Pharmacological evaluation of novel 5-HT3 receptor antagonist, QCM-13 (N-cyclohexyl-3-methoxyquinoxalin-2-carboxamide) as anti-anxiety agent in behavioral test battery

Deepali Gupta, Mahesh Radhakrishnan, Devadoss Thangaraj, Yeshwant Kurhe

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Objective: In the last few decades, serotonin type-3 (5-HT3 ) receptor antagonists have been identified as potential targets for anxiety disorders. In preclinical studies, 5-HT3 antagonists have shown promising antianxiety effects. In this study, a novel 5-HT3 receptor antagonist, QCM-13(N-cyclohexyl-3-methoxyquinoxalin-2-carboxamide) was evaluated for anxiolytic-like activity in rodent behavioral test battery. Materials and Methods: Mice were given QCM-13 (2 and 4 mg/kg, intraperitoneally [i.p.]) or diazepam (2 mg/kg, i.p.) or vehicle and after 30 min, mice were subjected to four validated behavioral test batteries viz. elevated plus maze, hole board, light-dark and open field tests. Interaction study of QCM-13 with m-chlorophenyl piperazine (mCPP) (mCPP, a 5-HT2A/2C receptor agonist, 1 mg/kg, i.p.) and buspirone (BUS, a partial 5-HT1A agonist, 10 mg/kg, i.p.) were performed to assess the pharmacological mechanism of the drug. Results: QCM-13 expressed potential anxiolytic effect with significant (P < 0.05) increase in behavioral parameters measured in aforementioned preliminary models. Besides, QCM-13 was unable to reverse the anxiogenic effect of mCPP, but potentiated anxiolytic affect of BUS. Conclusion: The results suggest that QCM-13 can be a potential therapeutic candidate for the management of anxiety-like disorders and combination doses of novel 5-HT3 receptor antagonist with standard anxiolytics may improve therapeutic efficacy.

Original languageEnglish (US)
Pages (from-to)103-108
Number of pages6
JournalJournal of Pharmacy and Bioallied Sciences
Volume7
Issue number2
DOIs
StatePublished - Apr 1 2015
Externally publishedYes

Keywords

  • 5-HT receptor antagonist
  • QCM-13
  • antianxiety activity

ASJC Scopus subject areas

  • General Pharmacology, Toxicology and Pharmaceutics
  • Bioengineering
  • General Biochemistry, Genetics and Molecular Biology

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