慢性新斯的明治疗对大鼠膈肌乙酰胆碱受体数量及乙酰胆碱释放的影响。

Influence of chronic neostigmine treatment on the number of acetylcholine receptors and the release of acetylcholine from the rat diaphragm.

Chang C C, Chen T F, Chuang S T

J Physiol. 1973 May;230(3):613-8. doi: 10.1113/jphysiol.1973.sp010207.

Abstract

Rats were treated twice daily for 7 days with neostigmine and the diaphragm was isolated for study of its acetylcholine content, release upon nerve stimulation and the number of receptors in the end-plate.2. While the content of total acetylcholine was unchanged, the release of acetylcholine on stimulation with trains of 500 pulses at 100 Hz every 20 sec was reduced by about 50%. Five days after the end of neostigmine treatment the release of acetylcholine recovered to normal.3. The total number of acetylcholine receptors in the end-plate as measured from the binding of N, O-di[(3)H]acetyl alpha-bungarotoxin was reduced from 2.1 x 10(7) to 1.2 x 10(7) per end-plate.4. The above-mentioned changes are not due to acute pharmacological effects of neostigmine, nor to an immediate effect of cholinesterase inhibition but presumably due to chronic accumulation of acetylcholine at the neuromuscular junction.

摘要

用新斯的明对大鼠每日进行两次治疗，持续7天，然后分离膈肌以研究其乙酰胆碱含量、神经刺激时的释放量以及终板中的受体数量。
虽然总乙酰胆碱含量未变，但每隔20秒以100Hz频率给予500次脉冲串刺激时，乙酰胆碱的释放量减少了约50%。新斯的明治疗结束五天后，乙酰胆碱的释放量恢复正常。
根据N，O-二[（3）H]乙酰α-银环蛇毒素的结合情况测定，终板中乙酰胆碱受体的总数从每个终板2.1×10（7）减少到1.2×10（7）。
上述变化并非由于新斯的明的急性药理作用，也不是由于胆碱酯酶抑制的即时效应，而是可能由于乙酰胆碱在神经肌肉接头处的慢性蓄积。