Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists

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. Selectivi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-08, Vol.15 (15), p.3604-3608
Hauptverfasser:	RÖVER, S, ADAMS, D. R, HEBEISEN, P, KENNETT, G. A, KNIGHT, A. R, MALCOLM, C. S, MATTEI, P, MISRA, A, MIZRAHI, J, MULLER, M, PORTER, R. H. P, RICHTER, H, BENARDEAU, A, TAYLOR, S, VICKERS, S. P, BENTLEY, J. M, BICKERDIKE, M. J, BOURSON, A, CLIFFE, I. A, COASSOLO, P, DAVIDSON, J. E. P, DOURISH, C. T
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Eating - drug effects Indoles - chemical synthesis Indoles - pharmacology Injections, Subcutaneous Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyrazines - chemical synthesis Pyrazines - pharmacology Pyridines - chemical synthesis Pyridines - pharmacology Rats Rats, Wistar Serotonin 5-HT2 Receptor Agonists Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - pharmacology Serotoninergic system Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.05.074