PHARMACOLOGICAL RELEVANCE OF PERIPHERAL-TYPE BENZODIAZEPINE RECEPTORS ON MOTOR-NERVE AND SKELETAL-MUSCLE

PHARMACOLOGICAL RELEVANCE OF PERIPHERAL-TYPE BENZODIAZEPINE RECEPTORS ON MOTOR-NERVE AND SKELETAL-MUSCLE
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DOI:
10.1111/j.1476-5381.1994.tb13060.x
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发表时间:
1994-05-01
影响因子:
7.3
通讯作者:
CHANG, CC
CHANG, CC
中科院分区:
医学2区
文献类型:
--
作者:
CHIOU, LC;CHANG, CC

文献摘要

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1 在小鼠离体膈神经隔膜制剂中研究了外周和中枢苯二氮卓受体激动剂和拮抗剂(pBZR 和 cBZR)对神经肌肉传递的影响。2 pBZR 激动剂 Ro5-4864 对神经肌肉传递没有影响,但增加了肌肉收缩力并拮抗由 新斯的明。3 Ro5-4864 抑制新斯的明存在下重复刺激引起的再生强直终板去极化,而不影响微型和诱发的单终板电位的振幅和衰减时间。4 Ro5-4864 的所有作用均由 pBZR 拮抗剂 PK11195 共享,但不由氯硝西泮和氟马西尼(a)共享。 cBZR 分别为激动剂和拮抗剂。5 表明外周型苯二氮卓受体可调节突触前功能和肌肉收缩。
1 Effects of agonists and antagonists of peripheral and central benzodiazepine receptors (pBZR and cBZR) on neuromuscular transmission were studied in mouse isolated phrenic nerve-diaphragm preparations.2 Ro5-4864, a pBZR agonist, had no effect on the neuromuscular transmission but increased muscle contractility and antagonized the tetanic fade induced by neostigmine.3 Ro5-4864 inhibited the regenerative tonic endplate depolarization caused by repetitive stimulation in the presence of neostigmine without affecting the amplitude and decay time of miniature and evoked single endplate potentials.4 All the effects of Ro5-4864 were shared by PK11195, a pBZR antagonist, but not by clonazepam and flumazenil, a cBZR agonist and antagonist, respectively.5 It is suggested that peripheral type benzodiazepine receptors modulate presynaptic function and muscle contraction.