Chronopharmacological studies of phenylbutazone in the rat

1983 ◽  
Vol 61 (6) ◽  
pp. 649-652 ◽  
Author(s):  
G. Labrecquf ◽  
P. M. Bélanger ◽  
F. M. Doré

Temporal variations in the anti-inflammatory action and in the ulcerogenic and lethal effects of phenylbutazone were studied in rats. The results indicate that small doses of the drug produced a larger reduction of paw edema in the morning than in the evening. At 0900, doses of 10, 30, and 100 mg/kg of phenylbutazone reduced the carrageenan-induced paw edema by 23, 44, and 66%, respectively. At 2000, the same doses of the drug decreased the paw edema by 9, 22, and 62%, respectively. No circadian variation was observed in the ulcerogenic effect of phenylbutazone. The mean lethal dose (LD50) of the drug was larger in the morning than in the evening and the values obtained were 710 ± 24 (SE) mg/kg at 0900 in comparison to 525 ± 38 (SE) mg/kg at 2000.

2018 ◽  
Vol 24 (4) ◽  
pp. 231-236 ◽  
Author(s):  
Dorota Żelaszczyk ◽  
Anna Lipkowska ◽  
Natalia Szkaradek ◽  
Karolina Słoczyńska ◽  
Agnieszka Gunia-Krzyżak ◽  
...  

AbstractXanthone derivatives of acetic, propionic and 2-methylpropionic acids were synthesized and assayed for their anti-inflammatory, analgesic and ulcerogenic activities. Compound 8 causes a dose-dependent diminution of paw edema (up to 61%) in the carrageenan model and at the highest tested dose reduces mechanical hyperalgesia in the Randall-Selitto test more effectively than the reference compound (~75% and ~32%, respectively). It shows high in vitro metabolic stability (Clint=12.5 μL/mg/min, t1/2=138.6 min) in the rat liver microsomes. None of the studied xanthone derivatives are ulcerogenic. The results of the present study suggest that compound 8 can be of interest in the future for the search for antinociceptive and antiedematous agents devoid of ulcerogenic effect.


2020 ◽  
pp. 1-2
Author(s):  
M. Medhabati ◽  
L. Babycha ◽  
L. Tarinita ◽  
Bikram Tewari ◽  
Saumya Kanti Sinha

In the present study, the anti-inflammatory activity of aqueous extract of Portulaca oleracea (POE 200, 400 and 600mg/kg) was studied using carrageenan induced paw oedema in albino rats. The mean increase in paw volume was recorded. POE produced significant (p<,0.01) anti-inflammatory activity when compared to the control. The anti-inflammatory action of POEcan be attributed to its flavonoid contents which are known to act through inhibition of prostaglandin biosynthesis. However, the test drug at maximum dose (600mg/kg) was found to be less effective than the standard drug, aspirin (100mg/Kg).


1957 ◽  
Vol 35 (11) ◽  
pp. 1029-1031 ◽  
Author(s):  
Hans Selye

Experiments on adrenalectomized rats maintained on small doses of cortisol acetate and desoxycorticosterone acetate indicate that aminoacetonitrile markedly inhibits the production of inflammatory exudate in the "granuloma pouch" test. It is concluded that this antiphlogistic effect is an inherent property of the lathyrogenic aminonitrile and not merely the consequence of an adrenal-mediated stressor action.


1957 ◽  
Vol 35 (1) ◽  
pp. 1029-1031
Author(s):  
Hans Selye

Experiments on adrenalectomized rats maintained on small doses of cortisol acetate and desoxycorticosterone acetate indicate that aminoacetonitrile markedly inhibits the production of inflammatory exudate in the "granuloma pouch" test. It is concluded that this antiphlogistic effect is an inherent property of the lathyrogenic aminonitrile and not merely the consequence of an adrenal-mediated stressor action.


2021 ◽  
Vol 17 (2) ◽  
pp. 189-199
Author(s):  
Amina B. Olorukooba ◽  
Ferhat Khan ◽  
Yahya M. Sani ◽  
Asmau N. Hamza ◽  
Aisha O. Musa

Uapaca togoensis Pax. (Euphorbiaceae) is used in traditional medicine to treat several diseases including pain, inflammation and fever. This study investigated analgesic, anti-inflammatory and anti-pyretic effects of the residual aqueous fraction of the plant. Preliminary phytochemical screening and acute toxicity studies were conducted. Analgesic activity was evaluated using acetic acid-induced writhing, hot plate and formalin-induced pain tests at doses of 250, 500 and 1000 mg/kg, p.o. Anti-inflammatory and antipyretic activities were investigated using carrageenaninduced paw edema and Brewer’s yeast-induced pyrexia model respectively in rats. Oral median lethal dose of the fraction was found to be greater than 5000 mg/kg. The fraction significantly (p<0.05) reduced the number of acetic acid-induced writhes and increased the reaction time of mice to thermal stimuli. In the formalin test, a significant (p<0.05) reduction in mean pain score was observed at the second phase. A significant (p<0.05) decrease in paw edema at the 4th and 5th hours and a reduction in temperature was also observed at the 22nd hour. Phytochemical screening revealed the presence of saponins, tannins, steroids, cardiac glycosides, flavonoids, alkaloids and triterpenes. The result of the study revealed that the fraction possesses analgesic, anti-inflammatory and antipyretic activities, validating the folkloric use of the plant. Keywords: Analgesic, Anti-inflammatory, Anti-pyretic, Uapaca togoensis, Residual Aqueous Fraction


Author(s):  
N. Ya. Golovenko ◽  
T. A. Kabanova ◽  
S. A. Andronati ◽  
O. I. Halimova ◽  
V. B. Larionov ◽  
...  

Background. Propoxazepam, 7-bromo-5-(2-chlorophenyl)-3-propoxy-1H-benzo[e][1,4]diazepin-2(3H)-one, is a promising analgesic and anticonvulsant and is on preclinical trial. Objective. The aim of the research was to study the anti-inflammatory and analgesic action of Propoxazepam. Methods. The anti-inflammatory action was evaluated by carrageenan induced rat paw edema, formalin-induced paw licking response in mice and bradykinin-induced pain response in rat models. Results. It was established for the first time that the administration of Propoxazepam caused a significant anti-inflammatory activity when tested in different in vivo chemical experimental models of induced inflammation, i.e. carrageenan-, bradykinin- and formalin-induced inflammation tests. Conclusions. Propoxazepam significantly reduced acute and sub-acute inflammation and proved its efficacy and similar to anti-inflammatory action.


Author(s):  
Purna Prasad Meegada ◽  
Rama Mohan Pathapati ◽  
Sriharsha Rayam ◽  
Raveendra Kumar Nallabothula

Background: The onion plant (Allium cepa) is the most widely cultivated species of the genus Allium. It has antibiotic, antidiabetic, antihypercholesterolemic, antioxidant, hemostatic, antimutagenic effects. The current study is aimed to evaluate analgesic and anti-inflammatory properties of Allium cepa extracts in rat models.Methods: In this study analgesic activity in rats is tested by Eddy’s hot plate method, tail flick method. In Eddy’s hot plate method rats are individually placed on the heated plate of the analgesic meter maintained at 550C and mean reaction time was calculated at regular time intervals. In tail flick method the tail withdrawal from the heat (flicking response) is taken as the end point. Anti-inflammatory property is studied by carrageenan induced paw edema model, in which the paw volume is measured with a plethysmograph.Results: In Eddy’s hot plate method the mean reaction time increased significantly (p<0.05) with high dose of Allium cepa at 1 hour and 2 hours when compared to control. In tail flick method the mean reaction time is increased significantly (p<0.05) with high dose of Allium cepa at 1 hour and 1.5 hour when compared to control. In carrageenan induced paw edema method Allium cepa exhibited anti-inflammatory activity by significant (p<0.05) suppression of paw edema when compare to control at 1 hour after carrageenan injection to rat paw.Conclusions: Allium cepa has significant analgesic and anti-inflammatory activity in hot plate, tail flick and carrageenan induced paw edema model.


Pharmacia ◽  
2020 ◽  
Vol 67 (3) ◽  
pp. 121-127
Author(s):  
Taras Chaban ◽  
Vasyl Matiychuk ◽  
Olexandra Komarytsya ◽  
Iryna Myrko ◽  
Ihor Chaban ◽  
...  

Synthesis of novel N3 and C5 substituted thiazolo[4,5-b]pyridin-2-ones was carried out on the basis of [3+3]-cyclocodensation, acylation and alkylation reactions. The structures of the obtained compounds were confirmed by 1H NMR spectroscopy, and elemental analysis. The anti-inflammatory action of novel thiazolo[4,5-b]pyridine-2-one derivatives was evaluated in vivo employing the carrageenan-induced rat paw edema method. When compared with Ibuprofen, some our compounds were found to be more potent. Graphical abstract


2010 ◽  
Vol 65 (9-10) ◽  
pp. 543-550 ◽  
Author(s):  
Reinaldo N. de Almeida ◽  
Damião P. de Sousa ◽  
Enilton A. Camargo ◽  
Fernando S. Oliveira

Hydroxydihydrocarvone (HC) is a synthetic intermediate obtained by hydration of the natural compound (R)-(-)-carvone. The aim of the present study was to investigate the possible anti-inflammatory activity of orally administered HC. Toxicity, motor coordination, tail immersion test, as well as carrageenan-induced paw edema and myeloperoxidase (MPO) activity or peritonitis were all evaluated in rodents. HC was force-fed to the animals 1 h before the stimulus. The lethal dose 50% (LD50) of orally administered HC was 1259 mg/kg. No changes in motor coordination were recorded in HC-treated mice in the rotarod test. The time of response to the thermoceptive stimulus in the tail immersion test was longer in HC-treated animals (50, 100, and 200 mg/kg) than in the vehicle-treated group. HC also significantly decreased the area under curve of carrageenan-induced rat paw edema at 100 and 200 mg/kg and MPO activity at 200 mg/kg. Carrageenan-induced neutrophil recruitment to the peritoneal cavity was significantly reduced by HC at doses of 100 or 200 mg/kg, but not 50 mg/kg. These findings demonstrate that orally administered HC exerts antinociceptive and anti-inflammatory activities in rats and mice.


Author(s):  
Samira Salem ◽  
Essaid Leghouchi ◽  
Rachid Soulimani ◽  
Jaouad Bouayed

Abstract. Paw edema volume reduction is a useful marker in determining the anti-inflammatory effect of drugs and plant extracts in carrageenan-induced acute inflammation. In this study, the anti-inflammatory effect of Lobaria pulmonaria (LP) and Parmelia caperata (PC), two lichen species, was examined in carrageenan-induced mouse paw edema test. Compared to the controls in carrageenan-induced inflammation (n = 5/group), our results showed that pretreatment by single oral doses with PC extract (50–500 mg/kg) gives better results than LP extract (50–500 mg/kg) in terms of anti-edematous activity, as after 4 h of carrageenan subplantar injection, paw edema formation was inhibited at 82–99% by PC while at 35–49% by LP. The higher anti-inflammatory effect of PC, at all doses, was also observed on the time-course of carrageenan-induced paw edema, displaying profile closely similar to that obtained with diclofenac (25 mg/kg), an anti-inflammatory drug reference (all p < 0.001). Both LP and PC, at all doses, significantly ameliorated liver catalase (CAT) activity (all p < 0.05). However, superoxide dismutase (SOD) activity, glutathione peroxidase (GPx) activity and glutathione (GSH) levels were found increased in liver of PC- compared to LP-carrageenan-injected mice. Our findings demonstrated on one hand higher preventive effects of PC compared to LP in a mouse carrageenan-induced inflammatory model and suggested, on the other hand, that anti-inflammatory effects elicited by the two lichens were closely associated with the amelioration in the endogenous antioxidant status of liver.


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