scholarly journals Involvement of GABAA Receptors in the Anxiolytic-Like Effect of Hydroxycitronellal

2021 ◽  
Vol 2021 ◽  
pp. 1-17
Author(s):  
Jéssica C. Andrade ◽  
Álefe B. Monteiro ◽  
Humberto H. N. Andrade ◽  
Thallita K. S. N. Gonzaga ◽  
Pablo R. Silva ◽  
...  

Hydroxycitronellal (HC) is a monoterpene present in essential oils of aromatic plants of different species, obtained from semisynthesis of citronellal, and is widely used as a fragrance in cosmetics. The objective of this work was to evaluate the possible anxiolytic-like activity of HC and its possible mechanism of action using in vivo and in silico methodologies. Swiss male mice (Mus musculus) were treated with HC (12.5, 25, and 50 mg/kg, i.p.) and subjected to the rota rod, elevated plus maze, and open field tests. No significant impairments were observed in the rota rod tests for the motor activity of the animals treated with HC at 12.5, 25, and 50 mg/kg, i.p., indicating no myo-relaxing or sedative effects. In the elevated plus maze, HC (in the three doses) induced significant increases in the percentage of entries (respectively, 34.8%, 33.8%, and 38.6%) and in the length of stay (respectively, 49.9%, 56.1%, and 57.0%) in the open arms of the EPM, as well as the number of crossings in the open field tests. The mechanism of action of the compound’s anxiolytic-like activity can be attributed to the involvement of GABAA receptors, and this interaction was observed in in vivo and in silico studies. For HC, the results suggest anxiolytic-like effects, possibly via modulation of the GABAergic system. The use of natural products to treat anxiety can become an alternative to existing synthetic products.

2019 ◽  
Vol 15 (1) ◽  
pp. 102-118 ◽  
Author(s):  
Carolina Campos-Rodríguez ◽  
José G. Trujillo-Ferrara ◽  
Ameyali Alvarez-Guerra ◽  
Irán M. Cumbres Vargas ◽  
Roberto I. Cuevas-Hernández ◽  
...  

Background: Thalidomide, the first synthesized phthalimide, has demonstrated sedative- hypnotic and antiepileptic effects on the central nervous system. N-substituted phthalimides have an interesting chemical structure that confers important biological properties. Objective: Non-chiral (ortho and para bis-isoindoline-1,3-dione, phthaloylglycine) and chiral phthalimides (N-substituted with aspartate or glutamate) were synthesized and the sedative, anxiolytic and anticonvulsant effects were tested. Method: Homology modeling and molecular docking were employed to predict recognition of the analogues by hNMDA and mGlu receptors. The neuropharmacological activity was tested with the open field test and elevated plus maze (EPM). The compounds were tested in mouse models of acute convulsions induced either by pentylenetetrazol (PTZ; 90 mg/kg) or 4-aminopyridine (4-AP; 10 mg/kg). Results: The ortho and para non-chiral compounds at 562.3 and 316 mg/kg, respectively, decreased locomotor activity. Contrarily, the chiral compounds produced excitatory effects. Increased locomotor activity was found with S-TGLU and R-TGLU at 100, 316 and 562.3 mg/kg, and S-TASP at 316 and 562.3 mg/kg. These molecules showed no activity in the EPM test or PTZ model. In the 4-AP model, however, S-TGLU (237.1, 316 and 421.7 mg/kg) as well as S-TASP and R-TASP (316 mg/kg) lowered the convulsive and death rate. Conclusion: The chiral compounds exhibited a non-competitive NMDAR antagonist profile and the non-chiral molecules possessed selective sedative properties. The NMDAR exhibited stereoselectivity for S-TGLU while it is not a preference for the aspartic derivatives. The results appear to be supported by the in silico studies, which evidenced a high affinity of phthalimides for the hNMDAR and mGluR type 1.


2002 ◽  
Vol 134 (1-2) ◽  
pp. 49-57 ◽  
Author(s):  
Valeria Carola ◽  
Francesca D'Olimpio ◽  
Emiliano Brunamonti ◽  
Franco Mangia ◽  
Paolo Renzi

2017 ◽  
Vol 28 (6) ◽  
pp. 617-648
Author(s):  
Robert Lalonde ◽  
Catherine Strazielle

AbstractWhen injected via the intracerebroventricular route, corticosterone-releasing hormone (CRH) reduced exploration in the elevated plus-maze, the center region of the open-field, and the large chamber in the defensive withdrawal test. The anxiogenic action of CRH in the elevated plus-maze also occurred when infused in the basolateral amygdala, ventral hippocampus, lateral septum, bed nucleus of the stria terminalis, nucleus accumbens, periaqueductal grey, and medial frontal cortex. The anxiogenic action of CRH in the defensive withdrawal test was reproduced when injected in the locus coeruleus, while the amygdala, hippocampus, lateral septum, nucleus accumbens, and lateral globus pallidus contribute to center zone exploration in the open-field. In addition to elevated plus-maze and open-field tests, the amygdala appears as a target region for CRH-mediated anxiety in the elevated T-maze. Thus, the amygdala is the principal brain region identified with these three tests, and further research must identify the neural circuits underlying this form of anxiety.


2021 ◽  
Vol 14 (03) ◽  
pp. 265-276
Author(s):  
Bigued ◽  
Germain Sotoing Taiwe ◽  
Jacqueline Stephanie Kameni Njapdounke ◽  
Joseph Ngaibi ◽  
Yvette Nguezeye ◽  
...  

Ethnopharmacological relevance: Dysphania ambrosioides (L.) Mosyakin & Clemants (Chenopodiaceae) is a medicinal plant known for its anxiolytic, antidepressant and anticonvulsant activities in Cameroonian folk medicine. Aim of the study: The aim of this work is to evaluate the anxiolytic effects of Dysphania ambrosioides aqueous extracts and investigate its mechanism of action. Materials and methods: Elevated plus maze test and open field test were used for detecting it anxiolytic properties. The possible mechanism of action of the aqueous extracts were investigated after pretreatment of animals with different antagonists of GABAA complex receptors (5 mg/kg N-methyl-β-carboline-3-carboxamide, 4 mg/kg flumazenil or 2 mg/kg bicuculline) 30 minutes prior to the oral administration of 370 mg/kg Dysphania ambrosioides aqueous extract. Results: Dysphania ambrosioides increased the percentage of entries into and percentage of time in open arms, and reduced rearing, head dipping, and percentage of time in closed arms, in the elevated plus maze. It reduced rearing and defecation, and increased crossing, in the open field. In addition, anxiolytic-like properties of Dysphania ambrosioides were blocked by different antagonists of GABAA complex receptors (N-methyl-β-carboline-3-carboxamide, flumazenil or bicuculline) as examined in elevated plus maze test. Finally, the activity of GABA-T activity was inhibited and the brain GABA concentration was increased by the extracts, respectively. Conclusion: These results suggest that Dysphania ambrosioides possess anxiolytic-like properties in mice that might involve an action on benzodiazepine and/or GABA sites in the GABAA receptor complex or by modulating brain GABA concentration in the central nervous system.


2019 ◽  
Vol 19 (3) ◽  
pp. 2526-2536 ◽  
Author(s):  
Hong-Biao Chu ◽  
Yue-De Tan ◽  
Yun-Jing Li ◽  
Bin-Bin Cheng ◽  
Bao-Qi Rao ◽  
...  

Background:Erythrina variegata has been widely used as a traditional medicine.Objective: The study was designed to evaluate the anxiolytic and anti-depressant effects of an extract from Erythrina variegata.Methods: The extract was evaluated for anxiolytic and anti-depressant action using the elevated plus maze, light/dark box, open field, forced swimming and tail suspension tests in mice. The mechanism of action was further elucidated using high-performance liquid chromatography with fluorescence detection methods to assay the levels of five neurotransmitters in brain.Results: The extract exhibited significant increase in the percentage of the open arms entries and the time spent in the open arms in the elevated plus maze test. The results of the light/dark box test revealed a significant increase in the amount of time spent in the light chamber. Extract- treated mice also produced significant increase in the number of crossings and rearings in the open field test.In the forced swimming and tail suspension tests, the extract was able to promote significant decrease in the immobility time. In addition, the extract significantly altered the levels of five neurotransmitters in the brain tissue.Conclusion: These findings suggest that Erythrina variegata presents potential anxiolytic and anti-depressant activity, and the mechanism may be related to the alteration of neurotransmitter levels.Keywords: Anxiolytic; anti-depressant; Erythrina variegata; elevated plus maze; forced swimming; neurotransmitters.


2015 ◽  
Vol 6 (6) ◽  
Author(s):  
Yaghoob Farbood ◽  
Seyyed Mohammad Taghi Mansouri ◽  
Seyyed Mostafa Ahmadian ◽  
Seyyad Ali Mard ◽  
Alireza Sarkaki

2017 ◽  
Vol 642 ◽  
pp. 77-85 ◽  
Author(s):  
Alberto Ferreira Donatti ◽  
Renato Nery Soriano ◽  
Christie Ramos Andrade Leite-Panissi ◽  
Luiz G.S. Branco ◽  
Albert Schiaveto de Souza

2021 ◽  
Author(s):  
fahad jibran siyal ◽  
rehan ahmed siddiqui ◽  
zahida memon ◽  
zahra batool ◽  
aneela Atta Ur Rahman ◽  
...  

Abstract Background: Anxiety can also be termed as excessive worry which last for at least more than six months and patients can have difficulty in controlling them. Anxiety is having 31% of life time prevalence and sad part is that the anxiety disorders are not treated and diagnosed well. 3.1% which is 6.8 Million peoples of America are having anxiety disorders. The main part of clove oil is eugenol along with caryophyllene. Eugenol is present at about 70 to 90 percentage and also it contains 15 percentage of total dry weight of bud. Methodology: Pre-clinical experimental study was conducted for 10-12 Months. Male BALB/c mice were purchased from ICCBS. Sample Size was 42 BALB/c mice and divided into 07 groups. Results: The animal model was developed and it was found that Eugenol and its liposomal based nano carrier protect anxiety disorders in mice with the help of behavioral tests such as Elevated plus maze and open field tests and was recorded as Mean and SD, frequency and percentages accordingly. Conclusion: Therefore with the help of behavioral studies i.e. open field test and elevated plus maze test, eugenol and its liposomal based nano particle protect anxiety disorder in the mice by increasing the entry time and stay of mice in open arms for longer duration in elevated maze plus test and in open field the anxiety was reduced after mice spent most of time in the center rather than periphery.


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