Alpha1- and alpha2-adrenoreceptor antagonist profiles of 1- and 2-[omega-(4-arylpiperazin-1-yl)alkyl]-1,2,3-benzotriazoles.
Chem Biodivers
; 2(10): 1290-304, 2005 Oct.
Article
em En
| MEDLINE
| ID: mdl-17191929
ABSTRACT
A series of pharmacologically interesting 1- and 2-[omega-(4-arylpiperazin-1-yl)alkyl]-1,2,3-benzotriazoles, compounds 1-27, were synthesized (Scheme) and subjected to various biological studies to identify structure-activity relationships (SAR). The new compounds were found to exhibit good non-selective binding affinity towards the alpha1-adrenoreceptor (Table 1). In several cases, high functional antagonism was observed towards the alpha1A-, alpha1B-, and alpha1D-adrenoreceptor subtypes (Table 2). The selectivity for these three subtypes was comparable with or superior to that displayed by the standard drug prazosin. The most-common selectivity rank order was alpha1D > alpha1B > alpha1A, followed by alpha1B > alpha1D > alpha1A. In functional experiments, antagonism towards the alpha2-adrenoreceptor was generally low; however, a few compounds were endowed with significant antagonist properties (pA2 values of up to 7.87).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Agonistas alfa-Adrenérgicos
/
Antagonistas Adrenérgicos alfa
Limite:
Animals
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article