Chemistry:Lergotrile

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Lergotrile (INN, USAN; developmental code name LY-79907) is an ergoline derivative which acts as a dopamine receptor agonist. It was developed for the treatment of Parkinson's disease, but failed in clinical trials due to liver toxicity.[1][2]

The drug's hydroxylated metabolite 13-hydroxylergotrile is 100-fold more potent as a dopamine receptor agonist than lergotrile itself in vitro.[3][4]

See also

References

  1. ↑ "Lergotrile in Parkinson disease: further studies". Neurology 29 (2): 267–72. February 1979. doi:10.1212/wnl.29.2.267. PMID 34808. 
  2. ↑ "Discriminative stimulus properties of lergotrile". The Journal of Pharmacology and Experimental Therapeutics 230 (1): 47–52. July 1984. PMID 6146709. 
  3. ↑ "Psychedelics". Pharmacological Reviews 68 (2): 264–355. April 2016. doi:10.1124/pr.115.011478. ISSN 0031-6997. PMID 26841800. 
  4. ↑ "Metabolism of lergotrile to 13-hydroxy lergotrile, a potent inhibitor of prolactin release in vitro". Biochemical Pharmacology 27 (9): 1405–1408. May 1978. doi:10.1016/0006-2952(78)90131-4. PMID 29651. 

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