2-[4-[3-(4-aryl/heteroaryl-1-piperazinyl)propoxy]phenyl]-2H- benzotriazoles and their N-oxides as ligands for serotonin and dopamine receptors
Articolo
Data di Pubblicazione:
1999
Citazione:
2-[4-[3-(4-aryl/heteroaryl-1-piperazinyl)propoxy]phenyl]-2H- benzotriazoles and their N-oxides as ligands for serotonin and dopamine receptors / A. Sparatore, M. Goegan, A. Cagnotto, F. Sparatore. - In: IL FARMACO. - ISSN 0014-827X. - 54:6(1999 Jun 30), pp. 402-410.
Abstract:
A small set of 2-{4-[3-(4-aryl/heteroaryl-piperazinyl)propoxy]phenyl}-2H-benzo tri azoles and corresponding N-oxides were prepared. The synthesized compounds were able to bind on some serotonin (5-HT1A, 5-HT2A) and dopamine (D2, D3) receptors, while displaying poor or no affinity for 5-HT1B, 5-HT2C, 5-HT3, and 5-HT4 subtypes. The strong contribution of the N-oxide function for the binding on 5-HT1A, D2 and D3 receptors is noteworthy. For 2-{4-[3-[4-(2-methoxyphenyl)-1-piperazinyl]propoxy]phenyl}-2H-benzotr iazole- 1-oxide (4b), the binding constants (Ki) were 11.9 (5-HT1A) and 10.5 nM (D3). In a general pharmacological screening, the 2-{4-[3-(4-phenyl-1-piperazinyl)propoxy]phenyl}-2H-benzotriazole (3a) exhibited only very weak activities, with the exception of protecting mice from cyanide-induced hypoxia.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Animals ; Spectrophotometry, Ultraviolet ; Mice ; Receptors, Serotonin ; Radioligand Assay ; Dopamine Agonists ; Structure-Activity Relationship ; Magnetic Resonance Spectroscopy ; Rats ; Serotonin Agents ; Binding, Competitive; Neostriatum ; Receptors, Dopamine; Tetrahydronaphthalenes ; Dopamine Agents; Olfactory Bulb ; Triazoles ; Spiperone ; Ligands
Elenco autori:
A. Sparatore, M. Goegan, A. Cagnotto, F. Sparatore
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