Anticonvulsant and acute neurotoxic characteristics of nicotinic acid benzylamide:a preclinical study.
Journal Title: Pharmacological Reports - Year 2006, Vol 58, Issue 3
Abstract
The aim of this study was to evaluate time-course and dose-response relationships of nicotinic acid benzylamide (Nic-BZA) with regard to its anticonvulsant activity in the maximal electroshock(MES)-induced seizures and acute neurotoxic effects in terms of motor coordination impairment in the chimney test in mice. The experimental determination of both median effective dose (ED(50)) and median toxic dose (TD(50)) allowed for the calculation of protective index (PI) values characterizing a preclinical profile of Nic-BZA. Results indicated that Nic-BZA produced the time-dependent and clear-cut anticonvulsant activity in the MES test and its ED(50) values ranged between 35.7 and 84.0 mg/kg (after the ip administration of the agent at 5 and 60 min, respectively), and between 72.0 and 152.1 mg/kg (at 5 and 60 min, respectively, following the po administration of Nic-BZA). In the chimney test, the TD(50) values for Nic-BZA, after its ip administration ranged between 188.5 and 509.9 mg/kg, whereas following its po administration the TD(50) values for Nic-BZA were between 552 and 1222.1 mg/kg. The PI values for Nic-BZA, calculated at various times after its ip and po administrations (ranging between 3.56 and 17), revealed that the agent has a favorable profile, when considering its both anticonvulsant and acute neurotoxic effects in this preclinical study. Based on this study, one can conclude that Nic-BZA might occur advantageous as a potential antiepileptic drug for breaking seizure attacks in patients with epilepsy.
Authors and Affiliations
Mariusz Świąder, Jarogniew Łuszczki, Ryszard Paruszewski, Stanisław Czuczwar, Waldemar Turski
Keywords
Related Articles
- EP ID EP144364
- DOI -
- Views 97
- Downloads 0
Involvement of PI3-K in neuroprotective effects of the 1,25-dihydroxyvitamin D(3) analogue - PRI-2191.
The active form of 1,25-dihydroxyvitamin D(3) prevents neuronal damage in vitro and in vivo , however, it induces also hypercalcemia and hyperphosphatemia. Side-chain-modified analogues of 1,25-dihydroxyvitamin D(3), whi...
Anxiolytic effect of noscapine in mice.
The anxiety-related effects of noscapine were investigated using male Balb-c mice. Since noscapine-induced locomotion may alter the animals' activity level in the dark-light model, the anxiety-related effects of noscapin...
Caffeine and the anticonvulsant potency of antiepileptic drugs: experimental and clinical data.
Caffeine (1,3,7-trimethylxanthine) is the most commonly ingested stimulant in the world. The daily consumption of this methylxanthine in coffee, tea and soft drinks is approximately 200 mg per person, which yields a phar...
Impact of maternal separation on neural cell adhesion molecules expression in dopaminergic brain regions of juvenile, adolescent and adult rats.
Stressful experiences in the early stages of life can influence brain development and maturation, and they can also increase the risk for some psychiatric disorders; however, the specific mechanisms of this effect are st...
Effect of an NMDA receptor agonist on T-maze and passive avoidance test in 12-week streptozotocin-induced diabetic rats.
This study examined behavioral effects mediated by NMDA (N-methyl-D-aspartic acid) receptors in 12-week streptozotocin (STZ)-induced diabetic rats. Effects of an NMDA receptor agonist on behavior in the open field test,...