Document Detail


Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus.
MedLine Citation:
PMID:  18072244     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
This paper reports the microwave-assisted synthesis and the binding assays on the 5-HT(1A), 5-HT(2A) and 5-HT(2C) receptors of new benzotriazinone derivatives, in order to identify selective ligands for the 5-HT(1A) subtype receptor. Conventional and microwave heating of the reactions were compared. Good yields and short reaction times are the main advantages of our synthetic route. More active compounds were selected and further evaluated for their binding affinities on D(1), D(2) dopaminergic and alpha(1), alpha(2) adrenergic receptors. The 3-(2-(4-(naphthalen-1-yl)piperazin-1-yl)ethyl)benzo[d][1,2,3]triazin-4(3H)-one 5 with K(i)= 0.000178 nM was the most active and selective derivative for the 5-HT(1A)receptor with respect to other serotonin receptors and the most selective derivative compared to dopaminergic and adrenergic receptors.
Authors:
Ferdinando Fiorino; Beatrice Severino; Francesca De Angelis; Elisa Perissutti; Francesco Frecentese; Paola Massarelli; Giancarlo Bruni; Elga Collavoli; Vincenzo Santagada; Giuseppe Caliendo
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  341     ISSN:  0365-6233     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  2008 Jan 
Date Detail:
Created Date:  2008-01-02     Completed Date:  2008-04-08     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  20-7     Citation Subset:  IM    
Affiliation:
Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli Federico II, Napoli, Italy.
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MeSH Terms
Descriptor/Qualifier:
Animals
Binding Sites
Cerebral Cortex / metabolism
Corpus Striatum / metabolism
Ligands
Male
Microwaves
Naphthalenes / chemical synthesis*,  chemistry,  pharmacology
Piperazines / chemical synthesis*,  chemistry,  pharmacology
Radioligand Assay
Rats
Rats, Sprague-Dawley
Receptor, Serotonin, 5-HT1A / metabolism*
Structure-Activity Relationship
Triazines / chemical synthesis*,  chemistry,  pharmacology
Chemical
Reg. No./Substance:
0/3-(2-(4-(naphthalen-1-yl)piperazin-1-yl)ethyl)benzo(d)(1,2,3)triazin-4(3H)-one; 0/Ligands; 0/Naphthalenes; 0/Piperazines; 0/Triazines; 112692-38-3/Receptor, Serotonin, 5-HT1A

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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