Two 2-aryl imidazo [2,1-a] isoquinolines were synthesized and tested for pregnancy terminating activities. Both of them are new compounds and their structures were confirmed by IR, (HNMR)-H-1, MS and elemental analysi...Two 2-aryl imidazo [2,1-a] isoquinolines were synthesized and tested for pregnancy terminating activities. Both of them are new compounds and their structures were confirmed by IR, (HNMR)-H-1, MS and elemental analysis. They both showed high activities in NIH mice.展开更多
Contragestazolin (L14105) belongs to the class of 2 phenyl triazole isoquinolines. When given subcutaneously, intramuscularly or orally showed potential pregnancy terminating activity in mice, rats, hamsters...Contragestazolin (L14105) belongs to the class of 2 phenyl triazole isoquinolines. When given subcutaneously, intramuscularly or orally showed potential pregnancy terminating activity in mice, rats, hamsters and guinea pigs, but the dialy doses of oral administration needed were 7.1, 6.3 and 47.6 times (for mouse, rat and hamster) greater than those needed parenterally. L14105 had low affinity to rat uterine progesterone receptor. When cultured human decidual cells were exposed to L14105 0.077～0.155 mmol/L for 24～48 h, the cells' viability markedly dropped and structural changes occurred in comparison with controls. Histological examination of conceptuses of rats showed edema, degeneration, necrosis and atrophy or disappearance of decidual cells nuclei and absorption of embryos after the sc administration of L14105 5 mg/kg for 24～48 h. L14105 stimulated the contractile force of uterine smooth muscle in vivo or in vitro. Conclusion: L14105 shows a very high pregnancy terminating activity. Multiple oral administration is also effective. The mode of action of contragestation is related to damage of decidual cells and stimulation of uterine contractility.展开更多
文摘Two 2-aryl imidazo [2,1-a] isoquinolines were synthesized and tested for pregnancy terminating activities. Both of them are new compounds and their structures were confirmed by IR, (HNMR)-H-1, MS and elemental analysis. They both showed high activities in NIH mice.
文摘Contragestazolin (L14105) belongs to the class of 2 phenyl triazole isoquinolines. When given subcutaneously, intramuscularly or orally showed potential pregnancy terminating activity in mice, rats, hamsters and guinea pigs, but the dialy doses of oral administration needed were 7.1, 6.3 and 47.6 times (for mouse, rat and hamster) greater than those needed parenterally. L14105 had low affinity to rat uterine progesterone receptor. When cultured human decidual cells were exposed to L14105 0.077～0.155 mmol/L for 24～48 h, the cells' viability markedly dropped and structural changes occurred in comparison with controls. Histological examination of conceptuses of rats showed edema, degeneration, necrosis and atrophy or disappearance of decidual cells nuclei and absorption of embryos after the sc administration of L14105 5 mg/kg for 24～48 h. L14105 stimulated the contractile force of uterine smooth muscle in vivo or in vitro. Conclusion: L14105 shows a very high pregnancy terminating activity. Multiple oral administration is also effective. The mode of action of contragestation is related to damage of decidual cells and stimulation of uterine contractility.
