| Autor: |
Röver S; Vernalis Research Ltd., Oakdene Court, 613 Reading Road, Wokingham RG41 5UA, UK. stephan.roever@roche.com, Adams DR, Bénardeau A, Bentley JM, Bickerdike MJ, Bourson A, Cliffe IA, Coassolo P, Davidson JE, Dourish CT, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Muller M, Porter RH, Richter H, Taylor S, Vickers SP |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 Aug 01; Vol. 15 (15), pp. 3604-8. |
| DOI: |
10.1016/j.bmcl.2005.05.074 |
| Abstrakt: |
Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT(2) receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT(2C) receptor agonists. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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