吡贝地尔

化合物

吡贝地尔INNpiribedil)是一种抗帕金森病药物和哌嗪衍生物,可作为D2D3受体激动剂。它还具有α2-肾上腺素受体拮抗剂特性。[2][3]

吡贝地尔
臨床資料
AHFS/Drugs.com国际药品名称
给药途径口服
ATC碼
法律規範狀態
法律規範
  • Rx-only[1]
  • 处方药(-only)
藥物動力學數據
生物利用度10%(1小时高峰)
血漿蛋白結合率70–80%
药物代谢广泛肝
生物半衰期1.7至6.9小时
排泄途徑(68%)和胆管(25%)
识别信息
  • 2-[4-(benzo[1,3]dioxol-5-ylmethyl)piperazin-1-yl]pyrimidine
CAS号3605-01-4  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.020.695 編輯維基數據鏈接
化学信息
化学式C16H18N4O2
摩尔质量298.35 g·mol−1
3D模型(JSmol英语JSmol
  • C1CN(CCN1CC2=CC3=C(C=C2)OCO3)C4=NC=CC=N4
  • InChI=1S/C16H18N4O2/c1-4-17-16(18-5-1)20-8-6-19(7-9-20)11-13-2-3-14-15(10-13)22-12-21-14/h1-5,10H,6-9,11-12H2 ☒N
  • Key:OQDPVLVUJFGPGQ-UHFFFAOYSA-N ☒N

参考资料

  1. ^ Active substance: piribedil (PDF). List of nationally authorised medicinal products. European Medicines Agency. 26 November 2020. 
  2. ^ Millan MJ, Cussac D, Milligan G, Carr C, Audinot V, Gobert A, et al. Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization. The Journal of Pharmacology and Experimental Therapeutics. June 2001, 297 (3): 876–887 [2024-04-05]. PMID 11356907. (原始内容存档于2019-12-14). 
  3. ^ Gobert A, Di Cara B, Cistarelli L, Millan MJ. Piribedil enhances frontocortical and hippocampal release of acetylcholine in freely moving rats by blockade of alpha 2A-adrenoceptors: a dialysis comparison to talipexole and quinelorane in the absence of acetylcholinesterase inhibitors. The Journal of Pharmacology and Experimental Therapeutics. April 2003, 305 (1): 338–346. PMID 12649387. S2CID 29234876. doi:10.1124/jpet.102.046383.