LOSS OF M2 MUSCARINE RECEPTORS IN THE CEREBRAL-CORTEX IN ALZHEIMERS-DISEASE AND EXPERIMENTAL CHOLINERGIC DENERVATION
LOSS OF M2 MUSCARINE RECEPTORS IN THE CEREBRAL-CORTEX IN ALZHEIMERS-DISEASE AND EXPERIMENTAL CHOLINERGIC DENERVATION
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DOI：
10.1126/science.3992249
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发表时间：
1985-01-01
期刊：
影响因子：
56.9
通讯作者：
POTTER, LT
中科院分区：
文献类型：
--
作者：
MASH, DC;FLYNN, DD;POTTER, LT
从阿尔茨海默病患者和实验性胆碱能去神经症大鼠的大脑皮层样本中，发现突触前标志物胆碱乙酰转移酶活性和M2受体数量减少，而M1受体的数量没有变化。这些结果与M2受体在胆碱能神经末梢调节乙酰胆碱释放的证据一致，而M1受体位于突触后细胞并促进细胞兴奋。针对突触后或突触前部位的新型M1选择性激动剂和M2选择性拮抗剂值得考虑作为潜在的治疗药物。
Cerebral cortex samples from patients with Alzheimer''s disease and from rats after experimental cholinergic denervation of the cerebral cortex exhibited reductions in the presynaptic marker choline acetyltransferase activity and in the number of M2 muscarine receptors, with no change in the number of M1 receptors. These results are in keeping with evidence that M2 receptors function in cholinergic nerve terminals to regulate the release of acetylcholine, whereas M1 receptors are located on postsynaptic cells and facilitate cellular excitation. New M1-selective agonists and M2-selective antagonists directed at post- or presynaptic sites deserve consideration as potential agents for the treatment of the disease.