Lergotrile
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| Other names | LY-79907; 2-Chloro-6-methylergoline-8β-acetonitrile |
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| Formula | C17H18ClN3 |
| Molar mass | 299.80 g·mol−1 |
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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
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.