Microwave facilitation of methylatropine antagonism of central cholinomimetic drug effects.
Microwave facilitation of methylatropine antagonism of central cholinomimetic drug effects.
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微波促进甲基阿托品拮抗中枢拟胆碱药物的作用。
DOI：
10.2307/3576689
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发表时间：
1986
影响因子：
3.4
通讯作者：
D. Lange
中科院分区：
文献类型：
--
作者：
R. Quock;J. Fujimoto;T. Ishii;D. Lange
毛果芸香碱诱导的低温和氧震颤素诱导的小鼠震颤是中枢拟胆碱药物作用，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不能穿透血脑屏障（BBB）和血脑脊髓液屏障（B-CSFB）而不能阻断这些拟胆碱药物作用。毛果芸香碱和oxotremorine效应的剂量-反应曲线没有明显的影响，无论是预处理甲基阿托品（1.0毫克/公斤）或暴露于中等水平的微波照射（2.45千兆赫，23.7 W/kg，连续波，10分钟曝光）。然而，在接受甲基阿托品预处理和微波照射的小鼠中，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，表明甲基阿托品具有中枢抗胆碱能作用。这些数据表明，一个单一的急性暴露于产热水平的微波辐射促进甲基阿托品拮抗中枢介导的拟胆碱药物的作用。对这一观察结果的一个可能的解释是，微波辐射可以增强季铵化合物如甲基阿托品穿过BBB和B-CSFB的通道。
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.