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indole/crise épileptique
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[Verification, on man, of the protective power of the neutral fumarate of 2-(N-methyl-2-piperidyl)-3-indole hydrate or RP 7065 against convulsions induced by partially elevated oxygen pressure and research on a predisposing sign of the imminence of the crisis].
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Identifying cytochrome P450s involved in oxidative metabolism of synthetic cannabinoid N-(adamantan-1-yl)-1-(5-fluoropentyl)-1H-indole-3-carboxamide (STS-135).
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Synthetic cannabinoids (SCBs), designer drugs marketed as legal alternatives to marijuana, act as ligands to cannabinoid receptors; however, they have increased binding affinity and potency, resulting in toxicity symptoms such as cardiovascular incidents, seizures, and potentially death.
Enzymatic analysis of glucuronidation of synthetic cannabinoid 1-naphthyl 1-(4-fluorobenzyl)-1H-indole-3-carboxylate (FDU-PB-22).
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Recently, there has been a rise in abuse of synthetic cannabinoids (SCBs). The consumption of SCBs results in various effects and can induce toxic reactions, including paranoia, seizures, tachycardia and even death. 1-Naphthyl 1-(4-fluorobenzyl)-1H-indole-3-carboxylate (FDU-PB-22) is a third
[Anti-convulsion effects of choto-san and chotoko (Uncariae Uncis cam Ramlus) in mice, and identification of the active principles].
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The crude drug, Chotoko (Uncariae Uncis cam Ramlus), the hooks of Uncaria spp. (Rubiaceae), has been claimed to possess sedative and anti-spasmodic actions, and is contained in a Chinese traditional preparation, Choto-san, as a main crude drug. Examinations were made on the anti-convulsion effects
Picolinic acid and indole-2-carboxylic acid: two types of glycinergic compounds modulate motor function differentially.
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1. A putative agonist for the strychnine-sensitive glycine receptor picolinic acid was tested for its anticonvulsant activities in mice and muscle-relaxant activities in rats and compared with indole-2-carboxylic acid (I2CA), an antagonist for the strychnine-insensitive glycine receptor. Their
Tricyclic indole-2-carboxylic acids: highly in vivo active and selective antagonists for the glycine binding site of the NMDA receptor.
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A series of tricyclic indole-2-carboxylic acid derivatives were synthesized and evaluated by the radioligand binding assay and the anticonvulsant effects in the mouse NMDA-induced seizure model. Among them, derivatives of 3S-(-)-4 such as 3a, 3f, and 3g which had certain zwitterionic anilides showed
A study of antidepressant activity of some indole alkylamines.
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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
Anticonvulsant evaluation of clubbed indole-1,2,4-triazine derivatives: a synthetic approach.
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A series of thirty indole C-3 substituted 5-amino-6-(5-substituted-2-phenyl-1H-indol-1-yl)-4,5-dihydro-1,2,4-triazine-3(2H)-thione 5a-f, 6a-f, 7a-f, 8a-f and 9a-f were synthesized to explore prospective anticonvulsant agents. The derivative
Evaluation of the anticonvulsant effect of novel melatonin derivatives in the intravenous pentylenetetrazol seizure test in mice.
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The design of new pharmacologically active compounds with affinity to melatonin receptors has become an area of great interest during the last decade. Recently, we reported that newly synthesized melatonin derivatives, containing aroylhydrazone moiety in the indole scaffold, with the highest
Evaluation of Anti-Epileptic Effect of New Indole Derivatives by Estimation of Biogenic Amines Concentrations in Rat Brain.
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The new heterocyclic compounds are used to treat epilepsy. In the present work new indole derivatives i.e. 5-[2(3)-di alkyl amino alkoxy] Indole 2,3-di-one derivatives are synthesized and characterized and these compounds was subjected to acute toxicity and then screened for antiepileptic activity
Intoxications of the new psychoactive substance 5-(2-aminopropyl)indole (5-IT): a case series from the Swedish STRIDA project.
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BACKGROUND
5-(2-aminopropyl)indole (5-IT) is a new psychoactive substance (NPS; "legal high" or "research chemical") structurally related to indoleamines and substituted phenethylamines and implicated in several fatalities. We describe the clinical characteristics and results of laboratory
Role of glutamate and dopamine receptors in the psychopharmacological profile of the indole alkaloid psychollatine.
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Psychollatine (1), a new glycoside indole monoterpene alkaloid isolated from Psychotria umbellata, has shown an interesting psychopharmacological profile. This study aimed to investigate the role of NMDA glutamate and dopamine receptors in mediating the properties of 1. Psychollatine (1) was
Cycloalkyl indole-2-carboxylates as useful tools for mapping the "north-eastern" region of the glycine binding site associated with the NMDA receptor.
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A novel series of indole-2-carboxylate analogues of GV 150526 (1) in which the terminal phenyl ring belonging to the side chain present in the position C-3 has been replaced with a bridged cycloalkyl group was synthesized and evaluated for its pharmacological profile. Modelling studies on this class
Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.
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A series of indole-2-carboxylates bearing suitable chains at the C-3 position of the indole nucleus was synthesized and evaluated in terms of in vitro affinity using [3H]glycine binding assay and in vivo potency by inhibition of convulsions induced by N-methyl-D-aspartate (NMDA) in mice.
Anxiolytic effect of indole-3-pyruvic acid (IPA) in mice.
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In an elevated plus-maze indole-3-pyruvic acid (IPA, 100-200 mg/kg), an endogenous metabolite of tryptophan, possesses in mice an activity typical of anxiolytics. IPA increased the ratio of the number of entries into open arms over the total number of entries into open and closed arms and the time
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