Anticonvulsant activity of the neuroactive steroid allopreganolone

2015 ◽  
Vol 67 (1) ◽  
pp. 169
Author(s):  
Dorota Zolkowska
Keyword(s):  
Anticonvulsant Activity ◽  
Neuroactive Steroid

Anxiolytic and anticonvulsant activity of a synthetic neuroactive steroid Co 3-0593

1997 ◽  
Vol 134 (1) ◽  
pp. 46-54 ◽  
Author(s):  
Scott Wieland ◽  
James Belluzzi ◽  
Jon E. Hawkinson ◽  
Derk Hogenkamp ◽  
R. Upasani ◽  
...  
Keyword(s):  
Anticonvulsant Activity ◽  
Neuroactive Steroid

Synthesis and Anticonvulsant Activity of Some Novel 2-Methyl Imidazole Derivatives

2012 ◽  
Vol 9 (4) ◽  
pp. 402-408 ◽  
Author(s):  
Rahul Mishra ◽  
Swastika Ganguly ◽  
Kalyan Kumar Sethi ◽  
Papiya Mitra Mazumder
Keyword(s):  
Anticonvulsant Activity ◽  
Imidazole Derivatives ◽  
Methyl Imidazole

Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones

2014 ◽  
Vol 11 (5) ◽  
pp. 628-635
Author(s):  
Zi-Shi Zhu ◽  
Shi-Ben Wang ◽  
Xian-Qing Deng ◽  
Da-Chuan Liu ◽  
Zhe-Shan Quan
Keyword(s):  
Anticonvulsant Activity ◽  
Activity Evaluation

Anticonvulsant Activity and 5-HT1A/5-HT7 Receptors Affinity of Piperazine Derivatives of 3,3-Diphenyl- and 3,3-Dimethyl-succinimides

2012 ◽  
Vol 10 (2) ◽  
pp. 173-182 ◽  
Author(s):  
Jolanta Obniska ◽  
Iwona Chlebek ◽  
Krzysztof Kaminski ◽  
Andrzej J.Bojarski ◽  
Grzegorz Satala
Keyword(s):  
Anticonvulsant Activity ◽  
Piperazine Derivatives ◽  
Derivatives Of

Lacosamide Derivatives with Anticonvulsant Activity as Carbonic Anhydrase Inhibitors. Molecular Modeling, Docking and QSAR Analysis

2014 ◽  
Vol 10 (2) ◽  
pp. 160-167 ◽  
Author(s):  
Juan Martinez ◽  
Esteban Vega-Hissi ◽  
Matias Andrada ◽  
Pablo Duchowicz ◽  
Francisco Torrens ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Carbonic Anhydrase ◽  
Anticonvulsant Activity ◽  
Carbonic Anhydrase Inhibitors ◽  
Qsar Analysis

Design, Synthesis, Anticonvulsant Activity, Preclinical Study and Pharmacokinetic Performance of N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin- 2-yl] methyl}, 2-[(2-isopropyl-5-methyl) 1-cyclo Hexylidene] Hydrazinecarboxamide

2019 ◽  
Vol 19 (1) ◽  
pp. 31-45
Author(s):  
Meena K. Yadav ◽  
Laxmi Tripathi
Keyword(s):  
Anticonvulsant Activity ◽  
Computational Study ◽  
Plasma Concentrations ◽  
Elimination Rate ◽  
Area Under The Curve ◽  
Preclinical Study ◽  
In Vivo Studies ◽  
Maximum Plasma ◽  
Seizure Models

Background: N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin-2-yl] methyl}, 2-[(2- isopropyl-5-methyl) 1-cyclohexylidene] hydrazinecarboxamide QS11 was designed by computational study. It possessed essential pharmacophoric features for anticonvulsant activity and showed good docking with iGluRs (Kainate) glutamate receptor. Methods: QSAR and ADMET screening results suggested that QS11 would possess good potency for anticonvulsant activity. QS11 was synthesised and evaluated for its anticonvulsant activity and neurotoxicity. QS11 showed protection in strychnine, thiosemicarbazide, 4-aminopyridine and scPTZ induced seizure models and MES seizure model. QS11 showed higher ED50, TD50 and PI values as compared to the standard drugs in both MES and scPTZ screen. A high safety profile (HD50/ED50 values) was noted and hypnosis, analgesia, and anaesthesia were only observed at higher doses. No considerable increase or decrease in the concentration of liver enzymes was observed. Optimized QS11 was subjected to preclinical (in-vivo) studies and the pharmacokinetic performance of the sample was investigated. The result revealed that the pharmacokinetic performance of QS11 achieved maximum plasma concentrations (Cmax) of 0.315 ± 0.011 µg/mL at Tmax of 2.0 ± 0.13 h, area under the curve (AUC0-∞) value 4.591 ± 0.163 µg/ml x h, elimination half-life (T1/2) 6.28 ± 0.71 h and elimination rate constant was found 0.110 ± 0.013 h-1. Results and Conclusion: Above evidences indicate that QS11 could serve as a lead for development of new antiepileptic drugs.

Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives

2018 ◽  
Vol 17 (6) ◽  
pp. 448-457 ◽  
Author(s):  
Xia Huang ◽  
Tie Chen ◽  
Rong-Bi Han ◽  
Feng-Yu Piao
Keyword(s):  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Anticonvulsant Activity ◽  
Mass Spectra ◽  
Maximal Electroshock ◽  
Test Compound ◽  
Maximal Electroshock Test ◽  
Mes Test ◽  
Structure Activity

Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1). Conclusion: Possible structure-activity relationship was discussed.

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