INCREASED ORAL ACTIVITY OF A NEW CLASS OF NON-HORMONAL PREGNANCY TERMINATING AGENTS

A series of selected analogues of 2-(3-ethoxyphenyl)-5, 6-dihydro-s-triazole [5, 1-α] 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...

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Veröffentlicht in:	Journal of Pharmacobio-Dynamics 1982, Vol.5(1), pp.55-61
Hauptverfasser:	GALLIANI, GIULIO, CRISTINA, TITO, GUZZI, UMBERTO, OMODEI-SALE, AMEDEO, ASSANDRI, ALESSANDRO
Format:	Artikel
Sprache:	eng
Schlagworte:	Abortifacient Agents - administration & dosage Abortifacient Agents, Nonsteroidal - administration & dosage Abortifacient Agents, Nonsteroidal - metabolism Administration, Oral Animals Cricetinae Female Injections, Subcutaneous Intestinal Absorption Isoquinolines - administration & dosage Isoquinolines - metabolism Kinetics L14105 Mesocricetus Pregnancy
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container_title	Journal of Pharmacobio-Dynamics
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creator	GALLIANI, GIULIO CRISTINA, TITO GUZZI, UMBERTO OMODEI-SALE, AMEDEO ASSANDRI, ALESSANDRO
description	A series of selected analogues of 2-(3-ethoxyphenyl)-5, 6-dihydro-s-triazole [5, 1-α] 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-α]-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.
doi_str_mv	10.1248/bpb1978.5.55
format	Article
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subjects	Abortifacient Agents - administration & dosage Abortifacient Agents, Nonsteroidal - administration & dosage Abortifacient Agents, Nonsteroidal - metabolism Administration, Oral Animals Cricetinae Female Injections, Subcutaneous Intestinal Absorption Isoquinolines - administration & dosage Isoquinolines - metabolism Kinetics L14105 Mesocricetus Pregnancy
title	INCREASED ORAL ACTIVITY OF A NEW CLASS OF NON-HORMONAL PREGNANCY TERMINATING AGENTS
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