Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0036572 (seizures)
 80,221 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Changes in the hippocampal theta rhythm were used as a model in which anticonvulsant drugs may be screened for their potential to antagonize soman-induced (1xLD(50)) seizures. The zinc chelator, ethylenediaminetetra acetic acid (EDTA) (300mg/kg), and the NMDA receptor antagonist, HA-966 (60mg/kg), both disrupted the theta rhythm, but did not antagonize soman-induced seizures, neither separately, nor in combination. The anticholinergic and antiglutamatergic procyclidine (6mg/kg) did not influence the theta activity. The GABAergic agonists, diazepam (10mg/kg) and pentobarbital (30mg/kg), both reduced the theta frequency. Procyclidine, diazepam, and pentobarbital did not stop soman-induced seizures when administered separately, but both convulsions and seizure activity terminated when these agents were given together, and the rats slept through the critical convulsion period. This triple therapy was 100% effective, when administered 30-40min following onset of convulsions, and the rats displayed apparently normal behavior the next day. A screening model of potential anticonvulsants cannot be based on alterations in hippocampal EEG activity. Procyclidine, diazepam, and pentobarbital in combination disrupted the theta rhythm like the combination of EDTA and HA-966, but the latter combination did not have anticonvulsant effect. It is concluded that a triple regimen consisting of procyclidine, diazepam, and pentobarbital can effectively terminate soman-induced seizures that have lasted 30min or more.
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PMID:Pharmacological agents, hippocampal EEG, and anticonvulsant effects on soman-induced seizures in rats. 1278 1

A simple and rapid method for the analysis of heroin seizures by micellar electrokinetic chromatography with short-end injection is described. Separations were performed using an uncoated fused silica capillary, 50 cm x 50 microm I.D. x 360 microm O.D. with an effective separation length of 8 cm. The system was run at 25 degrees C with an applied negative voltage of -25 kilovolts. Injection of each sample was for 2 s at -50 mbar. UV detection was employed with the wavelength set at 210 nm. The background electrolyte consisted of 85:15 (water:acetonitrile, v/v) containing final concentrations of 25 mM SDS and 15 mM sodium borate, pH 9.5. Samples and standards were prepared in 0.1% v/v acetic acid and diluted in the run buffer containing 1 mg/ml of N,N-dimethyl-5-methoxytryptamine as an internal standard. Under these conditions a text mixture containing caffeine, paracetamol, morphine, codeine, heroin, and acetylcodeine was resolved within 1.5 min. The method was used to determine the concentration of heroin in heroin seizure samples, and the results were in good agreement with those obtained by a validated gas chromatographic method.
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PMID:The rapid analysis of heroin drug seizures using micellar electrokinetic chromatography with short-end injection. 1583 Sep 95

The intrahippocampal perfusion of 4-aminopyridine (4-AP) in the rat produces immediate seizures and delayed neuronal death, due to the overactivation of N-methyl-D-aspartate (NMDA) receptors by endogenous glutamate released from nerve endings. With the same time course, 4-AP also induces the expression of the cell stress marker heat shock protein 70 (HSP70) in the contralateral non-damaged hippocampus. We have used this experimental model to study the mechanisms of the delayed neuronal stress and death. The NMDA receptor antagonist (+)-5-methyl-10,11-dihydro-5H-dibenzo(a,d)cyclohepten-5,10-imine maleate (MK-801), administered intraperitoneally 30 or 60 but not 120 min after 4-AP perfusion, when animals show intense electroencephalography epileptiform activity, prevented the delayed neurodegeneration whereas the seizures continued for about 3 h as in the control animals. With an identical time window, MK-801 treatment also modified the pattern of HSP70 expression; the protein was expressed in the protected perfused hippocampus but no longer in the undamaged contralateral hippocampus. The possible role of Ca2+ in the delayed cell death and HSP70 expression was also studied by coperfusing the intracellular Ca2+ chelator 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetra-acetic acid tetrakis(acetoxymethyl ester) with 4-AP. This treatment resulted in protective and HSP70 effects very similar to those of MK-801. These results suggest that the seizures are not linked to neurodegeneration and that NMDA receptors need to be continuously overactivated by endogenous glutamate for at least 60 min in order to induce delayed neuronal stress and death, which are dependent on Ca2+ entry through the NMDA receptor channel.
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PMID:Late N-methyl-D-aspartate receptor blockade rescues hippocampal neurons from excitotoxic stress and death after 4-aminopyridine-induced epilepsy. 1636 73

We examined antiepileptogenic and anticonvulsant effects of [2,3-dioxo-7-(1H-imidazol-1-yl)-6-nitro-1,2,3,4-tetrahydro-1-quinoxalinyl]-acetic acid monohydrate (YM872), a potent and highly water-soluble alpha-amino-3-hydroxy-5-methyl-isoxazole-4-propionic acid (AMPA) receptor antagonist, in the rat amygdala kindling model of epilepsy. Administration of YM872 significantly suppressed fully kindled seizures. Daily pretreatment with YM872 markedly retarded development of kindling during drug sessions. We also used the rekindling method to investigate the antiepileptogenic effect of YM872 in an attempt to differentiate between true and false effects in the conventional method of daily administration. The results using the rekindling method suggested that the effect of YM872 was truly antiepileptogenic, indicating its possible clinical usefulness as an antiepileptogenic drug. We also affirmed the importance of AMPA receptors in the seizure expression mechanism and development of kindling-induced epileptogenesis.
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PMID:Effect of YM872, a selective and highly water-soluble AMPA receptor antagonist, in the rat kindling and rekindling model of epilepsy. 1640 98

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.
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PMID:Analgesic and anticonvulsant effects of extracts from the leaves of Kalanchoe crenata (Andrews) Haworth (Crassulaceae). 1642 79

Previous studies on the anticonvulsant activity of N-Cbz-alpha-aminoglutarimides have shown that the derivatives of N-Cbz-alpha-amino-N-alkoxy glutarimide have significant anticonvulsant activity. In addition, their anticonvulsant activities are dependent on the presence of N-alkoxy groups. Based on these results, a series of N-Cbz-alpha-amino-glutarimidooxy carboxylates derivatives (3a-e) were synthesized in moderate yield using a known synthetic procedure. Their anticonvulsant activities were evaluated using the maximal electroshock seizure (MES) test, the pentylene tetrazole induced seizure (PTZ) test, and the strychinine (Str) threshold test with the ultimate aim of developing more active anticonvulsants. None of the compounds (3a-e) tested showed anticonvulsant activity in the MES and PTZ test. However, all the compounds tested exhibited significant anticonvulsant activity in the Str. test. The most active compound in the Str. test was the methyl ester of N-Cbz-alpha-amino-glutarimidooxy acetic acid 3a (ED50 = 42.9 mg/kg).
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PMID:Synthesis and anticonvulsant activities of N-Cbz-alpha-aminoglutarimidooxy carboxylate derivatives. 1683 11

The sedative, anticonvulsant and analgesic activity of ursolic acid, a terpenoid bioassay-isolated from Nepeta sibthorpii Bentham, was evaluated in mice. The oral administration of ursolic acid (2.3 mg/kg) produced a significant depressant effect on CNS by reducing spontaneous motor activity and the number and lethality of pentylenetetrazol (PTZ)-induced seizures. Two models of nociception, the writhing test and the hot plate test, were also used to examine the analgesic effect of ursolic acid. At a dose of 2.3 mg/kg, ursolic acid caused an inhibition of acetic acid-induced abdominal constriction, but was inactive in the hot plate test. Treatment at a higher dose (20 mg/kg) significantly increased the reaction time in the hot plate test. This effect, reversed by naloxone, evidently involves opioid receptors, but the analgesic activity of ursolic acid may be related also to the antiinflammatory and antioxidant properties of this compound.
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PMID:Ursolic acid plays a role in Nepeta sibthorpii Bentham CNS depressing effects. 1723 71

Renovascular disease accounts for 8-10% of all cases of paediatric hypertension, whereas, in adults, its incidence is approximately 1%. The Turkish Paediatric Hypertension Group aimed to create the first registry database for childhood renovascular hypertension in Turkey. Twenty of the 28 paediatric nephrology centres in Turkey responded to the survey and reported 45 patients (27 girls, 18 boys) with renovascular hypertension between 1990 and 2005. The age at presentation ranged from 20 days to 17 years. The mean blood pressure at the diagnosis was 169/110 mmHg. Chief complaints of symptomatic patients were headache (38%), seizure (18%), epistaxis (4%), growth retardation (4%), cognitive dysfunction (4%), polyuria (2%), palpitation (2%), and hemiplegia (2%). Renovascular hypertension was found incidentally in 11 children. The diagnosis of renovascular hypertension was established with conventional angiography in 39 patients, MR angiography in three, CT angiography in two, and captopril diethylene triamine penta-acetic acid (DTPA) scintigraphy in one patient. Twenty-one children had bilateral renal artery stenosis and 24 had unilateral renal artery stenosis. Of these, 14 (31%) had fibromuscular dysplasia; 12 (27%) Takayasu's arteritis; six (13%) neurofibromatosis; two (5%) Williams syndrome; one (2%) Kawasaki disease; one (2%) mid-aortic syndrome; one (2%) extrinsic compression to the renal artery, and eight (18%) unspecified bilateral renal artery stenosis. Hypertension was controlled with antihypertensive drugs in 17 patients. Percutaneous transluminal angioplasty (PTRA) or surgery had to be performed in 28 patients: PTRA in 16 patients, PTRA + surgery in one patient and surgery in 11 patients (four nephrectomies). The importance of vasculitic disease, especially Takayasu's arteritis, should not be underestimated in children with renovascular hypertension.
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PMID:Reno-vascular hypertension in childhood: a nationwide survey. 1753 66

In continuation of the search of new anticonvulsants, a series of N-4-arylpiperazin-1-yl 2-aza-1,3-dioxospiro[4.4]non-2-yl- (5-8) and [4.5]dec-2-yl- (9-15) propionamides, structurally related to the previously described N-4-arylpiperazin-1-yl amides of 2-aza-1,3-dioxospiro[4.5]dec-2-yl-acetic acid, were synthesized. The designed compounds 5-15 were prepared by condensation of the formerly obtained (2-aza-1,3-dioxospiro[4.5]dec-2-yl)- (3) and (2-aza-1,3-dioxo[4.4]non-2-yl)-(4) propionic acids with the appropriately substituted 4-arylpiperazines, in the presence of the N,N-carbonyldiimidazole (CDIM) reagent. All the compounds were tested for their anticonvulsant activity in the maximum electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure threshold tests. Several compounds 7-10, 13 and 14 revealed protection in the MES screening.
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PMID:Synthesis, physicochemical and anticonvulsant properties of new N-4-arylpiperazin-1-yl amides of (2-aza-1,3-dioxospiro[4.4]non-2-yl)- and [4.5]dec-2-yl)-propionic acid. 1762 31

Cestrum nocturnum is a garden shrub from the family Solanaceae and is used as a remedy for different health disorders. The aim of the present work was to investigate the potential neuropharmacological action profile of decoctions obtained from dry leaves of the plant. Decoctions were tested in different neuropharmacological models-Irwin test, exploratory behavior, tests for analgesia, isoniazid- and picrotoxin-induced convulsions, and maximal electroshock seizures-in mice, as well as in amphetamine-induced stereotypies and penicillin epileptic foci in rats. Decoctions of 1 and 5% (D1 and D5) induced restlessness, and the 30% decoction (D30) induced passivity. D5 and D30 reduced significantly exploratory behavior and amphetamine-induced stereotypies within a 3-hour observation period. The latter effect was apparent during the second 60 minutes. Decoctions reduced the amount of writhes induced by acetic acid in a dose-dependent manner, but were not effective in the hot plate model. The decoctions were not effective against pharmacologically induced convulsions. However, repeated administration of five doses of D5, at 1-hour intervals, reduced the amplitude of penicillin-induced epileptic spikes in both primary and secondary foci, in curarized rats. Taken together, the results suggest that C. nocturnum possesses active substances with analgesic activity provided through a peripheral action mechanism, in parallel with some psychoactive activity that does not fit well the neuropharmacological action profile of known reference neurotropic drugs.
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PMID:Behavioral and antiepileptic effects of acute administration of the extract of the plant Cestrum nocturnum Lin (lady of the night). 1827 93


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