenson AR, Fine RN (编). Handbook of dialysis therapy 5th. Philadelphia, PA: Elsevier. 2017. ISBN 978-0-323-39154-2. doi:10.1016/B978-0-323-39154-2.00053-9. The sulfhydryl agents, such as alacepril, delapril, and moveltopril, are prodrugs and thus are converted to captopril in vivo. These sulfhydryl-containing compounds have a slower onset and longer duration of action than captopril. 
  4. ^ Odaka C, Mizuochi T. Angiotensin-converting enzyme inhibitor captopril prevents activation-induced apoptosis by interfering with T cell activation signals. Clinical and Experimental Immunology. September 2000, 121 (3): 515–522. PMC 1905724 . PMID 10971519. doi:10.1046/j.1365-2249.2000.01323.x. 

外部链接