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   Pharmacological evaluation of novel 1-[4-(4-benzo[1,3]dioxol-5-ylmethyl-piperazin-1-yl)-phenyl]-3-phenyl-urea as potent anticonvulsant and antidepressant agent  
   
نویسنده kumari s. ,mishra c.b. ,tiwari m.
منبع pharmacological reports - 2016 - دوره : 68 - شماره : 2 - صفحه:250 -258
چکیده    Background earlier,we have identified a number of piperazine derivatives having good anticonvulsant activity in vivo and as a part of our ongoing search for potent anticonvulsant agent,we herein describes the synthesis of an aryl piperazine derivative 1-[4-(4-benzo[1,3]dioxol-5-ylmethyl-piperazin-1-yl)-phenyl]-3-phenyl-urea (bppu). the anticonvulsant and antidepressant activity of bppu was checked in various in vivo models. methods anticonvulsant activity was assessed in maximal electroshock test (mes) and subcutaneous pentylenetetrazole (scptz) induced seizure tests. moreover,plausible mechanistic studies were also performed by using several chemical induced seizure models. the antidepressant activity of bppu was checked in forced swim test (fst) and tail suspension test (tst) in mice. drug safety profile was studied in sub-acute toxicity rat model at a dose of 100 mg/kg,per oral for 14 days. results bppu exhibited excellent protection against seizures induced by mes and scptz in mice as well as rats. in pilocarpine induced model of status epilepticus (se),bppu demonstrated 50% protection at a dose of 100 mg/kg in rats. bppu also successfully inhibited seizures induced by 3-mercaptopropionic acid (3-mpa) and thiosemicarbazide (tsc) in mice thus,suggested that bppu might influence gaba-ergic neurotransmission in the brain. moreover,bppu showed good antidepressant activity and did not exhibit any significant toxicity. conclusion bppu displayed broad spectrum of anticonvulsant activity in several seizure models along with satisfactory antidepressant activity. therefore,bppu may be further developed as a potential therapeutic agent for therapy of epileptic disorders. © 2015 institute of pharmacology,polish academy of sciences.
کلیدواژه Anticonvulsant; Antidepressant; Piperazine; Synthesis; Toxicity
آدرس bio-organic chemistry laboratory,dr. b.r. ambedkar center for biomedical research,university of delhi,new delhi, India, bio-organic chemistry laboratory,dr. b.r. ambedkar center for biomedical research,university of delhi,new delhi, India, bio-organic chemistry laboratory,dr. b.r. ambedkar center for biomedical research,university of delhi,new delhi, India
 
     
   
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