thiosemicarbazide and Seizures

thiosemicarbazide has been researched along with Seizures* in 29 studies

Other Studies

29 other study(ies) available for thiosemicarbazide and Seizures

ArticleYear
Anticonvulsant effects of the aqueous and methanol extracts from the stem bark of Psychotria camptopus Verdc. (Rubiacaea) in rats.
    Journal of ethnopharmacology, 2021, May-23, Volume: 272

    The decoction from the stem bark of Psychotria camptopus (Rubiaceae) is used in the Cameroonian pharmacopoeia to treat neurological pathologies including epilepsy.. The present work was undertaken to study the anticonvulsant properties of the aqueous (AE) and methanol (ME) extracts from the stem bark of P. camptopus in acute models of epileptic seizures in Wistar rats.. AE and ME were obtained by decoction and maceration of the stem bark powder in water and methanol, respectively. They were tested orally at the doses of 40, 80 and 120 mg/kg, on the latency of onset and duration of epileptic seizures induced by pentylene tetrazole (PTZ, 70 mg/kg, i.p.). The kinetic effect of both extracts at 120 mg/kg was evaluated. Their effects on diazepam (50 mg/kg) induced sleep and strychnine (STR, 2.5 mg/kg, i.p.) induced seizures were determined. ME was further tested on picrotoxin (PIC, 7.5 mg/kg, i.p.) and thiosemicarbazide (TSC, 50 mg/kg, i.p.) induced seizure models. The phytochemical composition of ME was assessed using LC-MS method, as well as its acute toxicity.. AE and ME significantly (p < 0.001) reduced the duration of seizures in both PTZ and STR models. Their maximal effect was observed at 1 h after administration, though their effect at 120 mg/kg was maintained (p < 0.05) up to 24 h post-treatment. Both extracts significantly (p < 0.01) reduced sleep duration. ME significantly (p < 0.001) increased the latency of rat death on PIC-induced convulsions. In TSC rats, ME significantly (p < 0.001) delayed the latency to the first convulsion, and decreased the duration and frequency of convulsions. ME showed no acute toxicity while its phytochemical screening revealed the presence of two flavonoids (Rutin and Butin), two triterpenoid saponins (Psycotrianoside B and Bauerenone) and four alkaloids (10-Hydroxy-antirhine, 10-hydroxy-iso-deppeaninol, Emetine and Hodkinsine). In conclusion, AE and ME from the stem bark of P. camptopus have comparable anticonvulsant properties. The effect of ME is likely due to the presence of flavonoids and alkaloid and the activation of GABA pathway. These results further justify and support the use of P. camptopus in traditional medicine for the treatment of epilepsy.

    Topics: Animals; Anticonvulsants; Behavior, Animal; Diazepam; Disease Models, Animal; Epilepsy; Methanol; Mice; Pentylenetetrazole; Phytochemicals; Picrotoxin; Plant Bark; Plant Extracts; Plant Stems; Psychotria; Rats, Wistar; Seizures; Semicarbazides; Sleep; Sleep Latency; Strychnine; Water

2021
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.
    Pharmacological reports : PR, 2016, Volume: 68, Issue:2

    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.. 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 100mg/kg, per oral for 14 days.. 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 100mg/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.. 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.

    Topics: 3-Mercaptopropionic Acid; Animals; Anticonvulsants; Antidepressive Agents; Disease Models, Animal; Electroshock; Mice; Pentylenetetrazole; Phenylurea Compounds; Piperazine; Piperazines; Rats; Rats, Wistar; Seizures; Semicarbazides; Status Epilepticus

2016
Preliminary Pharmacological Screening of Some Thiosemicarbazide, s-triazole, and Thiadiazole Derivatives.
    CNS & neurological disorders drug targets, 2016, Volume: 15, Issue:6

    Two thiosemicarbazide derivatives 1 and 2, three 2-amino-1,3,4-thiadiazole derivatives 3-5, and three N1- substituted-4-methyl-1,2,4-triazole-5-thione derivatives 6-8 were synthesized and evaluated for their central nervous system effects using rodent behavioral models. With the exception of 6, all compounds were devoid of neurotoxicity and they did not affect the body temperature of mice. New lead structures 1-4 with potential analgesic activity were identified.

    Topics: Analgesics; Animals; Anxiety; Body Temperature; Central Nervous System Agents; Depression; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Female; Mice; Molecular Structure; Motor Activity; Nociceptive Pain; Seizures; Semicarbazides; Sleep; Thiadiazoles; Triazoles

2016
Synthesis and anticonvulsant activity evaluation of 6-substituted-[1,2,4]triazolo[3,4-a](tetrazolo[5,1-a])phthalazine derivatives.
    Journal of enzyme inhibition and medicinal chemistry, 2013, Volume: 28, Issue:4

    With the aim of finding new anticonvulsant drugs, new 6-substituted-[1,2,4]triazolo[3,4-a] (tetrazolo[5,1-a]) phthalazine derivatives (1-34) have been designed and synthesized. All the compounds were evaluated for their anticonvulsant activities using the maximal electroshock test (MES). Most of the synthesized compounds exhibited potent anticonvulsant activities in the MES. The most promising compound 14 showed significant anticonvulsant activity in MES test with ED₅₀ value of 9.3 mg/kg. It displayed a wide margin of safety with protective index much higher than the standard drug Carbamazepine. And the potency of compound 14 against seizures induced by Pentylenetetrazole, Isoniazid, Thiosemicarbazide and 3-Mercaptopropionic acid in the chemical-induced seizure tests suggested that compound 14 displayed wide spectrum of activity in several models.

    Topics: 3-Mercaptopropionic Acid; Animals; Anticonvulsants; Electroshock; Heterocyclic Compounds, 3-Ring; Isoniazid; Mice; Mice, Inbred Strains; Molecular Structure; Pentylenetetrazole; Phthalazines; Seizures; Semicarbazides

2013
Menthone aryl acid hydrazones: a new class of anticonvulsants.
    Medicinal chemistry (Shariqah (United Arab Emirates)), 2011, Volume: 7, Issue:1

    A series of ten compounds (Compounds J(1)-J(10)) of (±) 3-menthone aryl acid hydrazone was synthesized and characterized by thin layer chromatography and spectral analysis. Synthesized compounds were evaluated for anticonvulsant activity after intraperitoneal (i.p) administration to mice by maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure method and minimal clonic seizure test. Minimal motor impairment was also determined for these compounds. Results obtained showed that four compounds out of ten afforded significant protection in the minimal clonic seizure screen at 6 Hz. Compound J(6), 4-Chloro-N-(2-isopropyl-5-methylcyclohexylidene) benzohydrazide was found to be the most active compound with MES ED(50) of 16.1 mg/kg and protective index (pI) of greater than 20, indicating that (±) 3-menthone aryl acid hydrazone possesses better and safer anticonvulsant properties than other reported menthone derivatives viz. menthone Schiff bases, menthone semicarbazides and thiosemicarbazides.

    Topics: Animals; Anticonvulsants; Dose-Response Relationship, Drug; Electroshock; Hydrazones; Injections, Intraperitoneal; Male; Menthol; Mice; Molecular Structure; Motor Activity; Pentylenetetrazole; Rats; Rats, Sprague-Dawley; Rotarod Performance Test; Seizures; Semicarbazides; Structure-Activity Relationship

2011
Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:7

    Herein, we described the syntheses and anticonvulsant activities of 7-(substituted-phenyl)-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones (1a-1o) and their derivatives. Most of the synthesized compounds exhibited potent anticonvulsant activities in the maximal electroshock test (MES). The most promising compound 1i showed significant anticonvulsant activity in MES test with ED(50) value of 19.7 mg/kg. It displayed a wide margin of safety with protective index much higher than the standard drugs. In addition, the potence of compound 1i against seizures induced by Pentylenetetrazole, Isoniazid, Thiosemicarbazide, 3-Mercaptopropionic acid, and Bicuculline in the chemical-induced seizure tests suggested that compound 1i displayed broad spectrum activity in several models, and it is likely to have several mechanisms of action including inhibiting voltage-gated ion channels and modulating GABAergic activity.

    Topics: 3-Mercaptopropionic Acid; Animals; Anticonvulsants; Bicuculline; Electroshock; Isoniazid; Mice; Pentylenetetrazole; Pyrimidinones; Seizures; Semicarbazides; Structure-Activity Relationship; Triazoles

2011
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
    European journal of medicinal chemistry, 2009, Volume: 44, Issue:9

    A series of novel N-(2-hydroxyethyl) cinnamamide derivatives were synthesized and screened for their anticonvulsant activities by the maximal electroshock (MES) test and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox). The MES test showed that compounds I(N-(2-hydroxyethyl) cinnamamide) and 1d ((E)-3-(3-fluorophenyl)-N-(2-hydroxyethyl)acrylamide) were found to possess better anticonvulsant activity but also had lower toxicity. In the anti-MES potency test, these compounds exhibited median effective dose (ED(50)) of 17.7 and 17.0 mg/kg, respectively, and median toxicity dose (TD(50)) of 154.9 and 211.1, respectively, resulting in a protective index (PI) of 8.8 and 12.4, respectively, which is much greater than the PI of the marked antiepileptic drug carbamazepine. To further investigate the effects of the anticonvulsant activity in several different models, compounds I and 1d were tested against convulsions induced by chemical substances, including pentylenetetrazole (PTZ), isoniazid, 3-mercaptopropionic acid, and thiosemicarbazide.

    Topics: 3-Mercaptopropionic Acid; Animals; Anticonvulsants; Cinnamates; Electroshock; Isoniazid; Mice; Pentylenetetrazole; Seizures; Semicarbazides; Structure-Activity Relationship

2009
[Pharmacological effects of volatile oil of Valeriana amurensis on CNS].
    Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials, 2007, Volume: 30, Issue:8

    To study the pharmacological effects of volatile oil of Valeriana amurensis on central nervous system.. The pharmacological effects of volatile oil of Valeriana amurensis on the autonomic activities of mice, the sleeping synergistic action of mice with pentoharbital sodium at subthreshold and hypnotic dosages, the sleep phases of rats, the writhing response of mice caused by acetic acid and the convulsion of mice induced by thio-semicarbazide were investigated.. The autonomic activities of mice were significantly inhibited by the volatile oil of Valeriana amurensis. The rate of falling sleep and the extension of sleeping time of mice were significantly increased by the synergic action of pentobarbital sodium with the volatile oil. The sleep phases of SWS2 and REMS of rats were obviously extended by the volatile oil of Valeriana amurensis. In addition, the frequency of writhing response of mice caused by acetic acid was reduced, and the convulsion of mice induced by thio-semicarbazide was antagonized with the administration of the volatile oil.. The volatile oil of Valeriana amurensis has significantly sedative analgesic and anti-hyperspasmia effects.

    Topics: Animals; Central Nervous System; Central Nervous System Agents; Drug Synergism; Drugs, Chinese Herbal; Female; Male; Mice; Motor Activity; Oils, Volatile; Pentobarbital; Plant Roots; Rats; Rats, Wistar; Seizures; Semicarbazides; Sleep; Valerian

2007
Analgesic and anticonvulsant effects of extracts from the leaves of Kalanchoe crenata (Andrews) Haworth (Crassulaceae).
    Journal of ethnopharmacology, 2006, Jun-15, Volume: 106, Issue:1

    Kalanchoe crenata Andr. (Crassulaceae) is a fleshy herbaceous plant used in the African traditional medicine as remedies against otitis, headache, inflammations, convulsions and general debility. In the present work, the analgesic effects of methylene chloride/methanol (1:1) (CH(2)Cl(2)/CH(3)OH) extract and its hexane, methylene chloride (CH(2)Cl(2)), ethyl acetate, n-butanol fractions and aqueous residue have been evaluated using acetic acid, formalin and pressure test. The anticonvulsant effects of the CH(2)Cl(2)/CH(3)OH extract were also investigated on seizures induced by pentylenetetrazol (PTZ 70 mg/kg), strychnine sulphate (STN 2.5 mg/kg) and thiosemicarbazide (TSC 50 mg/kg). CH(2)Cl(2)/CH(3)OH extract and its fractions, administered orally at the doses of 150 and 300 mg/kg, exhibited protective effect of at least 30% on the pain induced by acetic acid. The CH(2)Cl(2) fraction at 300 mg/kg showed a maximal effect of 78.49%. The CH(2)Cl(2)/CH(3)OH extract and its CH(2)Cl(2) fraction at the doses of 150 and 300 mg/kg significantly reduced the first phase of pain induced by formalin while the second phase was completely inhibited. The CH(2)Cl(2) fraction produced more than 45% reduction in the sensitivity to pain induced by pressure. The CH(2)Cl(2)/CH(3)OH extract of Kalanchoe crenata significantly increased the latency period in seizures induced by PTZ and significantly reduced the duration of seizures induced by the three convulsant agents. The extract protected 20% of animals against death in seizures induced by TSC and STN. These results suggest a peripheral and central analgesic activities as well as an anticonvulsant effect of the leaves of Kalanchoe crenata.

    Topics: Analgesics; Animals; Anticonvulsants; Convulsants; Female; Kalanchoe; Male; Mice; Pentylenetetrazole; Phytotherapy; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Seizures; Semicarbazides

2006
Effect of bis(acetato)tetrakis(imidazole) copper(II) in delaying the onset and reducing the mortality rate of strychnine- and thiosemicarbazide- induced convulsions.
    Biological trace element research, 2004, Volume: 101, Issue:1

    The anticonvulsant activity of bis(acetato)tetrakis(imidazole) copper(II), Cu(OAc)2(Im)4, was studied in normal mice using chemical convulsions induced by strychnine, thiosemicarbazide, picrotoxin, and pentelenetetrazol. Intraperitoneal administration of Cu(OAc)2(Im)4, 50 mg/kg body mass, has delayed the onset of strychnine (3 mg/kg)-induced convulsion by 204% (p < or = 0.005) and thiosemicarbazide (20 mg/kg)-induced convulsant by 61% (p < or = 0.005). The changes in the onset of picrotoxin- (6 mg/kg) and pentelenetetrazol (50 mg/kg)-induced convulsions were not significant. The same dosage of the copper compound was effective in delaying the lethal time and reducing the mortality rate of treated animals. The anticonvulsant activity of Cu(OAc)2(Im)4 complex against strychnine was not related to its constituents because the inorganic form of copper such as copper chloride, copper acetate, and the parent imidazole has no anticonvulsant activity. Other copper(II) complexes like copper(II)aspirinate and bis(acetato)bis(2-methyl imidazole) copper(II) were less effective.

    Topics: Animals; Anticonvulsants; Female; Mice; Organometallic Compounds; Seizures; Semicarbazides; Strychnine; Time Factors

2004
Expression of anti-neuroexcitation peptide (ANEP) of scorpion Buthus martensii Karsch in Escherichia coli.
    Preparative biochemistry & biotechnology, 2001, Volume: 31, Issue:1

    According to the cDNA sequence of anti-neuroexcitation peptide of scorpion Buthus martensii Karsch, the putative mature anti-neuroexcitation peptide (ANEP) encoding DNA fragment was obtained by a PCR method, then was cloned into expression plasmid pET28a, fused with His tag at its 3' end. When expressed in E. coli BL21 (DE3), the expression of recombinant ANEP was 15% of total cellular proteins, while most recombinant ANEP products existed in the form of insoluble inclusion bodies. Coexpression of molecular chaperones or protein disulfide isomerase could not improve its solubility. The recombinant ANEP in the cell lysate was purified to homogeneity by metal chelating affinity chromatography and Superdex 30 chromatography. In bioassay with convulsive mice model induced by thiosemicarbazide, recombinant ANEP could apparently delay the convulsion seizure of model animals by 18% and showed anti-neuroexcitatory activity.

    Topics: Animals; DNA, Complementary; Escherichia coli; Gene Expression; Male; Mice; Plasmids; Polymerase Chain Reaction; Recombinant Fusion Proteins; RNA; Scorpion Venoms; Scorpions; Seizures; Semicarbazides; Transfection

2001
[Possible role of nitric oxide in pathogenesis of model seizure of the different etiology].
    Biulleten' eksperimental'noi biologii i meditsiny, 1998, Volume: 125, Issue:1

    Topics: Animals; Brain; Convulsants; Electron Spin Resonance Spectroscopy; Electroshock; Excitatory Amino Acid Agonists; gamma-Aminobutyric Acid; Lipid Peroxidation; Male; N-Methylaspartate; Nitric Oxide; Pentylenetetrazole; Rats; Rats, Wistar; Receptors, N-Methyl-D-Aspartate; Seizures; Semicarbazides

1998
[Nitric oxide in the rat cerebral cortex in seizure models: potential ways of pharmacological modulation].
    Rossiiskii fiziologicheskii zhurnal imeni I.M. Sechenova, 1998, Volume: 84, Issue:10

    Seizures induced with Thiosemicarbaside, Pentylenetetrasole, N-methyl-D,L-aspartate were used as models. The NO content increased 4-5-fold in the brain cortex at the peak of seizures. The increase could be prevented by pre-treatment with N-nitro-L-arginine and the seizures were weakened. Anticonvulsant drugs reduced the seizure manifestations and partially prevented the NO generation enhancement. The latter seems to be involved in pathophysiological mechanisms underlying the seizures.

    Topics: Animals; Anticonvulsants; Arginine; Convulsants; Dizocilpine Maleate; Electron Spin Resonance Spectroscopy; Electroshock; Excitatory Amino Acid Agonists; Excitatory Amino Acid Antagonists; Male; N-Methylaspartate; Nitric Oxide; Nitroarginine; Pentylenetetrazole; Rats; Rats, Wistar; Receptors, N-Methyl-D-Aspartate; Seizures; Semicarbazides

1998
The effect of GABAergic system activity on hyperthermia-induced seizures in rats.
    Brain research. Developmental brain research, 1997, Dec-19, Volume: 104, Issue:1-2

    Developing rats were given GABA antagonists and agonist before electrical seizure discharges were induced by heating the brain of a rat with infra-red rays. The thresholds for the GABA antagonist groups were significantly lower than that for the control, and the threshold for the GABA agonist group was significantly higher than that for the control. These results support the hypothesis that reduced GABAergic system activity underlies febrile seizures.

    Topics: Analysis of Variance; Animals; Bicuculline; Body Temperature Regulation; Electroencephalography; Female; GABA Agonists; GABA Antagonists; gamma-Aminobutyric Acid; Hot Temperature; Male; Muscimol; Rats; Rats, Inbred Lew; Seizures; Semicarbazides

1997
[Central inhibition action of Valeriana jatamansii Jones].
    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica, 1994, Volume: 19, Issue:1

    The use of water extract (ip or ig) of Valeriana jatamansii together with pentobarbital sodium can enhance sedative and hypnotic effect in mice, inhibit the spontaneous activity in mice, and antagonize convulsive action induced by thiosemicarbazide (TSZ). Although ineffective on the convulsion induced by picrotoxin (PT), it can prolong the latent period of convulsion induced by PT in mice. The number of writhings in mice can be reduced after ip or ig water extract.

    Topics: Analgesics; Animals; Anticonvulsants; Drug Synergism; Drugs, Chinese Herbal; Female; Hypnotics and Sedatives; Male; Mice; Pentobarbital; Picrotoxin; Seizures; Semicarbazides

1994
[The effect of the new amino acid-containing 1,4-dihydropyridine glutapyrone on penicillin-induced focal epileptic activity and convulsions induced by bicuculline and thiosemicarbazide].
    Biulleten' eksperimental'noi biologii i meditsiny, 1993, Volume: 116, Issue:10

    The experiments on focal penicillin-induced epileptic activity in the brain cortex (Wistar rats) and bicuculline- and thiosemicarbazide-induced seizures (Icr:Icl mice) showed that the glutapyrone possessed a significant antiepileptic activity. As previously shown, that glutapyrone has an influence on 45Ca2+ uptake by rat cortical synaptosomes (evoked by K+ depolarization) as compared with nifedipine and nimodipine, and it was effective in pentylenetetrazol-induced seizures in rats and mice. The mechanism of action of convulsants is associated with the disturbance of different links of GABAergic inhibition. It is suggested that the antiepileptic effects of glutapyrone are realized at least in part by the participation of GABAergic system.

    Topics: Animals; Anticonvulsants; Bicuculline; Convulsants; Dihydropyridines; Disease Models, Animal; Drug Evaluation, Preclinical; Epilepsies, Partial; Glutamates; Male; Mice; Mice, Inbred ICR; Penicillins; Rats; Rats, Wistar; Seizures; Semicarbazides

1993
c-Fos mRNA induction under vitamin B6 antagonist-induced seizure.
    Neuroscience letters, 1989, Apr-10, Volume: 98, Issue:3

    c-Fos mRNA expression was studied in mouse brain after vitamin B6 antagonist-induced seizure. The vitamin B6 antagonists used were hydrazine, thiosemicarbazide, penicillamine and deoxypyridoxine. Only deoxypyridoxine was effective in increasing c-fos mRNA and c-fos protein expression in nerve cells. The other 3 antagonists had levels of c-fos mRNA below or equal to basal level. The seizure activity induced by several vitamin B6 antagonists resulted in different effects on c-fos gene expression.

    Topics: Animals; Blotting, Northern; Brain; Hydrazines; Male; Mice; Mice, Inbred ICR; Penicillamine; Proto-Oncogenes; Pyridoxine; RNA, Messenger; Seizures; Semicarbazides

1989
Effects of carbon dioxide on onsets of seizures in mice induced by antagonists of vitamin B6.
    Biochemical pharmacology, 1987, Jun-15, Volume: 36, Issue:12

    Topics: Animals; Carbon Dioxide; Mice; Penicillamine; Pyridoxine; Seizures; Semicarbazides

1987
GABA-ergic mechanisms in the anticonvulsive activity of newly-synthesized barbiturates. I. Effects of barbiturates on the convulsive action of GABA-antagonists.
    Acta physiologica et pharmacologica Bulgarica, 1987, Volume: 13, Issue:3

    The anticonvulsive activity of seven newly-synthesized derivatives of barbituric acid, having a hydroxylamins groups substituted in second position, with respect to convulsive agents related with the GABA-ergic transmitter system: picrotoxin, bicuculline, thiosemicarbazide and 3-mercaptopropionic acid, was studied in experiments on mice. The anticonvulsive activity of these compounds in allylglycine-induced convulsions was investigated in experiments on rats, and was compared to that of well-known drugs, such as pentobarbital, phenobarbital, allobarbital and diphenylhydantoin. The results obtained show that the hydroxylamine derivatives of barbituric acid HB-2 (2-hydroxylamino-5-ethyl-5-propylbarbituric acid) and HB-7 (2-hydroxylamino-5-ethyl-5 sec. pentylbarbituric acid) have the most pronounced anticonvulsive activity, which suggests the considerable importance of the participation of GABA-ergic transmission in the realization of this activity.

    Topics: 3-Mercaptopropionic Acid; Allylglycine; Animals; Anticonvulsants; Barbiturates; Bicuculline; GABA Antagonists; gamma-Aminobutyric Acid; Male; Mice; Picrotoxin; Rats; Seizures; Semicarbazides

1987
[Anticonvulsant action of di-N-propylacetate combined with benzodiazepines, phenobarbital and phenytoin].
    Biulleten' eksperimental'noi biologii i meditsiny, 1981, Volume: 91, Issue:4

    The combined use of di-n-propylacetate with phenazepam, diazepam, phenobarbital or phenytoin was shown to be followed by reciprocal potentiation of the anticonvulsant activity of the drugs in a variety of experimental epileptic seizures in mice according to the tests of shock and antagonism with corasole and thiosemicarbazide. The potentiating effect of the subthreshold dose of di-n-propylacetate on anticonvulsant effects of benzodiazepines, phenobarbital and phenytoin was more pronounced than the effect of the drugs administered in the subthreshold doses on the anticonvulsant activity of di-n-propylacetate. Of both combinations, di-n-propylacetate plus benzodiazepines proved to be most efficacious one. The unidirectional effect of the combined drugs on the different stages of the development of GABA-ergic system inhibitory function in the CNS activity is assumed to be of importance in the mechanism of reciprocal potentiation.

    Topics: Animals; Anti-Anxiety Agents; Anticonvulsants; Benzodiazepines; Benzodiazepinones; Diazepam; Drug Therapy, Combination; Male; Mice; Pentylenetetrazole; Phenobarbital; Phenytoin; Seizures; Semicarbazides; Valproic Acid

1981
Anticonvulsant effects of caerulein, cholecystokinin octapeptide (CCK-8) and diazepam against seizures produced in mice by harman, thiosemicarbazide and isoniazid.
    Neuroscience letters, 1981, Jul-02, Volume: 24, Issue:2

    Caerulein, cholecystokinin octapeptide (CCK-8) and diazepam delayed the onset of seizures produced by harman and thiosemicarbazide (TSC). Caerulein had the potency of diazepam, whereas CCK-8 was less active by a factor of four. The convulsions induced by isoniazid (INH) were very resistant to both caerulein and diazepam; CCK-8 was not tested against isoniazid. Haloperidol did not influence the effect of TSC; it enhanced isoniazid-induced seizures, and antagonized the convulsant effect of harman.

    Topics: Animals; Anticonvulsants; Ceruletide; Cholecystokinin; Diazepam; Haloperidol; Harmine; Isoniazid; Male; Mice; Mice, Inbred Strains; Seizures; Semicarbazides; Sincalide

1981
[Convulsive syndrome activation in mice after administration of ADPT vaccine].
    Zhurnal mikrobiologii, epidemiologii i immunobiologii, 1980, Issue:1

    The experimental model of chemical convulsions allowed to establish the fact that the death of mice immunized with adsorbed DPT vaccine was accelerated, in comparison with the control group, as a result of convulsive fits caused by the injection of thiosemicarbazide. Immunization with adsorbed DPT vaccine was also found to induce a qualitative change in convulsive fits. The fact that an increase in convulsive activity occurs in the animals immunized with absorbed DPT vaccine may be related to the appearance of some forms of convulsive states in children during the postvaccination period.

    Topics: Animals; Child; Diphtheria Toxoid; Humans; Mice; Pertussis Vaccine; Seizures; Semicarbazides; Syndrome; Tetanus Toxoid; Vaccination

1980
Effect of antivitamin B6 on regional GABA metabolism in mouse brain and its relation to convulsions.
    Journal of nutritional science and vitaminology, 1979, Volume: 25, Issue:6

    The effects of administration of DL-penicillamine (PeA), thiosemicarbazide (TSC), semicarbazide-HCl (SC) as convulsants and pyridoxine (PN) as anticonvulsant on gamma-aminobutyric acid (GABA) content, glutamic acid decarboxylase (GAD) and gamma-aminobutyric acid transaminase (GABA-T) activities in cerebral cortex, striatum, diencephalon, mesencephalon, cerebellum and pons/medulla were investigated. The onset of convulsions induced by these convulsants coincides with the fall in GABA content and GAD activity in the mesencephalon area, and in contrast, the cessation of the convulsions by PN supplement coincides with the recovery in both the parameters. Aminooxyacetic acid (AOAA), a potent GABA-elevating agent showed an anticonvulsant property against convulsion by TSC for several hours after the injection of AOAA, but lost this property 16 hr after the treatment. The TSC administration 16 hr after the AOAA pretreatment significantly decreased the GABA content in all the regions, particularly in the mesencephalon and diencephalon areas, which had been elevated by the AOAA pretreatment, together with its ability to induce convulsion. FRom the above results it may be postulated that the critical drop of GABA level from a plateau to another lower level following the decrease of GAD activity in the mesencephalon area is an important factor in the induction of convulsion.

    Topics: 4-Aminobutyrate Transaminase; Aminooxyacetic Acid; Animals; Brain; gamma-Aminobutyric Acid; Glutamate Decarboxylase; Male; Mice; Penicillamine; Pyridoxine; Seizures; Semicarbazides

1979
Anticonvulsant activity of aminooxyacetic acid on convulsions induced by thiosemicarbazide.
    Journal of neurochemistry, 1976, Volume: 26, Issue:3

    Topics: Acetates; Aminobutyrates; Aminooxyacetic Acid; Animals; Anticonvulsants; Brain; gamma-Aminobutyric Acid; Male; Mice; Seizures; Semicarbazides

1976
A NEUROCHEMICAL STUDY OF THIOSEMICARBAZIDE SEIZURES AND THEIR INHIBITION BY AMINO-OXYACETIC ACID.
    Biochemical pharmacology, 1964, Volume: 13

    Topics: Acetates; Alanine; Amino Acids; Aminobutyrates; Ammonia; Animals; Aspartic Acid; Azides; Brain; Dogs; Electrophysiology; Glutamine; Lactates; Lysine; Nerve Tissue Proteins; Neurochemistry; Pentylenetetrazole; Pharmacology; Research; Seizures; Semicarbazides; Thiosemicarbazones; Toxicology; Tyrosine

1964
Demonstration of thiosemicarbazide-induced convulsions in rats with elevated brain levels of gamma-aminobutyric acid.
    Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.), 1960, Volume: 104

    Topics: Amino Acids; Animals; Brain; gamma-Aminobutyric Acid; Hydrazines; Neurochemistry; Rats; Seizures; Semicarbazides; Thiourea

1960
Convulsant hydrazides. II. Comparison of electrical changes and enzyme inhibition induced by the administration of thiosemicarbazide.
    The Journal of pharmacology and experimental therapeutics, 1957, Volume: 119, Issue:2

    Topics: Anti-Bacterial Agents; Convulsants; Lyases; Seizures; Semicarbazides; Thiosemicarbazones

1957
[Influence of pyridoxine and pyridoxal-5-phosphate on thiosemicarbazide cramps in rats].
    Naunyn-Schmiedebergs Archiv fur experimentelle Pathologie und Pharmakologie, 1957, Volume: 230, Issue:5

    Topics: Animals; Coenzymes; Muscle Cramp; Phosphates; Pyridoxal Phosphate; Pyridoxine; Rats; Seizures; Semicarbazides; Thiosemicarbazones; Vitamin B 6

1957
Pentylenetetrazole and thiosemicarbazide: a study of convulsant activity in the isolated cerebral cortex preparation.
    The Journal of pharmacology and experimental therapeutics, 1955, Volume: 115, Issue:1

    Topics: Cerebral Cortex; Convulsants; Hydrazines; Pentylenetetrazole; Seizures; Semicarbazides

1955