1.
Bioorg Med Chem Lett
; 17(4): 1033-6, 2007 Feb 15.
Article
in English
| MEDLINE
| ID: mdl-17129726
ABSTRACT
Investigation of halogen substitution in lead compound 1 has led to the identification of analogues which combine high affinity for 5-HT(1A) receptors and potent serotonin reuptake inhibitory activity. Several compounds show an improved selectivity over 5-HT(1B) and 5-HT(1D) receptors and a superior pharmacokinetic profile in the rat.
Subject(s)
Benzoxazines/chemical synthesis , Benzoxazines/pharmacology , Receptor, Serotonin, 5-HT1A/drug effects , Selective Serotonin Reuptake Inhibitors/chemical synthesis , Selective Serotonin Reuptake Inhibitors/pharmacology , Serotonin Antagonists/chemical synthesis , Serotonin Antagonists/pharmacology , Animals , Binding, Competitive/drug effects , CHO Cells , Callithrix , Cell Line , Cerebral Cortex/drug effects , Cerebral Cortex/metabolism , Cricetinae , Cricetulus , Guinea Pigs , Humans , Indicators and Reagents , Magnetic Resonance Spectroscopy , Mass Spectrometry , Models, Molecular , Piperazines/pharmacology , Pyridines/pharmacology , Radioligand Assay , Rats , Receptor, Serotonin, 5-HT1B/drug effects , Receptor, Serotonin, 5-HT1D/drug effects , Synaptosomes/drug effects
2.
Bioorg Med Chem Lett
; 15(22): 4989-93, 2005 Nov 15.
Article
in English
| MEDLINE
| ID: mdl-16168649
ABSTRACT
Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.
