Anxiolytic Properties of New Chemical Entity, 5TIO1

Fortes, Amanda Campos; Almeida, Antônia Amanda Cardoso de; Mendonça-Júnior, Francisco Jaime Bezerra; Freitas, Rivelilson Mendes de; Sobrinho, José Lamartine Soares; Soares, Mônica Felts de La Roca

doi:10.1007/s11064-013-0970-y

Cited by 24 publications

(12 citation statements)

References 22 publications

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“…Our results observed neurochemical alterations after administration of an anxiolytic-like compound, 5TIO1 [23]. …”

Section: Discussionmentioning

confidence: 99%

“…Drug dosages of 5TIO1 were determined from dose-response studies (data not shown) and from observation of dose currently used in animal's studies [23–25]. The doses of 5TIO1 used (0.1, 1, and 10 mg/kg) in the present study are not equivalent to those used by humans because rats have different metabolic rates.…”

Section: Methodsmentioning

confidence: 99%

“…5TIO1 showed anxiolytic-like effect in plus-maze, and light/dark box tests did not change locomotor and coordination activities in open field and rotarod tests, respectively [23]. …”

Section: Introductionmentioning

confidence: 99%

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Is Oxidative Stress in Mice Brain Regions Diminished by 2-[(2,6-Dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile?

Fortes

Almeida

Oliveira

et al. 2013

Oxidative Medicine and Cellular Longevity

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2-[(2,6-Dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile, 5TIO1, is a new 2-aminothiophene derivative with promising pharmacological activities. The aim of this study was to evaluate its antioxidant activity in different areas of mice central nervous system. Male Swiss adult mice were intraperitoneally treated with Tween 80 dissolved in 0.9% saline (control group) and 5TIO1 (0.1, 1, and 10 mg kg−1). Brain homogenates—hippocampus, striatum, frontal cortex, and cerebellum—were obtained after 24 h of observation. Superoxide dismutase and catalase activities, lipid peroxidation and nitrite content were measured using spectrophotometrical methods. To clarify the 5TIO1's mechanism on oxidative stress, western blot analysis of superoxide dismutase and catalase was also performed. 5TIO1 decreased lipid peroxidation and nitrite content in all brain areas and increased the antioxidant enzymatic activities, specially, in cerebellum. The data of Western blot analysis did not demonstrate evidence of the upregulation of these enzymes after the administration of this compound. Our findings strongly support that 5TIO1 can protect the brain against neuronal damages regularly observed during neuropathologies.

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“…Our results observed neurochemical alterations after administration of an anxiolytic-like compound, 5TIO1 [23]. …”

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Is Oxidative Stress in Mice Brain Regions Diminished by 2-[(2,6-Dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile?

Fortes

Almeida

Oliveira

et al. 2013

Oxidative Medicine and Cellular Longevity

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“…The open field arena (100 cm × 100 cm × 40 cm) is constructed of acrylic, with gray walls and a black floor, which is divided into 25 squares of equal areas as previously described [25, 26]. Instances of crossing-movement (Cm) and instances of rearing-movement (Rm) are usually used as measures of exploration and anxiety [27, 28].…”

Section: Methodsmentioning

confidence: 99%

Wen‐Dan Decoction Improves Negative Emotions in Sleep‐Deprived Rats by Regulating Orexin‐A and Leptin Expression

Song

Feng

et al. 2014

Evidence-Based Complementary and Alternative Medicine

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Wen-Dan Decoction (WDD), a formula of traditional Chinese medicine, has been clinically used for treating insomnia for approximately 800 years. However, the therapeutic mechanisms of WDD remain unclear. Orexin-A plays a key role in the sleep-wake cycle, while leptin function is opposite to orexin-A. Thus, orexin-A and leptin may be important factors in sleep disorders. In this study, 48 rats were divided into control, model, WDD-treated, and diazepam-treated groups. The model of insomnia was produced by sleep deprivation (SD) for 14 days. The expressions of orexin-A, leptin, and their receptors in blood serum, prefrontal cortex, and hypothalamus were detected by enzyme-linked immunosorbent assay, immunohistochemistry, and real time PCR. Open field tests showed that SD increased both crossing movement (Cm) and rearing-movement (Rm) times. Orexin-A and leptin levels in blood serum increased after SD but decreased in brain compared to the control group. mRNA expressions of orexin receptor 1 and leptin receptor after SD were decreased in the prefrontal cortex but were increased in hypothalamus. WDD treatment normalized the behavior and upregulated orexin-A, leptin, orexin receptor 1 and leptin receptor in brain. The findings suggest that WDD treatment may regulate SD-induced negative emotions by regulating orexin-A and leptin expression.

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“…In recent drugs investigations, they acquired a particular importance due to the innovations in their synthesis (Gewald reaction), availability, stability, and structural simplicity that allow them to be important scaffolds in chemical and therapeutic products; like the top selling drugs olanzepine and tinoridine. [16][17][18] In addition, they present a large spectrum of biological properties that include antimicrobial, 19,20) anti-inflammatory, 21) anxiolytic, 22) antileishmanial, 23) anti-diabetes, 24) antifungal, 25) antioxidant 26) and antiplatelet activities. 27) The antitumor evaluation of the 2-aminothiophenes has already been addressed through different reports.…”

mentioning

confidence: 99%

Uses of Cyclohexan-1,4-dione for the Synthesis of 2-Amino-4,5-dihydrobenzo[<i>b</i>]thiophen-6(7<i>H</i>)-one Derivatives with Anti-proliferative and Pim-1 Kinase Activities

Mohareb

Abbas

Ibrahim

2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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The reaction of cyclohexan-1,4-dione with elemental sulfur and any of the 2-cyano-N-arylacetamide derivatives 2a-c gave the 2-amino-4,5-dihydrobenzo[b]thiophen-6(7H)-one derivatives 3a-c to be used in some heterocyclization reactions. The multicomponent reactions of any of compounds 3a-c with aromatic aldehydes 6a-c and either of malononitrile or ethylcyanoacetate gave the 5,9-dihydro-4H-thieno[2,3-f ]chromene derivatives 9a-r, respectively. The anti-proliferative evaluation of the newly synthesized compounds against the six cancer cell lines A549, HT-29, MKN-45, U87MG, SMMC-7721 and H460 showed that the nine compounds 3c, 5c, 9e, 9h, 9i, 9j, 9l, 9q, 11e and 13e with highest cytotoxcity. Toxicity of these compounds against shrimp larvae revealed that compounds 3c, 9j, 9q, and 13e showed no toxicity against the tested organisms. The c-Met kinase inhibition of the most potent compounds showed that compounds 9j, 9q, 10e, 12e and 13e have the highest activities. Compounds 9j, 9l, 9q and 11e showed high activity towards tyrosine kinases. Moreover, compounds 9j, 9q and 13e showed the highest inhibitor activity towards Pim-1 kinase.

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Anxiolytic Properties of New Chemical Entity, 5TIO1

Cited by 24 publications

References 22 publications

Is Oxidative Stress in Mice Brain Regions Diminished by 2-[(2,6-Dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile?

Is Oxidative Stress in Mice Brain Regions Diminished by 2-[(2,6-Dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile?

Wen‐Dan Decoction Improves Negative Emotions in Sleep‐Deprived Rats by Regulating Orexin‐A and Leptin Expression

Uses of Cyclohexan-1,4-dione for the Synthesis of 2-Amino-4,5-dihydrobenzo[<i>b</i>]thiophen-6(7<i>H</i>)-one Derivatives with Anti-proliferative and Pim-1 Kinase Activities

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