scholarly journals Inhibitory Effects ofCoptidis rhizomaand Berberine on Cocaine-Induced Sensitization

2009 ◽  
Vol 6 (1) ◽  
pp. 85-90 ◽  
Author(s):  
Bombi Lee ◽  
Chae Ha Yang ◽  
Dae-Hyun Hahm ◽  
Eun Sang Choe ◽  
Hye-Jung Lee ◽  
...  

Substantial evidence suggests that the behavioral and reinforcing effects of cocaine can be mediated by the central dopaminergic systems. Repeated injections of cocaine produce an increase in locomotor activity and the expression of tyrosine hydroxylase (TH) in the main dopaminergic areas. Protoberberine alkaloids affect neuronal functions.Coptidis rhizoma(CR) and its main compound, berberine (BER) reduced the dopamine content in the central nervous system. In order to investigate the effects of CR or BER on the repeated cocaine-induced neuronal and behavioral alterations, we examined the influence of CR or BER on the repeated cocaine-induced locomotor activity and the expression of TH in the brain by using immunohistochemistry. Male SD rats were given repeated injections of saline or cocaine hydrochloride (15 mg/kg, i.p. for 10 consecutive days) followed by one challenge injection on the 4th day after the last daily injection. Cocaine challenge (15 mg/kg, i.p) produced a larger increase in locomotor activity and expression of TH in the central dopaminergic areas. Pretreatment with CR (50, 100, 200 and 400 mg/kg, p.o.) and BER (200 mg/kg, p.o.) 30 min before the daily injections of cocaine significantly inhibited the cocaine-induced locomotor activity as well as TH expression in the central dopaminergic areas. Our data demonstrate that the inhibitory effects of CR and BER on the repeated cocaine-induced locomotor activity were closely associated with the reduction of dopamine biosynthesis and post-synaptic neuronal activity. These results suggest that CR and BER may be effective for inhibiting the behavioral effects of cocaine by possibly modulating the central dopaminergic system.

2020 ◽  
Vol 19 (5) ◽  
pp. 336
Author(s):  
Luiza Minato Sagrillo ◽  
Viviane Nogueira De Zorzi ◽  
Luiz Fernando Freire Royes ◽  
Michele Rechia Fighera ◽  
Beatriz Da Silva Rosa Bonadiman ◽  
...  

Physical exercise has been shown to be an important modulator of the antioxidant system and neuroprotective in several diseases and treatments that affect the central nervous system. In this sense, the present study aimed to evaluate the effect of physical exercise in dynamic balance, motor coordination, exploratory locomotor activity and in the oxidative and immunological balance of rats treated with vincristine (VCR). For that, 40 adult rats were divided into two groups: exercise group (6 weeks of swimming, 1h/day, 5 days/week, with overload of 5% of body weight) and sedentary group. After training, rats were treated with 0.5 mg/kg of vincristine sulfate for two weeks or with the same dose of 0.9% NaCl. The behavioral tests were conducted 1 and 7 days after each dose of VCR. On day 15 we carried out the biochemical analyzes of the cerebellum. The physical exercise was able to protect against the loss of dynamic balance and motor coordination and, had effect per se in the exploratory locomotor activity, and neutralize oxidative stress, damage DNA and immune damage caused by VCR up to 15 days after the end of the training protocol. In conclusion, we observed that previous physical training protects of the damage motor induced by vincristine.Key-words: exercise, oxidative stress, neuroprotection, cerebellum.


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.


Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2072 ◽  
Author(s):  
Mustafa Barbaros ◽  
Özgür Can ◽  
Umut Üçel ◽  
Nazlı Turan Yücel ◽  
Ümide Demir Özkay

Atomoxetine is a selective noradrenaline reuptake inhibitor drug. Based on the knowledge that agents increasing monoamine levels in the central nervous system have therapeutic potential for neuropathic pain, it is planned to investigate the possible efficacy of atomoxetine on diabetes-induced hyperalgesia, in this study. Randall-Selitto (mechanical noxious stimuli) and Hargreaves (thermal noxious stimuli) tests were used to evaluate nociceptive perception of rats. Obtained data indicated that streptozotocin-induced diabetes causes significant decreases in the paw withdrawal threshold and paw withdrawal latency values of the animals, respectively. However, atomoxetine administered at 3 mg/kg/day for 7 and 14 days improved these diabetes-induced hyperalgesia responses. Furthermore, antihyperalgesic activity was antagonized with α-methyl-para-tyrosine methyl ester, phentolamine, propranolol, and sulpiride pre-treatments. The same effect was not reversed, however, by SCH 23390. These findings demonstrated, for the first time, that atomoxetine possesses significant antihyperalgesic activity on diabetes-induced neuropathic pain and this effect seems to be mediated by α- and β-adrenergic and D2/D3 dopaminergic receptors. Results of this present study seem to offer a new indication for an old drug; atomoxetine, but these preclinical data should first be confirmed with further well-designed clinical trials.


2018 ◽  
Vol 11 (1) ◽  
pp. 77-82
Author(s):  
Miroslav Ts. Eftimov ◽  
StefkaV. Valcheva-Kuzmanova

Summary Aronia melanocarpa fruit juice (AMFJ) has been intensively studied for effects on the central nervous system. The study aimed to investigate AMFJ for possible sedative-hypnotic effects in rats after acute and subchronic administration. Male Wistar rats were treated orally with three doses of AMFJ (2.5, 5.0 and 10.0 ml/kg) either once (acute treatment) or in 30 days (subchronic treatment). Control rats were similarly treated with distilled water. The tests were performed 1 hour after the last AMFJ administration. The possible sedative-hypnotic effects of the juice were investigated in the open field test (OFT) and thiopental-induced sleeping time test. Substances with sedative-hypnotic effects decrease locomotor activity in the OFT and prolong the time of thiopental-induced sleep. The results from the OFT showed that neither the acute, nor the subchronic treatment of rats with all AMFJ doses affected the horizontal and vertical locomotor activity significantly. The two patterns of administration of AMFJ (acute and subchronic) had no significant effect on the duration of thiopental-induced sleep. The lack of effect of AMFJ on locomotor activity and the lack of prolongation of thiopental-induced sleep showed that AMFJ did not display sedative-hypnotic effects in rats.


2018 ◽  
Vol 13 (8) ◽  
pp. 1934578X1801300
Author(s):  
Gislei F. Aragão ◽  
Manoel O. de Moraes Filho ◽  
Paulo N. Bandeira ◽  
Antônio P. Frota Junior ◽  
Yasmin Ingrid S. Oliveira de ◽  
...  

A triterpenic mixture of α and β-amyrin (AMY) extracted from Protium heptaphyllum has demonstrated several pharmacological effects, including activity in the central nervous system. The aim of this study was to evaluate the effect of AMY administration on locomotor activity of mice by the open field test using some monoaminergic agonists and antagonists and the cerebral cortex levels of monoamines and their major metabolites by high-performance liquid chromatography. Mice were treated acutely with AMY at doses of 1, 2.5 and 5 mg/kg given intraperitoneally and with the pharmacological agents and placed in open field test, then the animals were sacrificed and the cerebral cortex extracted, and monoamines were assayed in tissue homogenates. AMY at 1, 2.5 and 5 mg/kg decreased locomotor activity of animals by 25, 31 and 39%, respectively in the open field test. Ondasentron, doxazosin, oxymetazoline and clonidine did not reverse the inhibitory effect of 5 mg/kg AMY. Venlafaxine and yohimbine reversed the inhibitory effect of 5 mg AMY. In the cortex, the 5-HT and 5-HIAA were significantly reduced by the administration of AMY. NE and HVA were also reduced with 2.5 and 5 mg/kg AMY, while Dopamine and DOPAC were not increased with AMY. In conclusion, AMY decreased locomotor activity of animals accompanied by a decrease in 5-HT and NE levels in the cerebral cortex, this locomotor effect is reversed by drug that blocker the α-2-adrenoreceptor.


1999 ◽  
Vol 276 (3) ◽  
pp. R864-R871 ◽  
Author(s):  
Qin-Heng Huang ◽  
Victor J. Hruby ◽  
Jeffrey B. Tatro

Inflammation and microbial infection produce symptoms, including fever, anorexia, and hypoactivity, that are thought to be mediated by endogenous proinflammatory cytokines. Melanocortins are known to act centrally to suppress effects on fever and other sequelae of proinflammatory cytokine actions in the central nervous system, but the roles of melanocortins in anorexia and hypoactivity occurring during the acute phase response are unknown. The present study was designed to determine the effects of exogenous and endogenous α-melanocyte stimulating hormone (α-MSH) on lipopolysaccharide (LPS)-induced anorexia in relation to their effects on fever. Rats were fasted overnight to promote feeding behavior, then injected intraperitoneally with LPS (100 μg/kg ip), followed 30 min later by intracerebroventricular injection of either α-MSH or the melanocortin receptor subtype 3/subtype 4 (MC3-R/MC4-R) antagonist SHU-9119. Food intake, locomotor activity, and body temperature (Tb) were monitored during the ensuing 24-h period. Each of two intracerebroventricular doses of α-MSH (30 and 300 ng) potentiated the suppressive effects of LPS on food intake and locomotion, despite the fact that the higher dose alleviated LPS-induced fever. In control rats that were not treated with LPS, only the higher dose of α-MSH significantly inhibited food intake, and Tband locomotor activity were unaffected. To assess the roles of endogenous central melanocortins, LPS-treated rats received intracerebroventricular SHU-9119 (200 ng). Central MC3-R/MC4-R blockade did not affect Tbor food intake in the absence of LPS treatment, but it reversed the LPS-induced reduction in 24-h food intake and increased LPS-induced fever without altering the LPS-induced suppression of locomotion. Taken together, the results suggest that exogenous and endogenous melanocortins acting centrally exert divergent influences on different aspects of the acute phase response, suppressing LPS-induced fever but contributing to LPS-induced anorexia and hypoactivity.


2011 ◽  
Vol 2011 ◽  
pp. 1-14 ◽  
Author(s):  
José Luis Ordoñez-Librado ◽  
Verónica Anaya-Martínez ◽  
Ana Luisa Gutierrez-Valdez ◽  
Laura Colín-Barenque ◽  
Enrique Montiel-Flores ◽  
...  

The present study examines the effects of divalent and trivalent Manganese (Mn2+/Mn3+) mixture inhalation on mice to obtain a novel animal model of Parkinson disease (PD) inducing bilateral and progressive dopaminergic cell death, correlate those alterations with motor disturbances, and determine whetherL-DOPA treatment improves the behavior, to ensure that the alterations are of dopaminergic origin. CD-1 male mice inhaled a mixture of Manganese chloride and Manganese acetate, one hour twice a week for five months. Before Mn exposure, animals were trained to perform motor function tests and were evaluated each week after the exposure. By the end of Mn exposure, 10 mice were orally treated with 7.5 mg/kgL-DOPA. After 5 months of Mn mixture inhalation, striatal dopamine content decreased 71%, the SNc showed important reduction in the number of TH-immunopositive neurons, mice developed akinesia, postural instability, and action tremor; these motor alterations were reverted withL-DOPA treatment. Our data provide evidence that Mn2+/Mn3+mixture inhalation produces similar morphological, neurochemical, and behavioral alterations to those observed in PD providing a useful experimental model for the study of this neurodegenerative disease.


1979 ◽  
Vol 57 (3) ◽  
pp. 698-701 ◽  
Author(s):  
Ronald Chase

A response to the onset of light was recorded electrophysiologically from the rhinophore nerve of Aplysia californica. Except for the optic nerves, no other peripheral nerve is known to carry photic information to the central nervous system. The result suggests a peripheral location for the extraocular photoreceptors which are known to be capable of controlling the circadian rhythm of locomotor activity.


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