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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

Bernstein J R, Franklin R B

Department of Drug Disposition, Lilly Research Labs., Eli Lilly and Co., Indianapolis, IN 46285.

Xenobiotica. 1988 Dec;18(12):1335-45. doi: 10.3109/00498258809042258.

The metabolism and disposition of 14C-indolidan, a potent, orally-active positive inotrope with vasodilator properties, has been studied after single dose oral administration to rats, mice, dogs and monkeys. 2. Excretion of 14C in all 4 species was mostly via the urine, largely as parent drug together with two other major metabolites. 3. The two metabolites have been isolated and identified, by mass spectroscopy and 1H-n.m.r., as a dehydro-compound, with a double bond in the pyridazanone ring, and a hydroxylated derivative of the parent drug. 4. Plasma t 1/2 values, based on 14C, were 14 h in dog, 5 h in mouse and 8 h in monkey. Plasma t 1/2 of parent drug, by h.p.l.c. was 10 h in dog, approx. 5 h in rodents, and 8 h in monkeys. 5. Tissue distribution in rats showed no accumulation in any tissue; 14C concn. in all tissues were indistinguishable from background 48 h after dosage. 14C peaked at 6-8 h for most tissues but in blood and plasma, 14C was maximal 1 h after dosing.

对大鼠、小鼠、狗和猴子单次口服给药后，研究了14C-吲哚心安（一种具有血管舒张特性的强效口服活性正性肌力药）的代谢和处置情况。2. 所有4个物种中14C的排泄主要通过尿液，大部分以母体药物以及其他两种主要代谢物的形式排出。3. 这两种代谢物已通过质谱和1H-核磁共振分离并鉴定为一种在哒嗪酮环中有双键的脱氢化合物以及母体药物的羟基化衍生物。4. 基于14C的血浆半衰期值，狗为14小时，小鼠为5小时，猴子为8小时。通过高效液相色谱法测得的母体药物血浆半衰期，狗为10小时，啮齿动物约为5小时，猴子为8小时。5. 大鼠的组织分布显示在任何组织中均无蓄积；给药后48小时，所有组织中的14C浓度与本底无差异。大多数组织中的14C在6 - 8小时达到峰值，但在血液和血浆中，14C在给药后1小时达到最大值。

Bernstein J R, Franklin R B

Department of Drug Disposition, Lilly Research Labs., Eli Lilly and Co., Indianapolis, IN 46285.

Xenobiotica. 1988 Dec;18(12):1335-45. doi: 10.3109/00498258809042258.

The metabolism and disposition of 14C-indolidan, a potent, orally-active positive inotrope with vasodilator properties, has been studied after single dose oral administration to rats, mice, dogs and monkeys. 2. Excretion of 14C in all 4 species was mostly via the urine, largely as parent drug together with two other major metabolites. 3. The two metabolites have been isolated and identified, by mass spectroscopy and 1H-n.m.r., as a dehydro-compound, with a double bond in the pyridazanone ring, and a hydroxylated derivative of the parent drug. 4. Plasma t 1/2 values, based on 14C, were 14 h in dog, 5 h in mouse and 8 h in monkey. Plasma t 1/2 of parent drug, by h.p.l.c. was 10 h in dog, approx. 5 h in rodents, and 8 h in monkeys. 5. Tissue distribution in rats showed no accumulation in any tissue; 14C concn. in all tissues were indistinguishable from background 48 h after dosage. 14C peaked at 6-8 h for most tissues but in blood and plasma, 14C was maximal 1 h after dosing.

对大鼠、小鼠、狗和猴子单次口服给药后，研究了14C-吲哚心安（一种具有血管舒张特性的强效口服活性正性肌力药）的代谢和处置情况。2. 所有4个物种中14C的排泄主要通过尿液，大部分以母体药物以及其他两种主要代谢物的形式排出。3. 这两种代谢物已通过质谱和1H-核磁共振分离并鉴定为一种在哒嗪酮环中有双键的脱氢化合物以及母体药物的羟基化衍生物。4. 基于14C的血浆半衰期值，狗为14小时，小鼠为5小时，猴子为8小时。通过高效液相色谱法测得的母体药物血浆半衰期，狗为10小时，啮齿动物约为5小时，猴子为8小时。5. 大鼠的组织分布显示在任何组织中均无蓄积；给药后48小时，所有组织中的14C浓度与本底无差异。大多数组织中的14C在6 - 8小时达到峰值，但在血液和血浆中，14C在给药后1小时达到最大值。