大鼠肛门尾骨肌中的突触前γ-氨基丁酸受体及其被5-氨基戊酸的拮抗作用。
Presynaptic gamma-aminobutyric acid receptors in the rat anococcygeus muscle and their antagonism by 5-aminovaleric acid.
作者信息
Muhyaddin M, Roberts P J, Woodruff G N
出版信息
Br J Pharmacol. 1982 Sep;77(1):163-8. doi: 10.1111/j.1476-5381.1982.tb09282.x.
Abstract
1 The effects of gamma-aminobutyric acid (GABA) and related drugs on the isolated anococcygeus muscle of the rat were determined. 2 GABA caused a dose-related inhibition of the electrically-evoked twitch response. 3 The maximum response to GABA was a 56.8% depression of twitch response, with an EC50 of 0.68 microM. 4 (+/-)-Baclofen mimicked the effect of GABA (EC50 0.9 microM). (+)-Baclofen was more than 100 times less active than (--)-baclofen. 5 The response to GABA was unaffected by picrotoxin or bicuculline but was antagonized by 5-aminovaleric acid (0.5) mM). 6 Our results suggest that GABAB receptors are present on motor nerve terminals in the rat anococcygeus muscle and that 5-aminovaleric acid is an antagonist of these receptors.
摘要
测定了γ-氨基丁酸（GABA）及相关药物对大鼠离体尾骨肌的作用。
GABA引起电诱发抽搐反应的剂量相关抑制。
对GABA的最大反应是抽搐反应降低56.8%，半数有效浓度（EC50）为0.68微摩尔。
（±）-巴氯芬模拟了GABA的作用（EC50为0.9微摩尔）。（+）-巴氯芬的活性比（-）-巴氯芬低100多倍。
对GABA的反应不受印防己毒素或荷包牡丹碱影响，但被5-氨基戊酸（0.5毫摩尔）拮抗。
我们的结果表明，大鼠尾骨肌运动神经末梢存在GABAB受体，且5-氨基戊酸是这些受体的拮抗剂。
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