Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4794
Title: Alpha1-Adrenoceptor Antagonists. 6. Structural Optimization of Pyridazinone-Arylpiperazines. Study of the Influence on Affinity and Selectivity of Cyclic Substituents at the Pyridazinone Ring and Alkoxy Groups at the Arylpiperazine Moiety
Authors: L., Betti
Botta, Maurizio 
Corelli, Federico 
M., Floridi
G., Giannaccini
L., Maccari
Manetti, Fabrizio 
G., Strappaghetti
Issue Date: 2003
Project: None 
Journal: JOURNAL OF MEDICINAL CHEMISTRY
Abstract: 
In continuing our search for selective α1-adrenoceptor (AR) antagonists, we have synthesized new alkoxyarylpiperazinylalkylpyridazinone derivatives. The new compounds were tested for their affinity toward α1- and α2-AR and toward the 5-HT1A receptor. α1-AR affinity data are in the subnanomolar range, with 3 showing an affinity of 0.052 nM, about 5-fold higher than prazosin. None of the studied compounds was found to be α1/α2 selective, but 8 showed an interesting 5-HT1A/α1 affinity ratio of 119.
Description: 
24418
URI: http://hdl.handle.net/20.500.12779/4794
ISSN: 0022-2623
DOI: 10.1021/jm0307842
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