Potential anticonvulsants: Substituted N-benzylidene derivatives of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins

1983 ◽  
Vol 48 (4) ◽  
pp. 1173-1186 ◽  
Author(s):  
Václav Bártl ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Marie Bartošová ◽  
Miroslav Protiva
Keyword(s):  
Acute Toxicity ◽  
Water Soluble ◽  
Hypotensive Activity ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Soluble Salts ◽  
Sleeping Time ◽  
Central Depression ◽  
Derivatives Of ◽  
Electroshock Seizures

Reactions of 10-(4-aminopiperazino)-10,11-dihydrodibenzo[b,f]thiepins XIVa-XIVd with benzaldehyde, 3,4-dimethoxybenzaldehyde, 4-dimethylaminobenzaldehyde, salicylaldehyde, 3-ethoxy-4-hydroxybenzaldehyde, 2-(2-dimethylaminoethoxy)benzaldehyde, 3-(2-dimethylaminoethoxy)benzaldehyde and 3-ethoxy-4-(2-dimethylaminoethoxy)benzaldehyde afforded a series of 19 hydrazones IIIa-Xc. Some of them showed the expected anticonvulsant effect but only towards pentetrazole; antagonism of maximal electroshock seizures was not observed. In general, the products have a character of tranquillizers: in higher does they produce central depression, potentiate the thiopental sleeping time, have hypothermic action; in single cases antiamphetamine, antireserpine, antihistamine and cataleptic effects were observed. The water-soluble salts of the basic hydrazones VIIIa, VIIIc, IXc and Xc, administered parenterally, showed a rather high acute toxicity and revealed also adrenolytic and hypotensive activity.

Effects of Carbon Dioxide and Oxygen on Properties of Experimental Seizures in Mice

1955 ◽  
Vol 184 (1) ◽  
pp. 202-208 ◽  
Author(s):  
Dixon M. Woodbury ◽  
Lawrence T. Rollins ◽  
Joyce R. Henrie ◽  
Joseph C. Jones ◽  
Tada Sato
Keyword(s):  
Carbon Dioxide ◽  
Carbon Dioxide Concentration ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Low Oxygen ◽  
Excitatory Effect ◽  
The Brain ◽  
Electroshock Seizures ◽  
Tonic Phase ◽  
Convulsant Dose

The influence of various concentrations of carbon dioxide and oxygen on the pattern of maximal electroshock seizures (MES), on pentylenetetrazol (Metrazol)-induced seizures, and on recovery time (RT50) from MES has been studied in mice. The major results are summarized as follows: Increasing the concentration of carbon dioxide in 20% oxygen resulted in marked changes in the MES pattern. The duration of the tonic flexor component was increased, and the duration of the tonic extensor component and of the entire tonic phase was decreased; the ratio of flexion to extension was increased markedly. These changes indicate an anticonvulsant effect of carbon dioxide. Carbon dioxide in a concentration of 15.6% protected 50% of mice against a 97% convulsant dose (CD97) of Metrazol. Hypoxia, induced by inhalation of 15 or 10% oxygen, decreased the duration of the tonic flexor component and increased the duration of the tonic extensor component of the MES; the duration of the entire tonic phase was increased; the ratio of flexion to extension was slightly decreased. These changes indicate an excitatory effect of low oxygen concentrations on the brain, under the stated conditions. Hyperoxia, induced by inhalation of 50, 75 or 90% oxygen, in contrast to hypoxia, resulted in effects on MES similar to those produced by inhalation of carbon dioxide. The RT50 was slightly, but not significantly, decreased by hypoxia (15% oxygen), unchanged by hyperoxia (50% oxygen), and markedly increased by an increase in carbon dioxide concentration. Carbon dioxide (5 and 10%) combined with hypoxia (10% oxygen) produced effects on MES pattern and RT50 similar to those produced by carbon dioxide in 20% oxygen.

scholarly journals Protective Effect of Cucurbita maxima against Maximal Electroshock Induced Convulsions

2021 ◽  
pp. 91-101
Author(s):  
Nagnath R. Kadam ◽  
P. K. Mohanty ◽  
Ashish Jain
Keyword(s):  
Protective Effect ◽  
Albino Rats ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Cucurbita Maxima ◽  
Hydroalcoholic Extract ◽  
Indigenous Plant ◽  
Wistar Albino Rats ◽  
Electroshock Seizures ◽  
Different Doses

In the present investigation, an indigenous plant, Cucurbita maxima was studied for its protective effect against maximal electroshock (MES) induced convulsions in Wistar albino rats. The rats were pretreated with different doses (100, 200, 400 mg/kg) of hydroalcoholic extract of seeds of Cucurbita maxima for 14 days and then, they were subjected to maximal electroshock seizures (40 mA for 0.2 sec) treatment. Hydroalcoholic extract of Cucurbita maxima seeds at 200 and 400 mg/kg doses significantly reduced the duration of hind limb extension along with the protection of rats against maximal electroshock induced seizures. The reference standard i.e., phenytoin (20 mg/kg) provided complete protection. Thus, present study revealed anticonvulsant effect of Cucurbita maxima against maximal electroshock-induced convulsions in rats.

scholarly journals Anticonvulsant activity of nicardipine in experimentally induced seizures in wistar albino rats.

2020 ◽  
Vol 9 (3) ◽  
pp. 413
Author(s):  
Kayalvizhi M. K. ◽  
Sathiya Vinotha A. T.
Keyword(s):  
Experimental Animal ◽  
Anticonvulsant Activity ◽  
Albino Rats ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Standard Drug ◽  
Wistar Albino Rats ◽  
Electroshock Seizures ◽  
Experimentally Induced

Background: The objective of the study was to evaluate the anticonvulsant activity of nicardipine in wistar albino rats.Methods: Anticonvulsant activity of nicardipine in a dose 10 mg/kg, and its effect with the standard drug lamotrigine (5 mg/kg) was studied in a maximal electroshock seizures (MES) experimental animal model.Results: Nicardipine in dose of 10 mg/kg showed significant anticonvulsant effect (p<0.001) and combination with standard drug lamotrigine (p<0.001) also showed more significant anticonvulsant effect in MES model.Conclusions: Nicardipine is having anticonvulsant activity and it also potentiates the anticonvulsant effect of lamotrigine in MES model.

scholarly journals Anticonvulsant Effect of Alcea aucheri on Pentylenetetrazole and Maximal Electroshock Seizures in Mice

2020 ◽  
pp. 369-378
Author(s):  
Tajmah Mombeini ◽  
Babak Asadpour Behzadi ◽  
Ramtin Ejtemaei ◽  
Freidoun Tahmasbi ◽  
Mohammad Kamalinejad ◽  
...  
Keyword(s):  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Electroshock Seizures

scholarly journals Evaluation of anticonvulsant activity of amlodipine in albino rats

2017 ◽  
Vol 6 (3) ◽  
pp. 664
Author(s):  
Roopa B. ◽  
Janardhan M. ◽  
Venkata Rao Y.
Keyword(s):  
Experimental Animal ◽  
Anticonvulsant Activity ◽  
Low Dose ◽  
Combination Group ◽  
Albino Rats ◽  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Standard Drug ◽  
Dose Dependent ◽  
Electroshock Seizures

Background: The objective of the study was to evaluate the anticonvulsant activity of amlodipine in albino rats.Methods: Anticonvulsant activity of amlodipine was done in three graded doses (1 mg/kg, 2 mg/kg, 4 mg/kg), and combination group with low dose of amlodipine (1 mg/kg) and standard drug (phenytoin) in maximal electroshock seizures (MES) experimental animal model.Results: Amlodipine in dose of 2, 4 mg/kg showed dose dependent significant anticonvulsant effect and combination of low dose amlodipine and low dose of standard drug also showed significant anticonvulsant effect in MES model.Conclusions: Amlodipine is having anticonvulsant activity and also potentiated the anticonvulsant effect of phenytoin in MES model. 

Initial Studies of a Potent Antiheparin Agent (Ubiquin®)

1968 ◽  
Vol 20 (03/04) ◽  
pp. 588-595 ◽  
Author(s):  
E. B Goodsell ◽  
R. A Krause ◽  
E. T Kimura
Keyword(s):  
Side Effects ◽  
Acute Toxicity ◽  
Propylene Oxide ◽  
Toluidine Blue ◽  
Water Soluble ◽  
Per Se

SummaryUbiquin (oligo-3-(N-methylmorpholinium)-l,2-propylene oxide chloride) is a stable, water soluble, active heparin antagonist producing prompt neutralization when administered in a 1:1 ratio to rats and dogs. Initial studies indicate that it is devoid of any effect on coagulation per se; nor are there any obvious side effects manifested during the process of neutralization. The acute toxicity is less than that of other compounds in use: toluidine blue, protamine and hexadimethrine.

Verapamil enhances the anticonvulsant effect of oxcarbazepine in the maximal electroshock-induced seizure model in mice

2009 ◽  
Vol 22 (2) ◽  
pp. 115-124
Author(s):  
Anna Zadrożniak ◽  
MichaŁ K. Trojnar ◽  
Marcin P. Trojnar ◽  
Żaneta Kimber-Trojnar ◽  
Monika Dudra-Jastrzębska ◽  
...  
Keyword(s):  
Anticonvulsant Effect ◽  
Maximal Electroshock ◽  
Seizure Model

Chemosensitizing Activity of Histone Deacetylases Inhibitory Cyclic Hydroxamic Acids for Combination Chemotherapy of Lymphatic Leukemia

2018 ◽  
Vol 18 (4) ◽  
pp. 365-371 ◽  
Author(s):  
Denis V. Mishchenko ◽  
Margarita E. Neganova ◽  
Elena N. Klimanova ◽  
Tatyana E. Sashenkova ◽  
Sergey G. Klochkov ◽  
...  
Keyword(s):  
Lipid Peroxidation ◽  
Acute Toxicity ◽  
Histone Deacetylases ◽  
Hydroxamic Acids ◽  
Water Soluble ◽  
Male Rat ◽  
Hybrid Male ◽  
Cyclic Hydroxamic Acids

Background: Anti-tumor effect of hydroxamic acid derivatives is largely connected with its properties as efficient inhibitors of histone deacetylases, and other metalloenzymes involved in carcinogenesis. Objective: The work was aimed to (i) determine the anti-tumor and chemosensitizing activity of the novel racemic spirocyclic hydroxamic acids using experimental drug sensitive leukemia P388 of mice, and (ii) determine the structure-activity relationships as metal chelating and HDAC inhibitory agents. Method: Outbreed male rat of 200-220 g weights were used in biochemical experiments. In vivo experiments were performed using the BDF1 hybrid male mice of 22-24 g weight. Lipid peroxidation, Fe (II) -chelating activity, HDAC fluorescent activity, anti-tumor and anti-metastatic activity, acute toxicity techniques were used in this study. Results: Chemosensitizing properties of water soluble cyclic hydroxamic acids (CHA) are evaluated using in vitro activities and in vivo methods and found significant results. These compounds possess iron (II) chelating properties, and slightly inhibit lipid peroxidation. CHA prepared from triacetonamine (1a-e) are more effective Fe (II) ions cheaters, as compared to CHA prepared from 1- methylpiperidone (2a-e). The histone deacetylase (HDAC) inhibitory activity, lipophilicity and acute toxicity were influenced by the length amino acids (size) (Glycine < Alanine < Valine < Leucine < Phenylalanine). All compounds bearing spiro-N-methylpiperidine ring (2a-e) are non-toxic up to 1250 mg/kg dose, while compounds bearing spiro-tetramethylpiperidine ring (1a-e) exhibit moderate toxicity which increases with increasing lipophility, but not excite at 400 mg/kg. Conclusion: It was shown that the use of combination of non-toxic doses of cisplatin (cPt) or cyclophosphamide with CHA in most cases result in the appearance of a considerable anti-tumor effect of cytostatics. The highest chemosensitizing activity with respect to leukemia Р388 is demonstrated by the CHA derivatives of Valine 1c or 2c.

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