Microwave Assisted Synthesis of 2‐(4‐Substituted piperazin‐1‐yl)‐1,8‐naphthyridine‐3‐carbonitrile as a New Class of Serotonin 5‐HT<sub>3</sub> Receptor Antagonists.

Aim:The present study was designed to investigate the antidepressant potential of (4-phenylpiperazin-1-yl) (quinoxalin-3-yl) methanone (4a), a novel 5-HT3 receptor antagonist, with an optimal log P (2.84) and pA2 value (7.3) greater than ondansetron (6.9) using rodent behavioural models of depression.Materials and Methods:Swiss albino mice were used in actophotometer test, forced swim test (FST) and 5-hydroxytryptophan (5-HTP) induced head twitch response. Reserpine induced hypothermia (RIH) and olfactory bulbectomy were performed in male Wistar rats. Statistical analysis was carried out by using one-way analysis of variance followed by Tukey's test.Results:Acute treatment of 4a (1-4 mg/kg, i.p.) in mice produced antidepressant-like effects in FST without affecting the baseline locomotion in actophotometer test. Further, 4a (2-4 mg/kg, i.p.) potentiated the 5-HTP induced head twitches response in mice and also antagonized RIH in rats. Furthermore, sub-chronic (14 days) treatment with 4a (2-4 mg/ kg, p.o.) significantly attenuated the behavioural anomalies induced by bilateral olfactory bulbectomy in rats in modified open field exploration.Conclusions:These preliminary investigations confirm that 4a exhibits antidepressant-like activity in behaviour based rodent models of depression.

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Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT ₃ receptor antagonist: An investigation in behaviour-based rodent models of depression

Mahesh

Kumar

Jindal

et al. 2012

Indian J Pharmacol

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Microwave Assisted Synthesis of 2‐(4‐Substituted piperazin‐1‐yl)‐1,8‐naphthyridine‐3‐carbonitrile as a New Class of Serotonin 5‐HT₃ Receptor Antagonists.

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Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT ₃ receptor antagonist: An investigation in behaviour-based rodent models of depression

Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT ₃ receptor antagonist: An investigation in behaviour-based rodent models of depression

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Microwave Assisted Synthesis of 2‐(4‐Substituted piperazin‐1‐yl)‐1,8‐naphthyridine‐3‐carbonitrile as a New Class of Serotonin 5‐HT3 Receptor Antagonists.

Cited by 1 publication

References 1 publication

Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT 3 receptor antagonist: An investigation in behaviour-based rodent models of depression

Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT 3 receptor antagonist: An investigation in behaviour-based rodent models of depression

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Product

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Microwave Assisted Synthesis of 2‐(4‐Substituted piperazin‐1‐yl)‐1,8‐naphthyridine‐3‐carbonitrile as a New Class of Serotonin 5‐HT₃ Receptor Antagonists.

Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT ₃ receptor antagonist: An investigation in behaviour-based rodent models of depression

Antidepressant-like activity of (4-phenylpiperazin-1-yl) (quinoxalin-2-yl) methanone (4a), a novel 5-HT ₃ receptor antagonist: An investigation in behaviour-based rodent models of depression