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2-氨基-7-膦酰庚酸(AP7)产生与地西泮相似的辨别性刺激和抗冲突效应。

2-Amino-7-phosphonoheptanoic acid (AP7) produces discriminative stimuli and anticonflict effects similar to diazepam.

作者信息

Bennett D A, Amrick C L

出版信息

Life Sci. 1986 Dec 22;39(25):2455-61. doi: 10.1016/0024-3205(86)90488-1.

Abstract

The N-methyl-D-aspartate (NMDA) receptor antagonist, AP7, was evaluated in two animal test procedures known to be sensitive to the effects of diazepam. In rats trained to discriminate diazepam from vehicle, AP7 produced dose-dependent generalization to the diazepam interoceptive stimuli. This NMDA antagonist also increased the rates of conflict responding in a chronic test procedure used to identify compounds with potential anxiolytic effects. A comparison of AP7 with diazepam and two muscle relaxants (methocarbamol and baclofen) showed that excitatory amino acid antagonists (of the receptor site stimulated by NMDA) produce a muscle relaxant effect (drug discrimination) and may represent a new class of compounds for the treatment of anxiety-related disorders (conflict test).

摘要

N-甲基-D-天冬氨酸(NMDA)受体拮抗剂AP7,在已知对安定作用敏感的两种动物试验程序中进行了评估。在经过训练以区分安定和赋形剂的大鼠中,AP7产生了对安定内感受性刺激的剂量依赖性泛化。这种NMDA拮抗剂在用于鉴定具有潜在抗焦虑作用化合物的慢性试验程序中,也增加了冲突反应的速率。将AP7与安定以及两种肌肉松弛剂(美索巴莫和巴氯芬)进行比较表明,(作用于NMDA刺激的受体位点的)兴奋性氨基酸拮抗剂会产生肌肉松弛作用(药物辨别),并且可能代表一类用于治疗焦虑相关障碍的新型化合物(冲突试验)。

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