Curtis M T, Lefer A M
Arch Int Pharmacodyn Ther. 1982 Jan;255(1):48-58.
Tissue uptake and plasma levels of 3H-naloxone were studied in normotensive control cats, as well as in hemorrhagic hypotensive cats. Intravenous injection of naloxone resulted in a rapid and extensive uptake of naloxone label from plasma by several tissues. Plasma half-life of the radiolabel was determined to be 137 min. One and two hours after injection, large amounts of naloxone label were found in the liver, pancreas, adrenal, kidney and lung, with tissue/plasma ratios ranging from 2 to 30. Brain tissue displayed the lowest tissue/plasma ratios of any organ sampled. Infusion of 8 mg/kg -1.hr-1 naloxone resulted in an increase in concentration of radiolabel over a 2 hr period. Hemorrhagic shock did not significantly retard uptake of naloxone by tissues. Splanchnic organs displayed high uptake of naloxone even during hemorrhagic shock. Brain tissue in cats subjected to hemorrhagic shock had the lowest uptake naloxone of all tissues sampled. The degree of uptake of naloxone by tissues is consistent with its proposed role in lysosomal membrane stabilization and prevention of proteolysis during hemorrhagic shock.
在血压正常的对照猫以及失血性低血压猫中研究了3H-纳洛酮的组织摄取和血浆水平。静脉注射纳洛酮导致几种组织迅速且广泛地从血浆中摄取纳洛酮标记物。放射性标记物的血浆半衰期测定为137分钟。注射后1小时和2小时，在肝脏、胰腺、肾上腺、肾脏和肺中发现大量纳洛酮标记物，组织/血浆比值在2至30之间。在所有采样器官中，脑组织的组织/血浆比值最低。以8mg/kg -1·hr-1的速度输注纳洛酮导致放射性标记物浓度在2小时内增加。失血性休克并未显著阻碍组织对纳洛酮的摄取。即使在失血性休克期间，内脏器官对纳洛酮的摄取也很高。遭受失血性休克的猫的脑组织在所有采样组织中对纳洛酮的摄取最低。组织对纳洛酮的摄取程度与其在失血性休克期间溶酶体膜稳定和防止蛋白水解中所起的作用一致。
