Scapagnini U, Matera M
Institute of Pharmacology, University of Catania, Italy.
Arzneimittelforschung. 1997 Nov;47(11A):1310-4.
The effect of pivagabine (4-[(2,2-dimethyl-1-oxopropyl)amino]butanoic acid, CAS 69542-93-4, Tonerg), a synthetic molecule with neuromodulatory activity, was evaluated on a series of behavioural parameters in rats exposed to various stimuli, with the aim of evaluating the response to stress (open field exploration, water maze, psychic conflict), conditioning (active and passive avoidance and avoidance retention, aggressiveness, extinction of conditioned responses), learning and performing of specific psychophysical tests (rota-rod, ballasted swimming, taut thread). Pivagabine induced significant improvement of stress-related tests by reducing the anxiety-producing reactions related to the various experimental settings. In conditioning tests an improvement in learning of conditioned responses was observed at lower dosages (10 and 50 mg/kg); an opposite effect was obtained with higher dosages (100 and 200 mg/kg). Pivagabine did not influence the retention nor the extinction of conditioned responses. Pivagabine induced a marked improvement of all motor performance tests in young and in aged animals. By contrast with benzodiazepines, pivagabine did not alter the ability of learning tasks, the motor performance and the aggressive behaviours. It is likely that the observed effects of pivagabine are mediated by inhibition of release of corticotropin-releasing factor, a neurohormone involved in stress-generating mechanisms.
对具有神经调节活性的合成分子匹伐加宾（4-[(2,2-二甲基-1-氧代丙基)氨基]丁酸，化学物质登记号69542-93-4，商品名Tonerg）进行了评估，观察其对暴露于各种刺激下的大鼠一系列行为参数的影响，目的是评估其对应激（旷场探索、水迷宫、心理冲突）、条件反射（主动和被动回避及回避保持、攻击性、条件反应消退）、特定心理物理测试（转棒试验、负重游泳、悬线试验）的学习和执行的反应。匹伐加宾通过减少与各种实验环境相关的焦虑产生反应，显著改善了与应激相关的测试。在条件反射测试中，较低剂量（10和50毫克/千克）时观察到条件反应学习有所改善；较高剂量（100和200毫克/千克）时则得到相反的效果。匹伐加宾不影响条件反应的保持和消退。匹伐加宾使幼年和老年动物的所有运动性能测试都有显著改善。与苯二氮䓬类药物不同，匹伐加宾不改变学习任务的能力、运动性能和攻击行为。匹伐加宾观察到的效应可能是通过抑制促肾上腺皮质激素释放因子的释放介导的，促肾上腺皮质激素释放因子是一种参与应激产生机制的神经激素。
