Increased oral activity of a new class of non-hormonal pregnancy terminating agents.
J Pharmacobiodyn
; 5(1): 55-61, 1982 Jan.
Article
en En
| MEDLINE
| ID: mdl-7077522
ABSTRACT
A series of selected analogues of 2-(3-ethoxyphenyl)-5,6-dihydro-s-triazole [5, 1-a] isoquinoline (DL 204-IT) modified at the three sites of metabolism of the DL 204-IT molecule, were studied for their anti-fertility activity and absorption (in situ and in vivo) following oral administration to the hamster. All test-compounds were rather well absorbed, nevertheless, the ratios between the oral and subcutaneous pregnancy termination activity ranged between 3 and 722, suggesting a marked influence of metabolic first-pass. One of these new anti-fertility agents, 2-(1, 1'-biphenyl-4-yl)-s-triazole [5, 1-a]-isoquinoline (L 14105), showed an interesting oral activity (ED50 0.2 mg/kg/d), 300 times greater than that of the parent compound DL 204-IT.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Abortivos
/
Abortivos no Esteroideos
/
Isoquinolinas
Límite:
Animals
/
Pregnancy
Idioma:
En
Revista:
J Pharmacobiodyn
Año:
1982
Tipo del documento:
Article