Synthesis and pharmacological evaluation of 4-phenoxy-1,2,3,4-tetrahydroisoquinolines and 4,5,6,6a-tetrahydrochromeno[2,3,4-de]isoquinolines.
Med Chem
; 4(1): 1-10, 2008 Jan.
Article
em En
| MEDLINE
| ID: mdl-18220966
ABSTRACT
The novel 4-phenoxy-1,2,3,4-tetrahydroisoquinolines 6a-c and their rigid congeners 4,5,6,6a-tetrahydro-chromeno[2,3,4-de]isoquinolines 7a,b were synthesized in order to obtain dopamine D2-like receptor ligands. The new compounds were evaluated for their in vitro binding affinities, in vivo behavioral activities on rats, and for their effects on rat brain neurochemistry. Compounds 6b (toward both D2 and D3 dopamine receptors) and 7a,b (toward D3 only dopamine receptors) showed the most significant affinities. However none of the new compounds was able to stimulate behavioral activity in non pre-treated rats, nor to influence brain neurochemistry.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Agonistas de Dopamina
/
Isoquinolinas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2008
Tipo de documento:
Article
País de afiliação:
Itália