阿拉普利

化合物

阿拉普利INN:alacepril)是一種ACE抑制劑藥物,可用於治療高血壓。該藥物代謝為卡托普利去乙酰阿拉普利[1]阿拉普利主要用於治療高血壓,在某些情況下用於治療腎血管性高血壓。它通常與其他藥物結合使用,特別是其他降血壓藥物,如噻嗪類利尿劑,以最大限度地發揮其功效。[2]

阿拉普利
臨床資料
AHFS/Drugs.com國際藥品名稱
給藥途徑口服
ATC碼
  • 未分配
法律規範狀態
法律規範
  • 處方藥(-only)
識別資訊
  • (2S)-2-[[(2S)-1-[(2S)-3-acetylsulfanyl-2-methylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid
CAS號74258-86-9  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
化學資訊
化學式C20H26N2O5S
摩爾質量406.50 g·mol−1
3D模型(JSmol英語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

作用機制

在體內,當阿拉普利經歷脫乙酰化時,它會失去類似於苯丙氨酸的分子,從而將其轉化為卡托普利[3]卡托普利通過兩種方式發揮降血壓作用。首先,它抑制血管緊張素1(一種前體分子)轉化為血管緊張素II(一種使血管變窄的血管收縮劑)的過程。其次,卡托普利可以防止緩激肽的分解,緩激肽是一種自然鬆弛血管的血管舒張肽。[4]

參考資料

  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 (編). 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. 

外部連結