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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Ono K, Saito T, Sasano H, Moroi R, Sano M, Akimoto T

Xenobiotica. 1979 Apr;9(4):227-36. doi: 10.3109/00498257909038725.

[14C]Budralazine (I) administered orally to normotensive and spontaneously hypertensive rats showed no significant difference in metabolic fate between the two groups. 2. Peak plasma levels of 14C were 3.6 microgram equiv. of I per ml in both normotensive and hypertensive rats. Approx. 5% of total 14C in the plasma consisted of I within 4 h, but thereafter the parent drug was not detected. Approx. 15% of 14C in the plasma consisted of 1-hydrazinophthalazine within 16 h after the administration. 3. 45% and 37% of the dose of 14C was excreted into urine and faeces within 24 h, respectively. 4. A high retention of 14C in the aorta wall was found and the time course of 14C in the aorta wall was compatible with that of the reduction in blood pressure. The radioactive materials retained in the aorta wall were likely to be I or 1-hydrazinophthalazine, probably the latter, following macroautoradiography in hypertensive rats.

给正常血压大鼠和自发性高血压大鼠口服[14C]布屈嗪（I）后，两组之间的代谢命运无显著差异。2. 正常血压大鼠和高血压大鼠血浆中14C的峰值水平均为每毫升3.6微克当量的I。约5%的血浆中总14C在4小时内由I组成，但此后未检测到母体药物。给药后16小时内，血浆中约15%的14C由1-肼基酞嗪组成。3. 24小时内，14C剂量的45%和37%分别排泄到尿液和粪便中。4. 发现主动脉壁中14C有高度滞留，主动脉壁中14C的时间进程与血压降低的时间进程一致。在高血压大鼠中进行宏观放射自显影后，保留在主动脉壁中的放射性物质可能是I或1-肼基酞嗪，可能是后者。

Ono K, Saito T, Sasano H, Moroi R, Sano M, Akimoto T

Xenobiotica. 1979 Apr;9(4):227-36. doi: 10.3109/00498257909038725.

[14C]Budralazine (I) administered orally to normotensive and spontaneously hypertensive rats showed no significant difference in metabolic fate between the two groups. 2. Peak plasma levels of 14C were 3.6 microgram equiv. of I per ml in both normotensive and hypertensive rats. Approx. 5% of total 14C in the plasma consisted of I within 4 h, but thereafter the parent drug was not detected. Approx. 15% of 14C in the plasma consisted of 1-hydrazinophthalazine within 16 h after the administration. 3. 45% and 37% of the dose of 14C was excreted into urine and faeces within 24 h, respectively. 4. A high retention of 14C in the aorta wall was found and the time course of 14C in the aorta wall was compatible with that of the reduction in blood pressure. The radioactive materials retained in the aorta wall were likely to be I or 1-hydrazinophthalazine, probably the latter, following macroautoradiography in hypertensive rats.

给正常血压大鼠和自发性高血压大鼠口服[14C]布屈嗪（I）后，两组之间的代谢命运无显著差异。2. 正常血压大鼠和高血压大鼠血浆中14C的峰值水平均为每毫升3.6微克当量的I。约5%的血浆中总14C在4小时内由I组成，但此后未检测到母体药物。给药后16小时内，血浆中约15%的14C由1-肼基酞嗪组成。3. 24小时内，14C剂量的45%和37%分别排泄到尿液和粪便中。4. 发现主动脉壁中14C有高度滞留，主动脉壁中14C的时间进程与血压降低的时间进程一致。在高血压大鼠中进行宏观放射自显影后，保留在主动脉壁中的放射性物质可能是I或1-肼基酞嗪，可能是后者。