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Invest Clin ; 56(2): 137-54, 2015 Jun.
Artigo em Espanhol | MEDLINE | ID: mdl-26299055

RESUMO

In recent decades, many compounds with central dopaminergic activity have been designed, synthesized and evaluated pharmacologically. However, it has not been possible to obtain a drug able to improve or cure diseases involving dopaminergic regulation in the central nervous system, such as Parkinson's disease and schizophrenia, among others. Taking into consideration the term "atypical pharmacophore" and from the compound 5, the aralkyl fragment was incorporated, and the compounds 10, 11, 13a-h and 14a-h were synthesized. Both the compounds 10 and 13a-h under its methoxylated form and the compounds 11 and 14a-h under the phenolic form, were evaluated to determine their pharmacologically agonistic and antagonistic effects on central dopaminergic activity. For this, the effect of intracerebroventricular injection of said compounds on the hydromineral balance and stereotyped behavior in rats, was determined. The results of the preliminary pharmacological evaluation show a centrally acting action through dopamine mechanisms, in which the compounds 10, 11, 13d-h and 14a showed responses as agonists, whereas compounds 14b-h, had responses as antagonists.


Assuntos
Agonistas de Dopamina/farmacologia , Antagonistas de Dopamina/farmacologia , Indanos/farmacologia , Comportamento Estereotipado/efeitos dos fármacos , Animais , Comportamento Animal/efeitos dos fármacos , Agonistas de Dopamina/síntese química , Agonistas de Dopamina/química , Antagonistas de Dopamina/síntese química , Antagonistas de Dopamina/química , Indanos/síntese química , Indanos/química , Injeções Intraventriculares , Masculino , Ratos , Ratos Sprague-Dawley , Relação Estrutura-Atividade
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