Bhatt Shvetank, Mahesh Radhakrishnan, Devadoss Thangaraj, Jindal Ankur
Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333 031, India.
Indian J Exp Biol. 2013 Jul;51(7):510-4.
The present research was designed to explore the anxiolytic-like activity of a novel 5-HT3 receptor antagonist (60) in experimental mouse models of anxiety. The anxiolytic activity of '6o' at (1 and 2 mg/kg, ip) was evaluated in mice by using a battery of behavioural tests of anxiety such as elevated plus maze (EPM), light/dark aversion test, hole board (HB) and open field test (OFT) with diazepam (2 mg/kg, ip) as a standard anxiolytic. None of the tested doses of '6o' affected the base line locomotion. Compound '6o' (2 mg/kg, ip) and diazepam (2 mg/kg, ip) significantly increased the percentage of both time spent and open arm entries in the EPM test. Compound '6o' in (1 mg/kg, ip) dose was only able to affect the percentage time spent in open arm significantly in the EPM test. In the light and dark test, compound '6o' (2 mg/kg, ip) and diazepam (2 mg/kg, ip) significantly increased the total time spent in light compartment as well as number of transitions from one compartment to other and number of square crossed. Compound '6o' (1 and 2 mg/kg, ip) and diazepam (2 mg/kg, ip) also significantly increased number of head dips and number of squares crossed, whereas significantly decreased the head dipping latency in HB test as compared to vehicle control group. In addition, '6o' in both the doses and diazepam (2 mg/kg, ip) significantly increased the ambulation scores (squares crossed) in OFT however, there was no significant effect of '6o' (1 and 2 mg/kg, ip) and diazepam (2 mg/kg, ip) on rearing scores. To conclude compound '6o' exhibited an anxiolytic-like effect in animal models of anxiety.
本研究旨在探讨一种新型5-羟色胺3（5-HT3）受体拮抗剂（60）在焦虑实验小鼠模型中的抗焦虑样活性。以地西泮（2毫克/千克，腹腔注射）作为标准抗焦虑药，通过一系列焦虑行为测试，如高架十字迷宫（EPM）、明暗回避试验、洞板试验（HB）和旷场试验（OFT），评估“60”在1和2毫克/千克（腹腔注射）剂量下的抗焦虑活性。“60”的所有测试剂量均未影响基线运动。化合物“60”（2毫克/千克，腹腔注射）和地西泮（2毫克/千克，腹腔注射）在EPM试验中显著增加了在开放臂停留的时间百分比和进入开放臂的次数。“60”在1毫克/千克（腹腔注射）剂量下仅能在EPM试验中显著影响在开放臂停留的时间百分比。在明暗试验中，化合物“60”（2毫克/千克，腹腔注射）和地西泮（2毫克/千克，腹腔注射）显著增加了在亮区停留的总时间、从一个区到另一个区的转换次数以及穿过的方格数。与溶剂对照组相比，“60”（1和2毫克/千克，腹腔注射）和地西泮（2毫克/千克，腹腔注射）在HB试验中也显著增加了头部探洞次数和穿过的方格数，同时显著缩短了头部探洞潜伏期。此外，两种剂量的“60”和地西泮（2毫克/千克，腹腔注射）在OFT中均显著增加了行走得分（穿过的方格数），然而，“60”（1和2毫克/千克，腹腔注射）和地西泮（2毫克/千克，腹腔注射）对竖毛得分没有显著影响。总之，化合物“60”在焦虑动物模型中表现出抗焦虑样作用。
