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Lergotrile

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Lergotrile
Clinical data
Other namesLY-79907; 2-Chloro-6-methylergoline-8β-acetonitrile
Identifiers
  • 2-[(6aR,9S,10aR)-5-chloro-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]acetonitrile
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC17H18ClN3
Molar mass299.80 g·mol−1
3D model (JSmol)
  • CN1C[C@@H](C[C@H]2[C@H]1CC3=C(NC4=CC=CC2=C34)Cl)CC#N
  • InChI=1S/C17H18ClN3/c1-21-9-10(5-6-19)7-12-11-3-2-4-14-16(11)13(8-15(12)21)17(18)20-14/h2-4,10,12,15,20H,5,7-9H2,1H3/t10-,12-,15-/m1/s1
  • Key:JKAHWGPTNVUTNB-IXPVHAAZSA-N

Lergotrile (INNTooltip International Nonproprietary Name,USANTooltip United States Adopted Name; developmental code nameLY-79907) is anergolinederivative which acts as adopamine receptor agonist. It was developed for the treatment ofParkinson's disease, but failed inclinical trials due toliver toxicity.[1][2]

The drug'shydroxylatedmetabolite13-hydroxylergotrile is 100-fold morepotent as a dopamine receptor agonist than lergotrile itselfin vitro.[3][4]

See also

[edit]

References

[edit]
  1. ^Lieberman AN, Gopinathan G, Estey E, Kupersmith M, Goodgold A, Goldstein M (February 1979). "Lergotrile in Parkinson disease: further studies".Neurology.29 (2):267–72.doi:10.1212/wnl.29.2.267.PMID 34808.
  2. ^Cunningham KA, Callahan PM, Appel JB (July 1984). "Discriminative stimulus properties of lergotrile".The Journal of Pharmacology and Experimental Therapeutics.230 (1):47–52.PMID 6146709.
  3. ^Nichols DE (April 2016). Barker EL (ed.)."Psychedelics".Pharmacological Reviews.68 (2):264–355.doi:10.1124/pr.115.011478.ISSN 0031-6997.PMC 4813425.PMID 26841800.
  4. ^Parli CJ, Schmidt B, Shaar CJ (May 1978). "Metabolism of lergotrile to 13-hydroxy lergotrile, a potent inhibitor of prolactin release in vitro".Biochemical Pharmacology.27 (9):1405–1408.doi:10.1016/0006-2952(78)90131-4.PMID 29651.
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
Agonists
Antagonists
Indirect
modulators
Inhibitors
Releasers
Ergolines
(incl.lysergines)
Clavines
(6,8-dimethylergolines)
Lysergamides
(lysergic acid amides)
Ergopeptines
(peptide ergolines)
Partial ergolines
Related compounds
Natural sources


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