Ylitalo P, Lindén I B, Penttilä A, Vapaatalo H
Acta Pharmacol Toxicol (Copenh). 1986 Jan;58(1):84-7. doi: 10.1111/j.1600-0773.1986.tb00074.x.
The distribution into cerebrospinal fluid (CSF) of five 3H- or 14C-labelled beta-adrenoceptor blocking drugs given intravenously was studied in urethane-anaesthetized rats. The doses (mg/kg) were: alprenolol 5, metoprolol 1, oxprenolol 5, pindolol 0.5, propranolol 0.1 and 5. Within 15 min. a marked fraction of the given radioactivity appeared in CSF with all substances. During the follow-up period of 315 min., only propranolol, independently of dose, caused high CSF/plasma ratios (0.54-0.73) of radioactivity. The other four beta-adrenoceptor blocking drugs caused levels of CSF radioactivity which were 0.05-0.28 of that in plasma and 0.05-0.14 of the calculated levels of activity in the whole body. Since propranolol is bound to plasma proteins to a higher degree than the other drugs studied, the penetration of the unbound fraction of propranolol into rat CSF is even more pronounced than what would be expected on the basis of CSF/plasma ratio measured.
在氨基甲酸乙酯麻醉的大鼠中，研究了静脉注射五种3H或14C标记的β-肾上腺素受体阻断药物在脑脊液（CSF）中的分布情况。给药剂量（mg/kg）分别为：阿普洛尔5、美托洛尔1、氧烯洛尔5、吲哚洛尔0.5、普萘洛尔0.1和5。在15分钟内，所有物质的给药放射性中都有相当一部分出现在脑脊液中。在315分钟的随访期内，只有普萘洛尔，无论剂量如何，都会导致脑脊液与血浆的放射性比值较高（0.54 - 0.73）。其他四种β-肾上腺素受体阻断药物导致的脑脊液放射性水平为血浆中的0.05 - 0.28，以及全身计算活性水平的0.05 - 0.14。由于普萘洛尔与血浆蛋白的结合程度高于所研究的其他药物，普萘洛尔未结合部分进入大鼠脑脊液的情况比根据测量的脑脊液/血浆比值预期的更为明显。
