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优降宁

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优降宁
Skeletal formula of pargyline
Ball-and-stick model of the pargyline molecule
臨床資料
MedlinePlusa682088
ATC碼
识别信息
  • N-benzyl-N-methylprop-2-yn-1-amine
CAS号555-57-7  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.008.275 編輯維基數據鏈接
化学信息
化学式C11H13N
摩尔质量159.23 g·mol−1
3D模型(JSmol英语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

优降宁是不可逆、选择性的单胺氧化酶抑制剂MAO-A英语Monoamine oxidase AMAO-B英语Monoamine oxidase 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英语nialamide异卡波肼苯乙肼英语phenelzine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咪唑啉受体英语Imidazoline receptor结合。[8]

参见

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参考资料

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  1. ^ Fisar Z, Hroudová J, Raboch J. Inhibition of monoamine oxidase activity by antidepressants and mood stabilizers.. Neuro Endocrinol Lett. 2010, 31 (5): 645–56. PMID 21200377. 
  2. ^ Murphy DL, Karoum F, Pickar D, et al. Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (Clorgyline) or MAO-B (Selegiline and pargyline). MAO — the Mother of all Amine Oxidases. 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)页面存档备份,存于互联网档案馆) JAMA. 1963;184(11):887. doi:10.1001/jama.1963.03700240079013.
  6. ^ Eutonyl and MAO inhibitors. Drug and Therapeutics Bulletin. 15 November 1963, 1 (15): 59–60 [2024-02-18]. ISSN 1755-5248. S2CID 220162992. doi:10.1136/dtb.1.15.59. (原始内容存档于2024-06-06) (英语). Pargyline is promoted only for the treatment of hypertension, and not for depression. 
  7. ^ W. Steven Pray. Interactions Between Nonprescription Products and Psychotropic Medications. www.medscape.com. 2007 [2024-02-18]. (原始内容存档于2021-05-15). 
  8. ^ Critical Reviews in Neurobiology. CRC Press. 1995: 43.