scholarly journals Pharmacological Evaluation of Naproxen Metal Complexes on Antinociceptive, Anxiolytic, CNS Depressant, and Hypoglycemic Properties

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Md. Sharif Hasan ◽  
Narhari Das ◽  
Zobaer Al Mahmud ◽  
S. M. Abdur Rahman
Keyword(s):  
Metal Complexes ◽  
Elevated Plus Maze ◽  
Zinc Complexes ◽  
Antinociceptive Activity ◽  
Tail Flick ◽  
Dependent Manner ◽  
Cns Depressant ◽  
Plus Maze ◽  
Dose Dependent ◽  
Parent Ligand

Purpose. The present study was designed to investigate the antinociceptive, anxiolytic, CNS depressant, and hypoglycemic effects of the naproxen metal complexes.Methods. The antinociceptive activity was evaluated by acetic acid-induced writhing method and radiant heat tail-flick method while anxiolytic activity was evaluated by elevated plus maze model. The CNS depressant activity of naproxen metal complexes was assessed using phenobarbitone-induced sleeping time test and the hypoglycemic test was performed using oral glucose tolerance test.Results. Metal complexes significantly (P<0.001) reduced the number of abdominal muscle contractions induced by 0.7% acetic acid solution in a dose dependent manner. At the dose of 25 mg/kg body weight p.o. copper, cobalt, and zinc complexes exhibited higher antinociceptive activity having 59.15%, 60.56%, and 57.75% of writhing inhibition, respectively, than the parent ligand naproxen (54.93%). In tail-flick test, at both doses of 25 and 50 mg/kg, the copper, cobalt, silver, and zinc complexes showed higher antinociceptive activity after 90 minutes than the parent drug naproxen. In elevated plus maze (EPM) model the cobalt and zinc complexes of naproxen showed significant anxiolytic effects in dose dependent manner, while the copper, cobalt, and zinc complexes showed significant CNS depressant and hypoglycemic activity.Conclusion. The present study demonstrated that copper, cobalt, and zinc complexes possess higher antinociceptive, anxiolytic, CNS depressant, and hypoglycemic properties than the parent ligand.

scholarly journals Efficacy and safety of the metformin-mazindol anorectic combination in rat

2021 ◽  
Vol 71 (2) ◽  
pp. 279-291
Author(s):  
Federico Argüelles-Tello ◽  
José Eduardo Roa-Coria ◽  
Ángel Zúñiga-Romero ◽  
Juan Carlos Huerta-Cruz ◽  
Geovanna Nalley Quiñonez-Bastidas ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Effective Dose ◽  
Elevated Plus Maze ◽  
Blood Chemistry ◽  
Dependent Manner ◽  
Interaction Index ◽  
Elevated Plus Maze Test ◽  
Plus Maze ◽  
Anorectic Effect ◽  
Dose Dependent

AbstractThe current study investigates the anorectic interaction and safety of the mazindol-metformin combination in rats. Isobologram and interaction index were used to determine anorectic interaction between mazindol and metformin in the sweetened milk model. The safety profile of the mazindol-metformin combination was determined by measuring anxiety, blood pressure, hematic biometry and blood chemistry. An acute dose of mazindol and metformin administered per os, individually or as a mixture, has reduced the milk consumption in rats in a dose-dependent manner. Theoretical effective dose 40 (ED40t) did not differ from the experimental effective dose 40 (ED40e) obtained with the mazindol-metformin mixture in the anorexia experiments, by Student′s t-test. In addition, the interaction index confirmed the additive anorectic effect between both drugs. A single oral dose of ED40e mazindol-metformin mixture induced anxiolysis in the elevated plus-maze test. Moreover, oral administration of mazindol-metformin combination for 3 months significantly decreased glycemia, but not blood pressure nor other parameters of hematic biometry and blood chemistry. Results suggest that mazindol-metformin combination exerts an additive anorectic effect, as well as anxiolytic and hypoglycemic properties. Mazindol-metformin combination might be useful in obese patients with anxiety disorders or diabetes risk factors.

scholarly journals EFFECTS OF CINNAMOMUM ZEYLANICUM BARK EXTRACT ON NOCICEPTION AND ANXIETY LIKE BEHAVIOR IN MICE

2019 ◽  
pp. 236-241
Author(s):  
SEEMA JAIN ◽  
SPARSH GUPTA
Keyword(s):  
Formalin Test ◽  
Elevated Plus Maze ◽  
Antinociceptive Activity ◽  
Bark Extract ◽  
Control Group ◽  
Tail Flick ◽  
Pain Response ◽  
Cinnamomum Zeylanicum ◽  
Hot Plate ◽  
Plus Maze

Objectives: The aim of the study was to assess the effect of the extract of Cinnamomum zeylanicum (CZ) bark in the experimental models of pain and anxiety-like behavior in mice. Methods: The extract of CZ bark was administered at the doses of 100, 200, and 400 mg/kg, per orally (p.o) and morphine used as a positive control for pain models, was administered at the dose of 5 mg/kg, intraperitoneally (i.p.). Antinociceptive activity was evaluated using three experimental animal models of pain, namely, tail flick, hot plate, and formalin test. Elevated plus maze test was used to assess the effect on anxiety-like behavior. Rotarod apparatus and actophotometer were used to test muscle coordination and locomotor activity, respectively. Results: Administration of CZ bark extract in the dose of 200 and 400 mg/kg showed significantly increased in the tail-flick latency and latency to reaction time in hot plate test as compared to the control group. In the first phase (0–5 min) of the formalin test, a significant reduction in the pain response was found in CZ (200 and 400 mg/kg) and morphine-treated groups, however during the second phase (30–35 min) significant reduction in formalin-induced pain response was observed in 100, 200, and 400 mg/kg CZ extract-treated group when compared to control group. CZ extract administration at 200 and 400 mg/kg dose caused a significant increase in the percentage of time spent in open arms in the elevated plus maze as compared to the control group. Conclusion: Results suggest that CZ bark extract possesses the antinociceptive activity and modulates anxiety-like behavior.

scholarly journals TO EVALUATE THE EFFECT OF MORUS ALBA LEAVES EXTRACT ON SLEEP AND ANXIETY IN RAT MODELS

2021 ◽  
pp. 100-102
Author(s):  
SRIHARSHA RAYAM ◽  
KUDAGI BL ◽  
RAMYA JONNALAGADDA ◽  
RAVEENDRA KUMAR NALLABOTHULA
Keyword(s):  
Elevated Plus Maze ◽  
Morus Alba ◽  
Control Group ◽  
Dependent Manner ◽  
Sleeping Time ◽  
Elevated Plus Maze Test ◽  
Plus Maze ◽  
The Mean ◽  
Mean Time ◽  
Dose Dependent

Objectives: The objectives of the study were to study the effect of Morus alba leaves extract (MAE) on sleep by phenobarbitone-induced sleeping time and the antianxiety effect by elevated plus maze apparatus model in rats. Methods: In this study, the effect of MAE on sleep was evaluated by the phenobarbitone-induced sleeping time of rats. The onset and the duration of sleep were recorded in minutes. The antianxiety effect was evaluated by the elevated plus maze apparatus model in rats. During 5 min test period, the number of entries into the open arm and closed arm and time spent in the open arm and closed arm were recorded in seconds. Results: MAE at the dose 200 and 400 mg/kg, highly significantly (p<0.001) decreased the onset of phenobarbitone-induced sleeping time. The duration of sleeping time was increased significantly (p<0.01) for 200 mg/kg and highly significantly (p<0.001) for 400 mg/kg as compared to the control group. M. alba has significant antianxiety activity in comparison with control in a dose-dependent manner. M. alba in a dose of 200 mg showed significant (p<0.01) and 400 mg/kg treated groups showed highly significant (p<0.001) anxiolytic activity by increasing the mean time spent in open arms as compared to control but less significant with standard (diazepam). Conclusion: Results indicate that the MAE has a significant dose-dependent effect on phenobarbitone- induced sleeping time and antianxiety effect in the elevated plus maze test.

scholarly journals Dose-Dependent, Antidepressant, and Anxiolytic Effects of a Traditional Medicinal Plant for the Management of Behavioral Dysfunctions in Animal Models

Dose-Response ◽  
2019 ◽  
Vol 17 (4) ◽  
pp. 155932581989126 ◽  
Author(s):  
Hafiz Muhammad Asif ◽  
Abdul Hayee ◽  
Muhammad Rahil Aslam ◽  
Khalil Ahmad ◽  
Abdul Sattar Hashmi
Keyword(s):  
Open Field ◽  
Elevated Plus Maze ◽  
Tail Suspension Test ◽  
Antidepressant Effect ◽  
Tail Suspension ◽  
Hydroalcoholic Extract ◽  
Elevated Plus Maze Test ◽  
Plus Maze ◽  
Immobility Time ◽  
Dose Dependent

The present work was carried out to assess the Onosma bracteatum anxiolytic and antidepressant properties. Swiss albino mice (male) were fed orally with hydroalcoholic extract at different doses 50, 100, and 200 mg 1 hour prior to test with the standard diazepam and fluoxetine. Anxiolytic and antidepressant activities were evaluated by using open field, elevated plus maze, force swimming, and tail suspension test. Results of open field test showed an increase in number of line crossing as well as number of rearing in dosage-dependent design. Although results of elevated plus maze test evidently showed antianxiety effect of O bracteatum by increasing the time spent in open arms along with decreasing the time spent in closed arms in dosage-dependent way. For the evaluation of antidepressant effect, O bracteatum diminished the immobility time and expanded mobility time in forced swim model in dosage-dependent way. Likewise, O bracteatum expanded time span of mobility along with diminished immobility time in tail suspension method in dosage-dependent way. Outcome demonstrated that plant at the dose of 200 mg/kg body weight showed significant potential which was similar to that standard diazepam and fluoxetine. Hence, O bracteatum may be used as potent natural psychotherapeutic agent against the mental disorders.

scholarly journals Antinociceptive Activity of Methanolic Extract ofClinacanthus nutansLeaves: Possible Mechanisms of Action Involved

2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
Zainul Amiruddin Zakaria ◽  
Mohammad Hafiz Abdul Rahim ◽  
Rushduddin Al Jufri Roosli ◽  
Mohd Hijaz Mohd Sani ◽  
Maizatul Hasyima Omar ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Methanolic Extract ◽  
Cholinergic Receptors ◽  
Antinociceptive Activity ◽  
Receptor Subtypes ◽  
Dependent Manner ◽  
Opioid Receptor Subtypes ◽  
Glutamatergic Signaling ◽  
Clinacanthus Nutans ◽  
Dose Dependent

Methanolic extract ofClinacanthus nutansLindau leaves (MECN) has been proven to possess antinociceptive activity that works via the opioid and NO-dependent/cGMP-independent pathways. In the present study, we aimed to further determine the possible mechanisms of antinociception of MECN using various nociceptive assays. The antinociceptive activity of MECN was (i) tested against capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged against selective antagonist of opioid receptor subtypes (β-funaltrexamine, naltrindole, and nor-binaltorphimine); (iii) prechallenged against antagonist of nonopioid systems, namely,α2-noradrenergic (yohimbine),β-adrenergic (pindolol), adenosinergic (caffeine), dopaminergic (haloperidol), and cholinergic (atropine) receptors; (iv) prechallenged with inhibitors of various potassium channels (glibenclamide, apamin, charybdotoxin, and tetraethylammonium chloride). The results demonstrated that the orally administered MECN (100, 250, and 500 mg/kg) significantly (p<0.05) reversed the nociceptive effect of all models in a dose-dependent manner. Moreover, the antinociceptive activity of 500 mg/kg MECN was significantly (p<0.05) inhibited by (i) antagonists of μ-,δ-, andκ-opioid receptors; (ii) antagonists ofα2-noradrenergic, β-adrenergic, adenosinergic, dopaminergic, and cholinergic receptors; and (iii) blockers of different K+channels (voltage-activated-, Ca2+-activated, and ATP-sensitive-K+channels, resp.). In conclusion, MECN-induced antinociception involves modulation of protein kinase C-, bradykinin-, TRVP1 receptors-, and glutamatergic-signaling pathways; opioidergic,α2-noradrenergic,β-adrenergic, adenosinergic, dopaminergic, and cholinergic receptors; and nonopioidergic receptors as well as the opening of various K+channels. The antinociceptive activity could be associated with the presence of several flavonoid-based bioactive compounds and their synergistic action with nonvolatile bioactive compounds.

Anticompulsive effects of novel derivatives of coumarin in rats

2021 ◽  
Vol 19 (3) ◽  
pp. 339-344
Author(s):  
Bakhodir B. Daliev ◽  
Eugenii R. Bychkov ◽  
Leonid V. Myznikov ◽  
Andrei A. Lebedev ◽  
Petr D. Shabanov
Keyword(s):  
Elevated Plus Maze ◽  
Anxiolytic Effect ◽  
Emotional Behavior ◽  
Central Action ◽  
Elevated Plus Maze Test ◽  
Anxiogenic Effect ◽  
Plus Maze ◽  
Few Data ◽  
New Compounds ◽  
Dose Dependent

BACKGROUND: Until now, the neurotropic effect, in particular the effect on the emotional behavior of oxy-coumarins, has not been adequately studied. There are only few data on their central action. Currently, research is underway on the synthesis of new compounds based on natural oxy-coumarins, which will potentially have a higher biological activity. AIM: Was to study the central action of new oxycoumarin-based compounds IEM-2886, LVM-99, LVM-S144, in particular, on compulsive behavior in rats. MATERIALS AND METHODS: To assess the behavior of Wistar rats, the Marble-test and Elevated plus maze methods were used. Oxycoumarin derivatives (IEM-2886, LVM-99, LVM-S144) were injected intraperitoneally at doses of 1, 10 and 25 mg/kg. The effectiveness of the drugs was judged by the number of balls buried in the Marble test and by the duration of staying in the open and closed sleeves of the Elevated plus maze. Results. It was shown that in the Marble test, oxycoumarin-based compounds (IEM-2886, LVM-99, LVM-S144) caused a decrease in the number of buried balls, which shows their anti-compulsive effect. After administration of IEM-2886, LVM-99, LVM-S144 (125 mg / kg) compounds, dose-dependent effects were observed (p 0.05). The elevated plus maze test did not show the anxiolytic effect typical for tranquilizers. Moreover, after the administration of IEM-2886 and LVM-S144 at a dose of 25 mg / kg, an increase in the time spent in the closed sleeve of the maze (p 0.05) was observed, i.e. an anxiogenic effect. CONCLUSION: Thus, oxy-coumarin-based compounds are selective for the assessment of anticompulsive effects.

scholarly journals Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine

2014 ◽  
Vol 50 (1) ◽  
pp. 73-81
Author(s):  
Martín Hermógenes Estrada ◽  
Henry Insuasty ◽  
Luis Enrique Cuca ◽  
Mariel Marder ◽  
Angélica Fierro ◽  
...  
Keyword(s):  
Maximal Electroshock ◽  
Dependent Manner ◽  
Maximal Electroshock Seizure ◽  
Gaba A ◽  
Mao B ◽  
Plus Maze ◽  
Marble Burying ◽  
One Step ◽  
Dose Dependent ◽  
Benzodiazepine Site

This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.

scholarly journals Evaluation of antinociceptive and antipyretic effect of Pupalia lappacea Juss

2013 ◽  
Vol 2 (2) ◽  
pp. 23-28 ◽  
Author(s):  
Vajrala Neeharika ◽  
Humaira Fatima ◽  
Bommineni Madhava Reddy
Keyword(s):  
Acetic Acid ◽  
Antinociceptive Effect ◽  
Ethanolic Extract ◽  
Pharmaceutical Journal ◽  
Dependent Manner ◽  
Hot Plate ◽  
Hot Plate Test ◽  
Antipyretic Activity ◽  
Cns Depressant ◽  
Dose Dependent

Pupalia lappacea Juss (Family: Amaranthaceae) is claimed to be useful in treatment of bone fracture, wounds, boils, cough, toothache, fever and malaria. The study was aimed to evaluate the 80% aqueous ethanolic extract of aerial parts of P. lappacea for antinociceptive and antipyretic activities to verify the traditional claim. The extract was orally administered at doses of 200, 400 and 600 mg/kg. The extract has significantly (P<0.01) reduced the nociception induced by acetic acid. The effect produced was in dose dependent manner. The antinociceptive effect was not reversed by pretreatment with naloxone in acetic acid induced writhing test. In hot plate method, the extract has significantly increased the latency time of jump. The naloxone has partially antagonised the antinociception of extract in hot plate test indicating P. lappacea has morphinomimetic properties. In the study of the CNS-depressant effects, the extract was found to produce significant reduction in head pokes and locomotion in mice by using hole board and locomotor activity test respectively. The extract has significantly reduced the rectal temperature in yeast induced pyrexia in rats at 600 mg/kg. The activity produced by extract was in dose dependent manner. Phytochemical investigation of ethanolic extract of P. lappacea revealed the presence of steroids and/or triterpenoids, flavonoids and phenolic compounds which may be responsible for antinociceptive and antipyretic activity of P. lappacea.DOI: http://dx.doi.org/10.3329/icpj.v2i2.13193 International Current Pharmaceutical Journal 2013, 2(2): 23-28

scholarly journals Analgesic, Antidiarrheal and CNS-depressant Activities of Flemingia macrophylla (Willd.)

2020 ◽  
Vol 23 (2) ◽  
pp. 141-145
Author(s):  
Asheka Rahman ◽  
Mohammad Mahmudul Hasan ◽  
Mohammad Abdullah Taher ◽  
Tanvir Muslim
Keyword(s):  
Methanol Extract ◽  
Pharmaceutical Journal ◽  
Developed Countries ◽  
Dependent Manner ◽  
Flemingia Macrophylla ◽  
Cns Depressant ◽  
Time Test ◽  
Analgesic Activities ◽  
Dose Dependent ◽  
Developing And Developed Countries

Plants are the priceless sources of bioactive natural compounds. Medicinal plants have been used since time immemorial in both developing and developed countries. Flemingia macrophylla (Willd.) is widely used as a hereditary medicines. The current study was designed to observe the analgesic, antidiarrheal and CNS depressant activities of methanol extract of the leaves of F. macrophylla (MEFM) and its petroleum ether (PEFM), dichloromethane (DFM), chloroform (CFM) and aqueous (AFM) fractions. The analgesic activities was assessed by acetic acid induced writhing method at doses 200- and 400- mg/kg body weight. The CNS-depressant effect was assayed by phenobarbitone sodium-induced sleeping time test. The anti-diarrheal activity of the extract was evaluated using castor oil-induced diarrhea in mice. The crude extract displayed significant peripheral analgesic activity at both test doses with 56.72- to 59.70-% inhibition of writhing responses, respectively. In CNS-depressant test, the extract revealed its activity in a dose dependent manner. In screening for antidiarrheal activity, the extract exhibited 20.83 and 41.67 % inhibition of defecation at 200- and 400-mg/kg bw, respectively whereas the standard loperamide (50 mg/kg bw) displayed 70.83 % inhibition of defecation. Bangladesh Pharmaceutical Journal 23(2): 141-145, 2020

ISOLATION OF TECOMINE FROM ALKALOID FRACTION, INVESTIGATION OF ADAPTOGENIC AND NEUROPSYCHOPHARMACOLOGICAL EFFECTSOF ETHANOLIC, ETHYL ACETATE AND HEXANE FLOWER EXTRACTS OF TECOMA GAUDICHAUDI

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (04) ◽  
pp. 63-74
Author(s):  
K. Ravishankar ◽  
◽  
G.V.N. Kiranmayi ◽  
Y. Rajendra Prasad
Keyword(s):  
Ethyl Acetate ◽  
Conditioned Avoidance ◽  
Vanillylmandelic Acid ◽  
Nootropic Activity ◽  
Dependent Manner ◽  
Spectrophotometric Methods ◽  
Plus Maze ◽  
Forced Swim Stress ◽  
Alkaloid Fraction ◽  
Dose Dependent

The present study aims to evaluate antistress and neuropharmacological parameters of ethanolic, ethyl acetate and hexane flower extracts of Tecoma gaudichaudi. Forced swim stress was used to evaluate antistress activity. The 24 h urinary excretion of vanillylmandelic acid (VMA) and ascorbic acid were determined by spectrophotometric methods in all groups under normal and stressed conditions. In the present study, the extracts (200 and 400 mg/kg, p.o.) were investigated for nootropic activity in rats with and without stress. Cook’s pole climbing apparatus measures conditioned avoidance response, elevated plus maze determines transfer latency and staircase test calculates the number of steps climbed and rearings in normal and stress induced rats to assess cognitive-improving activities. Cognition was enhanced by daily administration of Tecoma gaudichaudi extracts at doses of 200 and 400 mg/kg, p.o. in dose dependent manner in normal rats. Tecomine and its derivatives were isolated from alkaloidal fraction.

Sign in / Sign up

Export Citation Format

Share Document