Increased oral activity of a new class of non-hormonal pregnancy terminating agents.

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Abstract
A series of selected analogs of 2-(3-ethoxyphenyl)-5,6-dihydro-s-triazole [5,1-a] isoquinoline (DL 204 IT) modified at the 3 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 well absorbed. The ratios between the oral and s.c. pregnancy termination activity ranged between 3 and 722, suggesting a marked influence of metabolic first-pass. 2-(1,1''-Biphenyl-4-yl)-s-triazole [5,1-a]-isoquinoline (L 14105) showed an interesting oral activity (ED50:0.2 mg/kg per day), 300 times greater than that of the parent compound DL 204-IT.

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