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γ-氨基丁酸和乙二胺对豚鼠十二指肠的影响。

Influence of GABA and ethylenediamine in the guinea-pig duodenum.

作者信息

Barbier A J, Guenaneche F, Lefebvre R A

机构信息

Heymans Institute of Pharmacology, University of Gent Medical School, Belgium.

出版信息

J Auton Pharmacol. 1989 Aug;9(4):279-91. doi: 10.1111/j.1474-8673.1989.tb00218.x.

Abstract
  1. GABA induced concentration-dependent transient contractions of the guinea-pig duodenum, but only occasionally evoked small relaxatory responses. The GABA-induced contractions were blocked by atropine and tetrodotoxin but were not influenced by hexamethonium; during electrically evoked twitch contractions, GABA had a concentration-dependent inhibitory effect. 2. The concentration-response curve for the contractile effect of GABA was shifted to the right in a dose-dependent manner by bicuculline and picrotoxin, with a clear reduction of the maximal effect in the presence of picrotoxin. 3. Homotaurine and delta-aminovaleric acid but not baclofen mimicked the GABA-induced contractions; the responses induced by these GABAA receptor agonists were antagonized by atropine, tetrodotoxin and bicuculline. Baclofen concentration-dependently inhibited electrically evoked twitch contractions. 4. Ethylenediamine also had a GABA-like effect, and cross-desensitization developed between GABA and ethylenediamine. 5. The ethylenediamine-induced contractions were not antagonized by thiosemicarbazide; they were reduced by 3-mercaptopropionic acid but the GABA-induced contractions were reduced to the same extent. 6. It is concluded that GABA induces contraction of the guinea-pig duodenum by excitation of GABAA receptors on postganglionic cholinergic neurones; a GABAB receptor-mediated inhibitory effect can be observed during electrically evoked twitch contractions. Ethylenediamine mimicks the GABAA receptor-mediated effect probably by a direct effect on the GABAA receptors.
摘要
  1. γ-氨基丁酸(GABA)可引起豚鼠十二指肠浓度依赖性的短暂收缩,但仅偶尔诱发小幅度的舒张反应。GABA诱导的收缩可被阿托品和河豚毒素阻断,但不受六甲铵影响;在电诱发的抽搐收缩过程中,GABA具有浓度依赖性的抑制作用。2. 荷包牡丹碱和印防己毒素可使GABA收缩效应的浓度-反应曲线呈剂量依赖性右移,在印防己毒素存在时最大效应明显降低。3. 高牛磺酸和δ-氨基戊酸可模拟GABA诱导的收缩,而巴氯芬则不能;这些GABAA受体激动剂诱导的反应可被阿托品、河豚毒素和荷包牡丹碱拮抗。巴氯芬浓度依赖性地抑制电诱发的抽搐收缩。4. 乙二胺也具有类似GABA的作用,且GABA与乙二胺之间会产生交叉脱敏。5. 乙二胺诱导的收缩不被氨基硫脲拮抗;它们可被3-巯基丙酸减弱,但GABA诱导的收缩也会减弱到相同程度。6. 得出结论:GABA通过兴奋节后胆碱能神经元上的GABAA受体诱导豚鼠十二指肠收缩;在电诱发的抽搐收缩过程中可观察到GABAB受体介导的抑制作用。乙二胺可能通过直接作用于GABAA受体来模拟GABAA受体介导的效应。

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