Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Rajasthan, India.
Indian J Pharmacol. 2013 Jul-Aug;45(4):348-53. doi: 10.4103/0253-7613.115014.
The present study was designed to investigate the antidepressant potential of N-n-butyl-3-ethoxyquinoxalin-2-carboxamide (6p), a novel 5-HT3 receptor antagonist in rodent behavioral models of depression.
The compound 6p was examined in various behavioral models like forced swim test (FST), tail suspension test (TST), mechanistic models [5-hydroxytryptophan (5-HTP)-induced head twitch and reserpine-induced hypothermia (RIH)], and in chronic surgery model-olfactory bulbectomy in rats.
Compound 6p (1, 2, and 4 mg/kg, i.p.) exhibited antidepressant-like effect in FST and TST after acute treatment without having an effect on baseline locomotor activity. Moreover, 6p (2 mg/kg, i.p.), potentiated the 5-HTP-induced head twitch responses in mice and inhibited the RIH in rats. Chronic treatment (14 days) with 6p (1 and 2 mg/kg, p.o.) and paroxetine (10 mg/kg, p.o.) in rats significantly reversed the behavioral anomalies induced by bilateral olfactory bulbectomy using open field exploration.
The preliminary studies reveal that compound 6p exhibits antidepressant-like effect in behavioral rodent models of depression.
本研究旨在探讨新型 5-HT3 受体拮抗剂 N-正丁基-3-乙氧基喹喔啉-2-甲酰胺（6p）在抑郁的啮齿动物行为模型中的抗抑郁潜力。
该化合物 6p 在各种行为模型中进行了检查，如强迫游泳试验（FST）、悬尾试验（TST）、机制模型[5-羟色氨酸（5-HTP）诱导的头部抽搐和利血平诱导的体温过低（RIH）]，以及在大鼠慢性手术模型-嗅球切除术。
6p（1、2 和 4 mg/kg，ip）在急性治疗后表现出抗抑郁样作用，而对基础运动活动没有影响。此外，6p（2 mg/kg，ip）增强了小鼠中 5-HTP 诱导的头部抽搐反应，并抑制了大鼠中的 RIH。6p（1 和 2 mg/kg，po）和帕罗西汀（10 mg/kg，po）在大鼠中的慢性治疗（14 天）显著逆转了双侧嗅球切除术引起的行为异常，使用开阔场探索。
初步研究表明，化合物 6p 在抑郁的啮齿动物行为模型中表现出抗抑郁样作用。
