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1,2,3,4-四氢-β-咔啉和6-甲氧基-1,2,3,4-四氢-β-咔啉在小鼠体内的分布。

Distribution of 1,2,3,4-tetrahydro-beta-carboline and 6-methoxy-1,2,3,4-tetrahydro-beta-carboline in mice.

作者信息

Leino M, Airaksinen M M, Antikainen R, Gynther J, Kari E, Kari I, Peura P

出版信息

Acta Pharmacol Toxicol (Copenh). 1984 May;54(5):361-71. doi: 10.1111/j.1600-0773.1984.tb01943.x.

Abstract

The distribution of radioactivity after intravenous injection of 14C-labelled 1,2,3,4-tetrahydro-beta-carboline (THBC) and 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-MeO-THBC) was studied on mice by whole-body autoradiography and by liquid scintillation counting (LSC). Following intravenous injection they rapidly distributed into different organs and were excreted into urine and the gut contents. A considerable uptake of the compounds was seen in the lungs, kidney, liver, bone marrow, urinary bladder, gastrointestinal tract and in various glands e.g. adrenal, Harderian and salivary glands. THBC moderately penetrated the blood-brain barrier and the placenta but 6-MeO-THBC seemed to penetrate poorly both. At early stages of the experiment the values of tissue radioactivity in LSC were generally much higher in the THBC group but 24 hours following injections the reverse was true with higher activities in the 6-MeO-THBC group. The initial excretion of 6-MeO-THBC seemed to be more rapid judged by the superfluous accumulation of activity in the bladder and a high accumulation of activity into the gut contents.

摘要

通过全身放射自显影和液体闪烁计数(LSC)研究了静脉注射14C标记的1,2,3,4-四氢-β-咔啉(THBC)和6-甲氧基-1,2,3,4-四氢-β-咔啉(6-MeO-THBC)后在小鼠体内的放射性分布。静脉注射后,它们迅速分布到不同器官,并排泄到尿液和肠道内容物中。在肺、肾、肝、骨髓、膀胱、胃肠道以及各种腺体(如肾上腺、哈德氏腺和唾液腺)中观察到这些化合物有相当程度的摄取。THBC能适度穿透血脑屏障和胎盘,但6-MeO-THBC似乎两者穿透性都很差。在实验早期,LSC中组织放射性的值在THBC组通常要高得多,但注射后24小时情况相反,6-MeO-THBC组的活性更高。从膀胱中活性的多余积累以及肠道内容物中活性的高积累判断,6-MeO-THBC的初始排泄似乎更快。

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