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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

Yoshimura T, Tanaka S, Sakurai H, Nagai Y, Yamada K, Katayama S, Abe S, Yamatsu I

Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.

Xenobiotica. 1991 May;21(5):627-34. doi: 10.3109/00498259109039502.

The 5-lipoxygenase inhibitor (I), a substituted benzothiazole is metabolized mainly by glucuronide and/or sulphate conjugation in rat, guinea-pig, beagle and rhesus monkey. Glucuronidation is the major pathway, and sulphation is more extensive in rat and beagle than in guinea-pig and rhesus monkey. 2. After a single oral dosing of 14C-I (10 mg/kg), more than 96% of the dose was excreted in 7 days in all four species, however there is species difference in urinary excretion, which was 2.8 +/- 0.3% in rat, 46.9 +/- 1.6% in guinea-pig, 2.6% in beagle and 68.2% in rhesus monkey. 3. After a single i.v. dose of 14C-I to bile duct-cannulated rats and guinea pigs, bile was a major route of elimination, and in rats the ratio of glucuronide to sulphate in excreta increased from 0.71 +/- 0.01 to 0.93 +/- 0.05 as the dose was increased from 0.2 to 20 mg/kg.

5-脂氧合酶抑制剂（I），一种取代苯并噻唑，在大鼠、豚鼠、比格犬和恒河猴体内主要通过葡萄糖醛酸化和/或硫酸化结合进行代谢。葡萄糖醛酸化是主要途径，硫酸化在大鼠和比格犬中比在豚鼠和恒河猴中更广泛。2. 单次口服给予14C-I（10mg/kg）后，在所有四个物种中，超过96%的剂量在7天内排出，但尿排泄存在物种差异，大鼠为2.8±0.3%，豚鼠为46.9±1.6%，比格犬为2.6%，恒河猴为68.2%。3. 对胆管插管的大鼠和豚鼠单次静脉注射14C-I后，胆汁是主要的消除途径，在大鼠中，随着剂量从0.2mg/kg增加到20mg/kg，排泄物中葡萄糖醛酸与硫酸盐的比例从0.71±0.01增加到0.93±0.05。

Yoshimura T, Tanaka S, Sakurai H, Nagai Y, Yamada K, Katayama S, Abe S, Yamatsu I

Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.

Xenobiotica. 1991 May;21(5):627-34. doi: 10.3109/00498259109039502.

The 5-lipoxygenase inhibitor (I), a substituted benzothiazole is metabolized mainly by glucuronide and/or sulphate conjugation in rat, guinea-pig, beagle and rhesus monkey. Glucuronidation is the major pathway, and sulphation is more extensive in rat and beagle than in guinea-pig and rhesus monkey. 2. After a single oral dosing of 14C-I (10 mg/kg), more than 96% of the dose was excreted in 7 days in all four species, however there is species difference in urinary excretion, which was 2.8 +/- 0.3% in rat, 46.9 +/- 1.6% in guinea-pig, 2.6% in beagle and 68.2% in rhesus monkey. 3. After a single i.v. dose of 14C-I to bile duct-cannulated rats and guinea pigs, bile was a major route of elimination, and in rats the ratio of glucuronide to sulphate in excreta increased from 0.71 +/- 0.01 to 0.93 +/- 0.05 as the dose was increased from 0.2 to 20 mg/kg.

5-脂氧合酶抑制剂（I），一种取代苯并噻唑，在大鼠、豚鼠、比格犬和恒河猴体内主要通过葡萄糖醛酸化和/或硫酸化结合进行代谢。葡萄糖醛酸化是主要途径，硫酸化在大鼠和比格犬中比在豚鼠和恒河猴中更广泛。2. 单次口服给予14C-I（10mg/kg）后，在所有四个物种中，超过96%的剂量在7天内排出，但尿排泄存在物种差异，大鼠为2.8±0.3%，豚鼠为46.9±1.6%，比格犬为2.6%，恒河猴为68.2%。3. 对胆管插管的大鼠和豚鼠单次静脉注射14C-I后，胆汁是主要的消除途径，在大鼠中，随着剂量从0.2mg/kg增加到20mg/kg，排泄物中葡萄糖醛酸与硫酸盐的比例从0.71±0.01增加到0.93±0.05。