优降宁

优降宁是不可逆、选择性的单胺氧化酶抑制剂MAO-AMAO-BIC50分别为11.52 nM和8.20 nM)。[1][2]1963年,它由雅培抗高血压药的形式进入美国及英国市场,商品名Eutonyl。同样于1960年代进入市场的单胺氧化酶抑制剂还有尼亚拉胺异卡波肼苯乙肼反苯环丙胺[3]:146[4]:60[5][6]优降宁于2007年被停用。[7]它除了作为单胺氧化酶抑制剂,也会与单胺氧化酶的别构中心I2咪唑啉受体结合。[8]

优降宁
Skeletal formula of pargyline
Ball-and-stick model of the pargyline molecule
臨床資料
MedlinePlusa682088
ATC碼
识别
  • N-benzyl-N-methylprop-2-yn-1-amine
CAS号555-57-7  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.008.275
化学
化学式C11H13N
摩尔质量159.23 g·mol−1
3D模型(JSmol
  • C#CCN(C)Cc1ccccc1
  • InChI=1S/C11H13N/c1-3-9-12(2)10-11-7-5-4-6-8-11/h1,4-8H,9-10H2,2H3 checkY
  • Key:DPWPWRLQFGFJFI-UHFFFAOYSA-N checkY

参见

参考资料

  1. Fisar Z, Hroudová J, Raboch J. . Neuro Endocrinol Lett. 2010, 31 (5): 645–56. PMID 21200377.
  2. Murphy DL, Karoum F, Pickar D, et al. . . Journal of Neural Transmission. Supplement 52. 1998: 39–48. ISBN 978-3-211-83037-6. PMID 9564606. doi:10.1007/978-3-7091-6499-0_5. |journal=被忽略 (帮助)
  3. Edward Shorter, A historical dictionary of psychiatry. Oxford University Press, Inc 2005. ISBN 0195176685
  4. William M. Wardell and Louis Lasagna. Regulation Drug Development (Evaluative Studies 21) American Enterprise Institute (1975) ISBN 0844731676
  5. Council on Drugs New Drugs and Developments in Therapeutics: Pargyline Hydrochloride (Eutonyl) JAMA. 1963;184(11):887. doi:10.1001/jama.1963.03700240079013.
  6. . Drug and Therapeutics Bulletin. 15 November 1963, 1 (15): 59–60. ISSN 1755-5248. S2CID 220162992. doi:10.1136/dtb.1.15.59 (英语). Pargyline is promoted only for the treatment of hypertension, and not for depression.
  7. W. Steven Pray. . www.medscape.com. 2007.
  8. . CRC Press. 1995: 43.
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