• Journal of Integrative Natural Science
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• v.9 no.2
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• pp.128-135
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• 2016

5-hydroxytryptamine (serotonin) receptor ($5-HT_7R$) 7 is one of G-Protein coupled receptors, which is activated by the neurotransmitter Serotonin. After activation by serotonin, $5-HT_7$ activates the production of the intracellular signaling molecule cyclic AMP. $5-HT_7$ receptor has been found to be involved in the pathophysiology of various disorders. It is reported that $5-HT_7$ receptor antagonists can be used as antidepressant agents. In this study, we report the important structural and chemical parameters for 2-methoxyphenylpiperazinylakanamides as $5-HT_7R$ inhibitors. A 3D QSAR study based on comparative molecular field analysis (CoMFA) was performed. The best predictions were obtained for the best CoMFA model with $q^2$ of 0.594 with 6 components, $r^2$ of 0.986, Fisher value as 60.607, and an estimated standard error of 0.043. The predictive ability of the test set was 0.602. Results obtained the CoMFA models suggest that the data are well fitted and have high predictive ability. The contour maps are generated and studied. The contour analyses may serve as tool in the future for designing of novel and more potent $5-HT_7R$ derivatives.

• Journal of Integrative Natural Science
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• v.5 no.3
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• pp.168-174
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• 2012

Gal (1-3) receptors are members of GPCR superfamily with seven transmembrane helices. The neuropeptide galanin mediates its effects through the receptor subtypes Gal1, Gal2, and Gal3 and has been implicated in anxiety and depression related behaviors. Galanin receptors are considered to be important targets for the development of novel antidepressant drugs. Owing to the importance of these receptors, a short communication about the sequential and structural studies about the functional Galanin (1-3) receptors has been reported. Structural studies have been hampered due to the lack of X-ray crystal structures. However with the availability of templates with close homologs comparative modeling could be encouraging. Sequence analysis was done for each receptors and homology modeling of each receptors were done with recently reported templates. Comparative analyses were done between these receptors to identify the relationships between them sequentially. Phylogram was generated between these receptors to identify the close homologue between this receptor and found that Gal2 and Gal3 receptors are closer. Our results could be useful for further structure based drug design targeting Gal1, Gal2 and Gal3 receptors.

• Journal of Pharmacopuncture
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• v.26 no.1
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• pp.10-17
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• 2023

Objectives: Murraya paniculata (family-Rutaceae), popularly known as orange jasmine, is the most important evergreen plant. The Rutaceae family is economically significant due to its diverse edible fruits and essential oils. Methods: Murraya paniculata extracts (MPE) of leaf have been shown to include phenolic compounds, highly oxygenated flavonoids, flavanones, sesquiterpenoids, polymethoxy glycosides, and coumarins. Cyclocitral, methyl salicylate, trans-nerolidol, cubenol, isogermacrene, -cadinol, and cubeb-11-ene are all abundant in MPE. The usages of various parts of this plant, such as bark, leaves and flower, as a remedy for a variety of ailments as widely recorded in the traditional literature. The plant has anti-diabetic, anti-obesity, antibacterial, anti-implantation, anti-oxidative, cytotoxic, anti-diarrheal, antidepressant and anti-anxiety properties and many others. Results: The goal of the review is to reignite interest in this potential plant, encouraging researchers to continue their research in order to uncover novel therapeutic compounds for the treatment and management of a range of infections. The current review provided a comprehensive overview of this traditional unique plant. Conclusion: The review paves a way for exploring its active chemical elements with substantial pharmacological values further for potential benefits of mankind.

• Biomolecules & Therapeutics
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• v.27 no.4
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• pp.349-356
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• 2019

Behavioral analysis in mice provided important contributions in helping understand and treat numerous neurobehavioral and neuropsychiatric disorders. The behavioral performance of animals and humans is widely different among individuals but the neurobehavioral mechanism of the innate difference is seldom investigated. Many neurologic conditions share comorbid symptoms that may have common pathophysiology and therapeutic strategy. The forced swim test (FST) has been commonly used to evaluate the "antidepressant" properties of drugs yet the individual difference analysis of this test was left scantly investigated along with the possible connection among other behavioral domains. This study conducted an FST-screening in outbred CD-1 male mice and segregated them into three groups: high performers (HP) or the active swimmers, middle performers (MP), and low performers (LP) or floaters. After which, a series of behavioral experiments were performed to measure their behavioral responses in the open field, elevated plus maze, Y maze, three-chamber social assay, novel object recognition, delay discounting task, and cliff avoidance reaction. The behavioral tests battery revealed that the three groups displayed seemingly correlated differences in locomotor activity and novel object recognition but not in other behaviors. This study suggests that the HP group in FST has higher locomotor activity and novelty-seeking tendencies compared to the other groups. These results may have important implications in creating behavior database in animal models that could be used for predicting interconnections of various behavioral domains, which eventually helps to understand the neurobiological mechanism controlling the behaviors in individual subjects.

• Korean Journal of Psychosomatic Medicine
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• v.7 no.2
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• pp.274-280
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• 1999

A variety of mechanism may generate pain resulting from injury to the central and peripheral nervous system. None of these mechanism is disease-specific, and several different pain mechanism may be simultaneously present in anyone patient, independent of diagnosis. Diagnosis of neuropathic pain is often easily made from information gathered on neurologic examination and from patient history. Although treatment of neuropathic pain may be difficult, optimum treatment can be achieved if the neurologist has a complete understanding of therapeutic options, the mainstay of which is pharmacotherapy. Selection of an appropriate rharmacologic agent is by trial and error since individual responses to different agents, doses, and serum levels are highly variable. An adequate trial for each agent tried is key to pharmacologic treatment of neuropathic pain. Tricyclic antidepressants are first-line agents, although other drugs, including anticonvulsants, local anesthetic antiarrhythmics, clonidine, opiates, and certain topical agents, also offer pain relief in some patient populations. The novel antidepressants venlafaxine and nefazodone are potentially useful new drugs that are better tolerated than tricyclic antidepressants. Also Gabapentine seems an interesting and promising drug for the treatment of neuropathic pain.