A novel specific binding site for anxiolytic homophthalazines in the rat brain.
FEBS Lett
; 308(2): 215-7, 1992 Aug 17.
Article
em En
| MEDLINE
| ID: mdl-1354173
ABSTRACT
Radioligand binding studies were performed in order to elucidate the mechanism of action of anxiolytic-neuroleptic homophthalazines. Rat striatal membrane preparations were found to bind 3H-EGIS 6775 [3H-GYKI-52 322, 3H-(1-(4-aminophenyl)-4-methyl-7,8-dimethoxy-5H-homophthalazine)] in a specific and displaceable manner. Several other brain regions tested were devoid of similar binding activity. Saturation analysis revealed that binding affinity was in the 10(-8)-10(-7) M range. Binding was enhanced by Mg2+ ions and, to a smaller extent by Ca2+ ions. The binding principle was sensitive to heat or trypsin treatment. This specific binding site appears, according to competition studies, different from the receptors whose presence in the rat striatum has been reported earlier.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ansiolíticos
/
Benzodiazepinas
/
Encéfalo
Limite:
Animals
Idioma:
En
Revista:
FEBS Lett
Ano de publicação:
1992
Tipo de documento:
Article
País de afiliação:
Hungria