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Query: UMLS:C0036572 (seizures)
 80,221 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The antidepressant characteristics of three indole alkylamines were investigated and compared with phenelzine and imipramine by utilising specific pharmacological tools like reserpine, amphetamine, tryptamine and tetrabenazine for determining their possible mechanism of action. Amongst the three indole compounds investigated, indole-3-(2-aminopropyl)-acetate (U-14 164E), indole-3(2-aminobutyl)-d-acetate (u-17 312E) and beta-phenethylhydrazine (phenelzine) produced complete antagonism to reserpine induced sedation, hypothermia as well as facilitation of convulsive seizures. Some of these features suggest that MAO inhibition might be a common mechanism of action of these indoles. The potentiation of CNS effects of tryptamine by these compounds is an outstanding feature of MAO inhibitors, while imipramine is ineffective. Qualitative differences between these indoles and imipramine are evident in the tetrabenazine test. The potentiation of amphetamine induced motor excitation and pentobarbitone narcosis has been explained.
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PMID:A study of antidepressant activity of some indole alkylamines. 2 69

The literature dealing with the convulsant effects of the antidepressant drugs of the non-monoamine oxidase inhibitor variety is reviews. It is concluded that most of these drugs do lower the seizure threshold and may precipitate seizures even at normal therapeutic doses. The pathophysiology of antidepressant-induced seizures is discussed, and attention is drawn to biochemical differences in those antideprssants that have the least epileptogenic potential or may even be anticonvulsant. The clinical difficulties regarding administration of antidepressant drugs to epileptic patients are mentioned, and some practical advice is offered.
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PMID:Non-monoamine oxidase inhibitor antidepressants and epilepsy: a review. 35 20

Fourteen 1-[N-acetyl(4-hydroxy-4-phenyl-piperidino)]-3-aryl carbamides were synthesized, characterized and evaluated for their anticonvulsant, analgesic and monoamine oxidase inhibitory properties. All carbamides (100 mg/kg, i.p.) provided 20--60% protection against pentylenetetrazol-induced seizures in mice. The analgesic activity possessed by these carbamides, with the exception of two compounds, was reflected by their ability to provide 17--67% protection against tail pinch response in mice. All carbamides (1 mM) inhibited (5--90%) in vitro activity of rat brain monoamine oxidase. The low toxicity of these carbamides was reflected by their higher approximate LD50 values which ranged from 500 - greater than 1000 mg/kg.
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PMID:Anticonvulsant, analgesic and monoamine oxidase inhibitory properties of newer 4-hydroxy-4-phenylpiperidinocarbamides. 46 59

The present study reports the synthesis and characterization of eight new substituted benzylideneamino guanidines. All compounds inhibited the monoamine oxidase (MAO) activity of rat brain mitochondria in vitro. The I50 values were determined and were found to be in the range of 10(-4) to 10(-5) mol/l. Preincubation, dialysis and kinetic studies carried out with isolated brain mitochondria by conventional Dixon plot revealed reversible and noncompetitive type of MAO inhibition. These compounds were also screened for anticonvulsant and antidepressant activities. In the present series of compounds only one compound -- 1-amino-3-(4-chloromethylbenzylidene-amino)guanidine hydroiodide -- was found to afford 20% protection against pentetrazol-induced seizures in mice. 1-Amino-3-(3,4-dichlorobenzylideneamino)guanidine hydroiodide which produced maximum inhibition of MAO activity, also produced reversal of reserpine-induced sedation and miosis into excitation and mydriasis in mice.
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PMID:Monoamine oxidase inhibition by substituted benzylideneamino guanidines and their CNS activities. 52 4

Seventeen 4-[3-(N-cyclohexylamino)propyl]-1-substituted-3-thiosemicarbazones were synthesized and evaluated for their ability to inhibit rat brain monoamine oxidase (MAO) and pyruvate oxidase in vitro. Anticonvulsant activity exhibited by these thiosemicarbazones (100 mg/kg,i.p.) against pentylenetetrazol-induced seizures ranged from 10-50%.
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PMID:Monoamine oxidase and pyruvate oxidase inhibitory properties of some newer thiosemicarbazones and their anticonvulsant activity. 52 87

The effects of L-DOPA, L-tryptophan, monoamine oxidase inhibitor (MAOI), and MAOI plus L-tryptophan, each for 3 months, have been assessed in 10 severe, adult epileptics with placebo control. There was no overall reduction in seizure frequency, but 2 patients with minor partial seizures improved, 1 with L-DOPA, MAOI, and MAOI plus L-tryptophan, and the other with L-tryptophan and MAOI plus L-tryptophan. We have not been able to demonstrate an increased turnover of cerebral serotonin (5-HT), as measured by cerebrospinal fluid 5-hydroxyindoleacetic acid, after treatment with L-tryptophan for 3 months. This observation casts doubt on the ability of L-tryptophan to alter the long-term metabolism and functional activity of brain 5-HT. The importance of further exploration of manipulation of cerebral monoamines as a possible approach to the treatment of epilepsy is emphasized.
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PMID:Manipulation of cerebral monoamines in the treatment of human epilepsy: a pilot study. 62 66

To investigate pretreatment patient variables that might correlate with dose-response characteristics of electroconvulsive therapy (ECT) and treatment outcomes, 14 patients were assessed on a daily basis, before and during treatment, using self-report affective scales, three simple paper-and-pencil tests of cognitive function,and finger-tapping speed. From these data, dose-response ratios and treatment outcome measures were derived. The dose-response ratio of ECT was found to correlate with age--the younger the patient, the more favorable the ratio. This finding is discussed in terms of the known relationships between brain monoamine oxidase levels and age, and the established relationship between seizure duration and treatment efficacy. The dose-response ratio over the first two electroconvulsive treatments as well as lesser degrees of initial congnitive and greater degrees of initial affective impairment correlated strongly with greater overall affective improvement. Some clinical and research implications of these findings are discussed.
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PMID:The dose-response ratio in electroconvulsive therapy a preliminary study. 68 73

Six 1-[N-acetyl(4-phenylpiperidino)]-3-aryl carbamides were synthesized, characterized and evaluated for their anticonvulsant, monoamine oxidase inhibitory and antihemolytic properties. These compounds (100 mg/kg, i.p.) provided 10--80% protection against pentylenetetrazol-induced seizures in mice. All carbamides (1 mM) inhibited (34--82%) in vitro activity of rat brain monoamine oxidase and provided 18--51% protection against in vitro hypoosmotic hemolysis of human red blood cells at a final concentration of 1 mM. Low toxicity of these carbamides was reflected by their high approximate LD50 values.
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PMID:Anticonvulsant activity and monoamine oxidase inhibitory and antihemolytic properties of some newer 4-phenylpiperidino carbamides. 72 17

Eight 4-aryl-1-(2,3,4-trihydroxy acetophenone)-3-thiosemicarbazones were synthesised and evaluated for their ability to inhibit rat brain monoamine oxidase (MAO). All compounds exhibited concentration dependent inhibition of enzyme. The degree of enzyme inhibition was also evaluated on the basis of their I50 and I50/(S) values. Preincubation of these compounds with the enzyme system for varying lengths of time prior to the addition of substrate in no way altered their degree of inhibition. Kinetic study carried out with 4-(2-methoxyphenyl)-1-(2,3,4-trihydroxyacetophenone)-3-thiosemicarbazone revealed a competitive nature of inhibition. Anticonvulsant activity exhibited by these thiosemicarbazones (100mg/kg, i.p.) against pentylene-tetrazol-induced seizures ranged between 10-60%. Low toxicity possessed by these compounds was reflected by their approximate LD50 values ranging from 750 mg/kg to greater than 1000 mg/kg.
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PMID:Monoamine oxidase inhibitory and anticonvulsant properties of some newer thiosemicarbazones. 73 17

2-(N-Arylcarboxamide)-3-substituted ethoxyindoles were synthesized by the reaction of 2-(N-arylcarboxamide)-3-hydroxyindoles, which were obtained by the cyclization of 2-carbomethoxyphenylglycine-substituted anilides. These 2-(N-arylcarboxamide)-3-substituted ethoxyindoles were evaluated for their in vitro monoamine oxidase inhibitory ability and in vivo monamine oxidase inhibitory property as evidence by reserpine reversal response. Their anticonvulsant activity also was determined against pentylenetetrazol-induced seizures. No definite correlation could be observed between chemical structure and biological activity.
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PMID:Synthesis of 2-(N-arylcarboxamide)-3-substituted ethoxyindoles and their monoamine oxidase inhibitory and anticonvulsant activities. 113 15


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