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Psychomotor Seizure Screening and in vitro Neuroprotection Assay of Hydrazones Derived from 2-Acetyl Thiophene.

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BACKGROUND Hydrazone core is a versatile structural linker for the development of various classes of antiepileptic agents. The aim of this study was to investigate the anticonvulsant activity of thiophene based hydrazones according to the antiepileptic drug development program protocol. METHODS The

Thiophene, a sulfur-containing heterocyclic hydrocarbon, causes widespread neuronal degeneration in rats.

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Thiophene is a sulfur-containing heterocyclic hydrocarbon that has been detected in a number of environmental sources as various derivatives. Previous studies with rats have shown that thiophene induces selective degeneration of granule cells in the cerebellum, as observed with methyl mercury. To

Convulsive effects of thiophene, a heterocyclic hydrocarbon: behavioral, electrographic and c-Fos immunocytochemical studies.

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The behavioral, electrographic and histopathological changes induced by the heterocyclic hydrocarbon thiophene were investigated in rats following intramuscular injection of 0.3 mL thiophene for 5 days. Generalized convulsions were noted in 29 out of 34 animals (85%) between 1 and 28 h after the

Kappa opioid receptor agonists suppress absence seizures in WAG/Rij rats.

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Involvement of the kappa opioid receptor in the regulation of epileptic activity was studied in WAG/Rij rats, a genetic model of absence epilepsy. I.c.v. administration of the kappa agonists U50,488H (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide), U69,593 (5 alpha,

Effects of carbamazepine, AF-CX 921, and AF-CX 1325 on epileptic discharges and seizures in hippocampally kindled rats.

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In nine hippocampally kindled rats (5 normal and 4 microcephalic) a comparative study of the antiepileptic effects of carbamazepine, and AF-CX 921 [(E)-2-[(alpha-amino)-phenylmethylene]-benzo-[b]-thiophene-3(2H)- one] and its metabolite AF-CX 1325

A new class of anticonvulsants possessing 6 Hz activity: 3,4-dialkyloxy thiophene bishydrazones.

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Thirty nine new 3,4-di(substituted)oxy-N(2),N(5)-bis(substituted)thiophene-2,5-dicarbohydrazides were synthesized starting from ethyl thiodiglycolate through multi-step reactions. In the synthetic sequence, 3,4-dihydroxythiophene-2,5-diester (1) was obtained by condensing the ethyl thiodiglycolate

Synthesis, in-vitro cholinesterase inhibition, in-vivo anticonvulsant activity and in-silico exploration of N-(4-methylpyridin-2-yl)thiophene-2-carboxamide analogs.

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In our current research, a diverse effect of acetylcholinesterase inhibitors was studied on BALB-C mice by using pentylenetetrazole (PTZ) seizure model. A series of carboxamide analogs (4a-4i) have been synthesized via Suzuki coupling reaction in moderate to good yields (35-84%). To study the

Benzothiophene carboxamide derivatives as novel antimalarials.

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Bromo-benzothiophene carboxamide derivatives have been shown in the preceding article to inhibit Plasmodium falciparum Enoyl-ACP reductase. Here, we report bromo-benzothiophene carboxamide derivatives as potent inhibitors of Plasmodium asexual blood-stages in vitro as well as in vivo in the mouse

Studies on cerebral protective agents. X. Synthesis and evaluation of anticonvulsant activities for novel 4,5,6,7-tetrahydrothieno[3,3-c]pyridines and related compounds.

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Novel 4,5,6,7-tetrahydrothieno[3,2-c]pyridines, 1-thienyl-1,2,3,4-tetrahydroisoquinolines and related compounds, in which the benzene rings of (+)-1 (FR115427) were replaced with heteroaromatic rings such as thiophene, furan, benzothiophene and indole, were synthesized and evaluated for

Functional Chemical Groups that May Likely Become a Source for the Synthesis of Novel Central Nervous System (CNS) Acting Drugs.

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BACKGROUND Central Nervous System (CNS) disorders are on increase perhaps due to genetic, enviromental, social and dietetic factors. Unfortunately, a large number of CNS drugs have adverse effects such as addiction, tolerance, psychological and physical dependence. In view of this, literature search

Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.

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A series of substituted 9,10-dihydroxyhexahydrobenzo[f]thieno[c]quinolines (TB[f]Q), varying with respect to the position of the thiophene relative to the benzo[f]quinoline core and the nature and position of the substituent on the thiophene, were prepared and evaluated for their affinity and

Identification of tiagabine degradation products using liquid chromatography with electrospray ionization multistage mass spectrometry and ultra-performance liquid chromatography/high-resolution mass spectrometry.

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BACKGROUND Tiagabine hydrochloride monohydrate drug substance (TGB) is an antiepileptic agent effective in the treatment of seizure disorders. The stability of TGB was studied and its degradation products were identified for the first time. METHODS TGB was heated in the presence of H(2)O(2).

SYNTHESIS OF 1,3,4-OXADIAZOLES AS SELECTIVE T-TYPE CALCIUM CHANNEL INHIBITORS

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Neuropathic pain, epilepsy, insomnia, and tremor disorder may arrive from an increase of intracellular Ca²⁺ concentration through a dysfunction of T-type Ca²⁺ channels. Thus, T-type calcium channels could be a target in drug discovery for the treatments of neuropathic pain and

New phenethylamines in Europe.

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Sixteen phenethylamines are now included in Schedules I and II of the United Nations 1971 Convention on Psychotropic Substances. Most of the ring-substituted compounds are in Schedule I, whereas 2C-B, amphetamine, and methamphetamine are listed in Schedule II. Substances in Schedule IV (e.g.

Synthesis, Anticonvulsant and Antinociceptive Activity of New Hybrid Compounds: Derivatives of 3-(3-Methylthiophen-2-yl)-pyrrolidine-2,5-dione

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The present study aimed to design and synthesize a new series of hybrid compounds with pyrrolidine-2,5-dione and thiophene rings in the structure as potential anticonvulsant and antinociceptive agents. For this purpose, we obtained a series of new compounds and evaluated their anticonvulsant

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