Quock R M, Fujimoto J M, Ishii T K, Lange D G
Radiat Res. 1986 Mar;105(3):328-40.
Pilocarpine-induced hypothermia and oxotremorine-induced tremors in mice are central cholinomimetic drug effects that are readily blocked by the muscarinic antagonist atropine. However, the quaternary ammonium derivative of atropine, methylatropine, is unable to block these cholinomimetic drug effects by virture of its inability to penetrate the blood-brain barrier (BBB) and blood-cerebral spinal fluid barrier (B-CSFB). Dose-response curves for pilocarpine and oxotremorine effects are not appreciably affected either by pretreatment with methylatropine (1.0 mg/kg) or by exposure to moderate-level microwave irradiation (2.45 GHz, 23.7 W/kg, CW, 10-min exposure). However, in mice receiving both the methylatropine pretreatment and microwave irradiation, the dose-response curves for both pilocarpine and oxotremorine effects were significantly shifted to the right, signifying a central anticholinergic action by methylatropine. These data indicate that a single acute exposure to a thermogenic level of microwave irradiation facilitates methylatropine antagonism of centrally mediated cholinomimetic drug effects. One possible explanation for this observation is that microwave radiation may enhance passage of quaternary ammonium compounds like methylatropine across the BBB and B-CSFB.
毛果芸香碱诱发的小鼠体温过低和氧化震颤素诱发的小鼠震颤是中枢拟胆碱药物效应,很容易被毒蕈碱拮抗剂阿托品阻断。然而,阿托品的季铵衍生物甲基阿托品由于无法穿透血脑屏障(BBB)和血脑脊髓液屏障(B-CSFB),因而无法阻断这些拟胆碱药物效应。毛果芸香碱和氧化震颤素效应的剂量-反应曲线,无论是用甲基阿托品(1.0毫克/千克)预处理,还是暴露于中等水平的微波辐射(2.45吉赫兹,23.7瓦/千克,连续波,照射10分钟),均未受到明显影响。然而,在同时接受甲基阿托品预处理和微波辐射的小鼠中,毛果芸香碱和氧化震颤素效应的剂量-反应曲线均显著右移,这表明甲基阿托品具有中枢抗胆碱能作用。这些数据表明,单次急性暴露于产热水平的微波辐射可促进甲基阿托品对中枢介导的拟胆碱药物效应的拮抗作用。对此观察结果的一种可能解释是,微波辐射可能会增强甲基阿托品等季铵化合物穿过血脑屏障和血脑脊髓液屏障的能力。