Potential anxiolytic properties of R-(+)-8-OSO2CF3-PAT, a 5-HT1A receptor agonist
Potential anxiolytic properties of R-(+)-8-OSO2CF3-PAT, a 5-HT1A receptor agonist
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DOI：
10.1016/0014-2999(95)00782-2
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发表时间：
1996-02-22
影响因子：
5
通讯作者：
Wikstrom, H
中科院分区：
文献类型：
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作者：
Barf, T;Korte, SM;Wikstrom, H
研究了5-HT1A受体激动剂R-(+)-8-[[（三氟甲基）磺酰基]氧]-2-（正丙基氨基）四氢化萘(R-（+)-8-[[（三氟甲基）磺酰基]氧]-2-（正丙基氨基）四氢化萘）对Wistar大鼠的抗焦虑性，分别采用焦虑动物模型、条件性防御埋藏模型和条件性应激诱导冻结反应后升高的正迷宫撕裂模型，并研究了大鼠脑浆液5-HIAA/5-HT比值（5-羟基吲哚乙酸/5-羟色胺）。急性给药（3mg /kg i.p.）可使小鼠的掩埋行为消失，饲养量呈剂量依赖性减少，并诱导贪食。R-(+)8-OSO2CF3-PAT对条件足震诱导的冻结行为没有影响，但增加了正迷宫大鼠的张开臂活动，外侧隔区（1和3 mg/kg）、海马背区（3 mg/kg）和体感皮层（3 mg/kg）的5-HIAA/5-HT比值降低，表明R-(+)-8-OSO2CF3-PAT在焦虑诱导情况下特别影响边缘系统。
The anxiolytic property of R-(+)-8-OSO3CF3-PAT (R-(+)-8-[[(trifluoromethyl)sulfonyl]oxy]-2-(n-propyl-amino)tetralin), a 5-HT1A receptor agonist, was evaluated in Wistar rats by means of animal models of anxiety, the conditioned defensive burying model and the conditioned stress-induced freezing response followed by the elevated plus-maze tear, respectively, In addition, the 5-HIAA/5-HT ratio (5-hydroxy-indole acetic acid/5-hydroxytryptamine) of rat brain homogenates was studied. Acute drug administration resulted in abolition of the burying behaviour (3 mg/kg i.p.), a dose-dependent decrease of rearing and induction of hyperphagia. R-(+)8-OSO2CF3-PAT had no effect on conditioned footshock-induced freezing behaviour but increased open-arm activity in the rats on the plus-maze, The 5-HIAA/5-HT ratio was decreased in the lateral septum (1 and 3 mg/kg), dorsal hippocampus (3 mg/kg) and somatosensory cortex (3 mg/kg), implying that R-(+)-8-OSO2CF3-PAT affects particularly the limbic system in anxiety-inducing situations.