Moor M, Honegger U E, Wiesmann U N
Department of Pharmacology, University of Bern, Switzerland.
Biochem Pharmacol. 1988 May 15;37(10):2035-9. doi: 10.1016/0006-2952(88)90553-9.
Rats were chronically treated with daily i.p. injections of 10 mg/kg desipramine for 21 days. A 30% decrease in the number of beta-adrenoceptors was observed in brain. A receptor desensitization of similar extent was noted in submaxillary glands and lung. No change in beta-adrenoceptor number was present in heart. Total phospholipid contents were not altered in these organs after chronic drug treatment. However, organ-specific changes were found in the phospholipid composition of submaxillary glands, lung and liver but not in whole brain and heart. The changes were variable but an increase in phosphatidylinositol and decreases in phosphatidylethanolamine and sphingomyelin were consistent. Possible alterations in the phospholipid composition of the brain might have been masked by the large and stable pool of myelin phospholipids. A casual relationship between changes in the phospholipid composition and beta-adrenoceptor desensitization is discussed.
大鼠连续21天每天腹腔注射10毫克/千克地昔帕明进行长期治疗。在大脑中观察到β-肾上腺素能受体数量减少了30%。在颌下腺和肺中也发现了类似程度的受体脱敏现象。心脏中的β-肾上腺素能受体数量没有变化。长期药物治疗后，这些器官中的总磷脂含量没有改变。然而，在颌下腺、肺和肝脏的磷脂组成中发现了器官特异性变化，而在全脑和心脏中未发现。这些变化各不相同，但磷脂酰肌醇增加、磷脂酰乙醇胺和鞘磷脂减少是一致的。大脑磷脂组成的可能变化可能被大量稳定的髓鞘磷脂库所掩盖。讨论了磷脂组成变化与β-肾上腺素能受体脱敏之间的偶然关系。
