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词条 Pargyline
释义

  1. See also

  2. References

{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 414591272
| IUPAC_name = N-benzyl-N-methylprop-2-yn-1-amine
| image = Pargyline.svg
| alt = Skeletal formula of pargyline
| image2 = Pargyline-3D-balls.png
| alt2 = Ball-and-stick model of the pargyline molecule
| tradename =
| MedlinePlus = a682088
| pregnancy_category =
| legal_status =
| routes_of_administration =
| bioavailability =
| protein_bound =
| metabolism =
| elimination_half-life =
| excretion =
| IUPHAR_ligand = 7262
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 555-57-7
| ATC_prefix = C02
| ATC_suffix = KC01
| ATC_supplemental = {{ATC|C02|LL01}}
| PubChem = 4688
| DrugBank_Ref = {{drugbankcite|changed|drugbank}}
| DrugBank = DB01626
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 4526
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 9MV14S8G3E
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 673
| C=11 | H=13 | N=1
| molecular_weight = 159.23 g/mol
| smiles = C#CCN(C)Cc1ccccc1
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C11H13N/c1-3-9-12(2)10-11-7-5-4-6-8-11/h1,4-8H,9-10H2,2H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = DPWPWRLQFGFJFI-UHFFFAOYSA-N
}}Pargyline (brand name Eutonyl) is an irreversible selective monoamine oxidase (MAO)-B inhibitor drug (IC50 for MAO-A is 0.01152 µmol/L and for MAO-B is 0.00820 µmol/L)[1][2] It was brought to market in the US and the UK by Abbott in 1963 as an antihypertensive drug branded "Eutonyl". It was one of several MAO inhibitors introduced in the 1960s including nialamide, isocarboxazid, phenelzine, and tranylcypromine.[3]{{rp|146}}[4]{{rp|60}}[5][6] By 2007 the drug was discontinued[7] and as of 2014 there were no generic versions available in the US.[8] In addition to its actions as an MAOI, pargyline has been found to bind with high affinity to the I2 imidazoline receptor (an allosteric site on the MAO enzyme).[9]

See also

  • Clorgyline
  • Rasagiline
  • Selegiline

References

1. ^{{cite journal |vauthors=Fisar Z, Hroudová J, Raboch J |title=Inhibition of monoamine oxidase activity by antidepressants and mood stabilizers. |journal=Neuro Endocrinol Lett. |volume=31 |issue=5 |pages=645–56|year=2010 |pmid=21200377}}
2. ^{{cite journal |vauthors=Murphy DL, Karoum F, Pickar D, etal |title=Differential trace amine alterations in individuals receiving acetylenic inhibitors of MAO-A (clorgyline) or MAO-B (selegiline and pargyline) |journal=J. Neural Transm. Suppl. |volume=52 |issue= |pages=39–48 |year=1998 |pmid=9564606 |doi= 10.1007/978-3-7091-6499-0_5|url=|series=Journal of Neural Transmission. Supplement |isbn=978-3-211-83037-6 }}
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. ^{{Cite journal|title = Eutonyl and MAO inhibitors|url = http://dtb.bmj.com/content/1/15/59|journal = Drug and Therapeutics Bulletin|date = 15 November 1963|issn = 1755-5248|pages = 59–60|volume = 1|issue = 15|doi = 10.1136/dtb.1.15.59|language = en|quote = Pargyline is promoted only for the treatment of hypertension, and not for depression.|doi-broken-date = 2019-03-10}}
7. ^W. Steven Pray Interactions Between Nonprescription Products and Psychotropic Medications US Pharmacist. 2007;32(11):12-15.
8. ^FDA Eutonyl in the Drugs@FDA Database Accessed July 19, 2014
9. ^{{cite book|title=Critical Reviews in Neurobiology|url=https://books.google.com/books?id=EP9FAQAAIAAJ|year=1995|publisher=CRC Press|page=43}}
{{Antihypertensives and diuretics}}{{Antiparkinson}}{{Monoamine metabolism modulators}}{{antihypertensive-stub}}{{nervous-system-drug-stub}}

7 : Abandoned drugs|Alkynes|Amines|Antihypertensive agents|Benzyl compounds|Disulfiram-like drugs|Monoamine oxidase inhibitors

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