Extremely potent orally active benzo[g]quinoline analogue of the dopaminergic prodrug
| Autor: | Håkan Wikström, Danyang Liu, Durk Dijkstra, Jan B. De Vries, Bastiaan Johan Venhuis |
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| Přispěvatelé: | Molecular Biophysics, Medicinal Chemistry |
| Jazyk: | angličtina |
| Rok vydání: | 2006 |
| Předmět: |
RING
Stereochemistry Dopaminergic CORPUS STRIATUM CIS-TRANS ISOMERIZATION Prodrug D-2 RECEPTOR Dopamine agonist Cis trans isomerization CYCLIZATION Apomorphine chemistry.chemical_compound chemistry D1 Dopamine receptor Dopamine DENSITY Drug Discovery medicine Molecular Medicine Enone SCH-23390 medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry, 49(4), 1494-1498. AMER CHEMICAL SOC |
| ISSN: | 0022-2623 |
| DOI: | 10.1021/jm051111h |
| Popis: | Enone prodrugs of dopaminergic catecholamines represent a new type of prodrug in the research area of dopamine agonists. Here, we demonstrate the first benzo[g]quinoline-derived enone that induces potent dopamine agonist effects similar to arninotetralin-derived enones. Significant effects of (-)-4 were observed in microdialysis studies after administration of 1 nmol kg(-1) sc and 3 nmol kg(-1) po. With a potency comparable to that of the most potent apomorphines, (-)-4 could potentially compete with L-DOPA and apomorphine in the treatment of Parkinson's disease. |
| Databáze: | OpenAIRE |
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