Neuropharmacological and neurochemical evaluation of N-n-propyl-3-ethoxyquinoxaline-2-carboxamide (6n): a novel serotonergic 5-HT3 receptor antagonist for co-morbid antidepressant- and anxiolytic-like potential using traumatic brain injury model in rats
-
Shvetank Bhatt
,
Radhakrishnan Mahesh
Abstract
Background:
Several preclinical studies have shown that serotonergic 5-HT3 receptor antagonists play an important role in the management of neuropsychiatric disorders, such as depression and anxiety. In the present study the compound “6n” (N-n-propyl-3-ethoxyquinoxaline-2-carboxamide), a novel 5-HT3 receptor antagonist with an optimal log P (2.52) and pA2 (7.6) value was screened for its neuro-pharmacological potential in chronic rodent models of depression and anxiety named traumatic brain injury (TBI).
Methods:
In this model, a 1 cm midline scalp incision was made, and the muscles were retracted to expose the skull. A stainless steel disc (10 mm in diameter and 3 mm in depth) was placed centrally between the lambda and bregma regions. The injury was induced using the impact acceleration model of TBI. Specifically, a 400 g metal weight was dropped from a height of 1 m guided by a straight pipe, onto the metal disc placed over the rat’s skull.
Results:
The behavioral anomalies of the TBI rats were attenuated by the chronic treatment of compound 6n (1 and 2 mg/kg, p.o.; 14 days) as observed by the modified open field test (ambulation, rearing, and fecal pellet), sucrose consumption test (% sucrose consumption), elevated plus maze [% open arm entries [OAE] and % time spent in open arm (TSOA)], and marble burying test (numbers). In addition, 6n also increased the levels of neurotransmitters (norepinephrine and serotonin) and brain derived neurotrophic factor (BDNF) in TBI rats.
Conclusions:
The result suggests that compound 6n exhibited antidepressant- and anxiolytic-like effects in rodent models of depression and anxiety.
Author contributions: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.
Research funding: None declared.
Employment or leadership: None declared.
Honorarium: None declared.
Competing interests: The funding organization(s) played no role in the study design; in the collection, analysis, and interpretation of data; in the writing of the report; or in the decision to submit the report for publication.
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©2017 Walter de Gruyter GmbH, Berlin/Boston
Artikel in diesem Heft
- Frontmatter
- Editorial
- Antidepressant and anxiolytic-like, sedation and hypnosis
- Behavior and Neuroprotection
- Neuropharmacological and neurochemical evaluation of N-n-propyl-3-ethoxyquinoxaline-2-carboxamide (6n): a novel serotonergic 5-HT3 receptor antagonist for co-morbid antidepressant- and anxiolytic-like potential using traumatic brain injury model in rats
- Neuropharmacological evaluation of a novel 5-HT3 receptor antagonist (4-benzylpiperazin-1-yl)(3-methoxyquinoxalin-2-yl) methanone (6g) on lipopolysaccharide-induced anxiety models in mice
- Effect of Salacia reticulata W. and Clitoria ternatea L. on the cognitive and behavioral changes in the streptozotocin-induced young diabetic rats
- In vivo sedative and hypnotic activities of methanol extract from the leaves of Jacquemontia paniculata (Burm.f.) Hallier f. in Swiss Albino mice
- Reproduction
- Bonny light crude oil-induced alteration in levels of testicular stress proteins is accompanied by apoptosis in rats after treatment withdrawal
- Cardiovascular-Pulmonary Interactions
- Meteorological parameters and pollutants on asthma exacerbation in Bangalore, India – an ecological retrospective time-series study
- Oxidative Stress
- Antioxidant and acetylcholinesterase inhibitory activities of leaf extract and fractions of Albizia adianthifolia (Schumach) W.F. Wright
- Oxidative stress, histopathological and electron microscopic alterations induced by dimethylnitrosamine in renal male mice and the protective effect of α-lipoic acid
- Effects of altered thyroid states on oxidative stress parameters in rats
- Metabolism
- The effects of smoking and nicotine ingestion on exercise heat tolerance
- Inflammation
- Investigation of antinociceptive activity of methanolic extract of Persicaria orientalis leaves in rodents
- Infection
- Antiplasmodial activity of the ethanolic root bark extract of Icacina senegalensis in mice infected by Plasmodium berghei
- Phytotherapy
- Evaluation of cytotoxic, analgesic, antidiarrheal and phytochemical properties of Hygrophila spinosa (T. Anders) whole plant
Artikel in diesem Heft
- Frontmatter
- Editorial
- Antidepressant and anxiolytic-like, sedation and hypnosis
- Behavior and Neuroprotection
- Neuropharmacological and neurochemical evaluation of N-n-propyl-3-ethoxyquinoxaline-2-carboxamide (6n): a novel serotonergic 5-HT3 receptor antagonist for co-morbid antidepressant- and anxiolytic-like potential using traumatic brain injury model in rats
- Neuropharmacological evaluation of a novel 5-HT3 receptor antagonist (4-benzylpiperazin-1-yl)(3-methoxyquinoxalin-2-yl) methanone (6g) on lipopolysaccharide-induced anxiety models in mice
- Effect of Salacia reticulata W. and Clitoria ternatea L. on the cognitive and behavioral changes in the streptozotocin-induced young diabetic rats
- In vivo sedative and hypnotic activities of methanol extract from the leaves of Jacquemontia paniculata (Burm.f.) Hallier f. in Swiss Albino mice
- Reproduction
- Bonny light crude oil-induced alteration in levels of testicular stress proteins is accompanied by apoptosis in rats after treatment withdrawal
- Cardiovascular-Pulmonary Interactions
- Meteorological parameters and pollutants on asthma exacerbation in Bangalore, India – an ecological retrospective time-series study
- Oxidative Stress
- Antioxidant and acetylcholinesterase inhibitory activities of leaf extract and fractions of Albizia adianthifolia (Schumach) W.F. Wright
- Oxidative stress, histopathological and electron microscopic alterations induced by dimethylnitrosamine in renal male mice and the protective effect of α-lipoic acid
- Effects of altered thyroid states on oxidative stress parameters in rats
- Metabolism
- The effects of smoking and nicotine ingestion on exercise heat tolerance
- Inflammation
- Investigation of antinociceptive activity of methanolic extract of Persicaria orientalis leaves in rodents
- Infection
- Antiplasmodial activity of the ethanolic root bark extract of Icacina senegalensis in mice infected by Plasmodium berghei
- Phytotherapy
- Evaluation of cytotoxic, analgesic, antidiarrheal and phytochemical properties of Hygrophila spinosa (T. Anders) whole plant
