Wedzony K, Czyrak A
Institute of Pharmacology, Polish Academy of Sciences, Kraków.
Brain Res. 1994 Sep 19;657(1-2):351-6. doi: 10.1016/0006-8993(94)90991-1.
In the present study, we investigated the role of corticosterone and glucocorticoid receptors in the acquisition of sensitization to locomotor stimulant effects of MK-801 in rats. MK-801 (two doses, 0.4 mg/kg i.p. each, given twice, 48 h apart) evoked sensitization, observed as enhancement of the locomotor activity to a challenging dose of MK-801 (0.4 mg/kg) but not of a stereotypy-like activity. Pharmacological manipulations which deplete endogenous corticosterone, i.e., administration of the corticosterone synthesis inhibitor metyrapone (two injections, 150 and 50 mg/kg, given at 24 and 2 h before the first injection of MK-801, 4 mg/kg) or blockade of glucocorticoid receptors by administration of the antiglucocorticoid RU 38486 (20 mg/kg, 45 min before MK-801, 0.4 mg/kg) abolished the acquisition of sensitization. The obtained results indicate that the endogenous corticosterone and glucocorticoid receptors (type II) are involved in the acquisition of sensitization to locomotor stimulant effects of MK-801. Final experiments showed that MK-801 in doses used in the present study (0.4 mg/kg) enhanced the plasma concentration of corticosterone and that single injection of exogenous corticosterone (10 mg/kg s.c.) enhanced the locomotor stimulant effects of MK-801 (0.2 mg/kg). The obtained data indicate that the acquisition of sensitization to locomotor stimulant effects of MK-801 involves secretion of corticosteroids which probably act through glucocorticoid receptors, as was found previously for amphetamine and its congeners.
在本研究中,我们调查了皮质酮和糖皮质激素受体在大鼠对MK-801运动刺激作用致敏反应形成过程中的作用。MK-801(两个剂量,每次腹腔注射0.4mg/kg,间隔48小时给药两次)诱发了致敏反应,表现为对挑战性剂量的MK-801(0.4mg/kg)运动活性增强,但刻板样活动未增强。消耗内源性皮质酮的药理学操作,即给予皮质酮合成抑制剂美替拉酮(两次注射,150mg/kg和50mg/kg,在首次注射4mg/kg MK-801前24小时和2小时给药)或通过给予抗糖皮质激素RU 38486(20mg/kg,在注射0.4mg/kg MK-801前45分钟)阻断糖皮质激素受体,均消除了致敏反应的形成。所得结果表明,内源性皮质酮和糖皮质激素受体(II型)参与了对MK-801运动刺激作用致敏反应的形成。最终实验表明,本研究中使用的剂量(0.4mg/kg)的MK-801提高了皮质酮的血浆浓度,单次皮下注射外源性皮质酮(10mg/kg)增强了MK-801(0.2mg/kg)的运动刺激作用。所得数据表明,对MK-801运动刺激作用致敏反应的形成涉及皮质类固醇的分泌,其可能通过糖皮质激素受体发挥作用,这与先前对苯丙胺及其同系物的研究结果一致。