罂粟碱的代谢。II. 种属差异。

Metabolism of papaverine. II. Species differences.

Belpaire F M, Bogaert M G

Xenobiotica. 1975 Jul;5(7):421-9. doi: 10.3109/00498257509056112.

Abstract

The urinary and biliary excretion of radioactive products in a 6 hr period after intravenous administration of [3H]papaverine was studied in rat, guinea-pig, rabbit, cat and dog. All species excreted metabolites extensively in the bile; only in rabbit and guinea-pig is urinary excretion important. 2. Metabolites in urine and bile of all species studied are mainly monophenolic compounds conjugated to glucuronic or sulphuric acid. Differences in the excretion patterns of the metabolites between different species are only quantitative. 3. Blood or plasma levels of papaverine after intravenous injection decreased with half-lives of approximately 12, 15, 22, 60 and 60 min for rabbit, rat, guinea-pig, cat and dog, respectively. The metabolites disappeared much more slowly than papaverine from the plasma. 4. Binding of papaverine to plasma proteins, as studied by equilibrium dialysis, was more than 90% in all species.

摘要

在大鼠、豚鼠、兔子、猫和狗静脉注射[3H]罂粟碱后的6小时内，研究了放射性产物的尿排泄和胆汁排泄情况。所有物种都在胆汁中大量排泄代谢物；只有兔子和豚鼠的尿排泄较为重要。2. 所有研究物种的尿液和胆汁中的代谢物主要是与葡萄糖醛酸或硫酸结合的单酚类化合物。不同物种之间代谢物排泄模式的差异只是数量上的。3. 静脉注射后，兔子、大鼠、豚鼠、猫和狗的罂粟碱血药或血浆水平下降，半衰期分别约为12、15、22、60和60分钟。代谢物从血浆中消失的速度比罂粟碱慢得多。4. 通过平衡透析研究，罂粟碱与血浆蛋白的结合在所有物种中均超过90%。