Current Issue : October - December Volume : 2013 Issue Number : 4 Articles : 6 Articles
Agomelatine is a potent MT1 and MT2 melatonin receptor agonist and a 5-HT2C serotonin receptor antagonist and also has anticonvulsant property .We analyzed whether agomelatine has the potential to inhibit or attenuate ethanol withdrawal induced handling convulsion in mice or not .The anticonvulsant activity of agomelatine (75 mg/kg, i.p.) was evaluated in mouse models of pentylenetetrazole .In the PTZ-induced seizure model, agomelatine treatment was given where acute treatment showed protection against convulsion while chronic agomelatine treatment showed complete absence of convulsions....
The object of study was to develop and compare the new method dose weight response curve with graphical dose response curve (DRC) method to study drug receptor interaction and dose response relationship in experimental pharmacology. The graphical DRC method was performed by adding graded doses of acetylcholine and it has produced dose dependent increase in tissue contraction and response. For dose weight response curve method the assembly was setup and same graded response of acetylcholine were added and it has produced dose dependent increase in tissue contraction and response in terms of weight reduction. For establishment and validation of dose weight response curve method different experiment were performed using isolated chicken ileum such as concentration response curve, potentiating effect and antagonistic effect and results compared with graphical dose response curve. The result suggests that a dose weight response curve method is simple, ease of setup of assembly, accurate, sensitive, precise and feasible for the purpose of experiment on isolated preparation and various bioassay methods....
Diabetes mellitus is associated with disturbances of cognitive functioning. Diabetes impaired spatial learning and memory of rats. The aim of this study was to examine cognitive functioning in diabetic rats. Diosmin has been reported to exhibit anti-hyperglycemic, antioxidant effects. Therefore we tested its efficacy against memory dysfunction in streptozotocin-induced diabetic rats. Diosmin was administered to streptozotocin-induced diabetic rats at different doses ( 50, 100 mg/kg b.w)for four weeks . Thirty days after diabetes induction rats showed a severe deficit in learning and memory associated with increased lipid peroxidation,nitric oxide level decreased reduced glutathione, and elevated ChE activity in hippocal region. Different parameter such as Morris water maze , object recognition test were performed . Lipid peroxidation and glutathione levels as parameters of oxidative stress was evaluated.To rule out possibility for locomotor activity open field test was conducted. In conclusion diosmin showed marked improvement in memory of diabetic rats ,prevent changes in oxidative stress and cholinesterase activity. . Furthermore, protection against body weight loss of diabetic animals was also observed. These concluded that diosmin has potential in treatment of diabetic memory dysfunction....
Alzheimer’s disease is one of the most serious neurodegenerative disorders occurring mainly in the old age. It results into memory and cognitive impairment leading to inability to perform routine tasks in day to day life and worsening of quality of life. Excitotoxic-neurodegeneration caused by over functioning of glutamatergic transmission is of the main pathophysiological aspects. Glutamate release is mainly mediated by sodium channels and blockade of these channels decreases the excessive release of this excitatory neurotransmitter. The previous study has already revealed Mexiletine, a sodium channel blocker established as an anti-arrhythmic agent, as a remedy in progressive Alzheimer’s disease caused by excitotoxicity. It was found out that Mexiletine averted memory impairment in mice which were administered aluminum chloride to produce Excitotoxic-neurodegeneration. The protective effect was evident in animal models of passive avoidance and elevated plus maze and was comparable with standard drug Memantine. Fluorometric estimation was undertaken to measure amount of glutamate present in homogenates of animal brains of each group animals. Brain homogenates of animals treated with Mexiletine exhibited low fluorescence indicating low amount of glutamate, while that of positive control group animals showed significantly higher fluorescence and presence of higher amount of glutamate. Brain homogenates with Memantine also showed less amount of glutamate released probably because of its capacity to block calcium channels and not sodium channels. It is well stipulated that beneficiary effect of Mexiletine in the treatment of Alzheimer’s disease is attributed to its capacity to block sodium channels, control release of glutamate and ultimately averting Excitotoxic-neurodegeneration....
The present study was aimed to develop an in-vitro model for estimating the potency of three H1-antagonists (chlorpheniramine maleate, promethazine theoclate and dimenhydrinate). We have evaluated histamine-induced contractions in various tissues such as guinea-pig ileum, rat ileum, goat ileum and goat tracheal smooth muscle in absence and presence of various concentrations of antihistamines. Histamine-induced contractions were H1-receptor-mediated effect, which were competitively inhibited by the antihistamines. The pD2 values of chlorpheniramine maleate, promethazine theoclate and dimenhydrinate were found to be 8.67±0.00, 7.78±0.00 and 6.35±0.00 in g.pig ileum, 6.67±0.00, 5.78±0.00 and 4.61±0.00 in rat ileum, 6.37±0.00, 5.48±0.00 and 4.37±0.00 in goat ileum, and 6.29±0.00, 5.36±0.00 and 4.27±0.00 in goat trachea respectively. There appeared to be a marked difference in sensitivity to histamine in the tissue preparations used. The pA2 values of chlorpheniramine maleate, promethazine theoclate and dimenhydrinate were found to be 7.98±0.02, 6.93±0.03 and 5.47±0.02 in g.pig ileum, 5.69±0.03, 4.79±0.02 and 3.75±0.01 in rat ileum, 5.38±0.02, 4.45±0.01 and 3.37±0.02 in goat ileum and 5.25±0.01, 4.33±0.02 and 3.27±0.03 in goat trachea respectively by Schild plot method. The contractions were concentration-dependent and surmountable and slope was not significantly different from unity, which indicates that nature of antagonism of antihistamines were reversible and competitive type. The results indicated, the increasing order of potency of antihistamines as dimenhydrinate < promethazine theoclate < chlorpheniramine maleate....
Furosemide is potent loop diuretic and widely prescribed for the treatment for hypertension as a single drug therapy and multidrug therapy. It is also used for the treatment of edema, acute pulmonary edema, cerebral edema, hypercalcemia and renal insufficiency. Long term use of furosemide may produce genotoxicity as per recent evidence. There are several studies had been done to prove genotoxic potential of furosemide. However, the results are varied as some suggests its genotoxic potential or its weak genotoxic potential while some had reported that furosemide is not genotoxic and some results are still inconclusive. So there is need to study further about its genotoxic potential after recollecting all the data of its genotoxicity....
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