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HBK-14 and HBK-15, triple 5-HT1A, 5-HT7 and 5-HT3 antagonists with potent antidepressant- and anxiolytic-like properties, increase seizure threshold in various seizure tests in mice.

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Most antidepressants lower seizure threshold, which might be due to the modulation of serotonergic neurotransmission. Here, we investigated the effects of two 5-HT1A, 5-HT7 and 5-HT3 antagonists, i.e., 1-(2-(2-(2,6-dimethylphenoxy)ethoxy)ethyl)-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14)

Strychnine seizure potentiation by azaspirodecanedione anxiolytics in rats.

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Buspirone, gepirone and ipsaperone administered intraperitoneally (40 mg/kg) to naive rats were found to be proconvulsive for strychnine-induced seizures. The dose of strychnine required to induce seizures in 50% of test animals (CD50) was 2.18 mg/kg in naive rats, while CD50s for rats treated with

Convulsions induced by centrally administered NMDA in mice: effects of NMDA antagonists, benzodiazepines, minor tranquilizers and anticonvulsants.

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1. Convulsions were induced reproducibly by intracerebroventricular injection of N-methyl-D-aspartic acid (NMDA) to conscious mice. 2. Competitive (carboxypiperazine-propylphosphonic acid, CPP; 2-amino-7-phosphonoheptanoic acid, AP7) and non-competitive (MK801; phencyclidine, PCP;

Effect of anxiolytic, antidepressant, and antipsychotic drugs on cocaine-induced seizures and mortality.

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Cocaine abuse may lead to overdose (related to seizures and/or status epilepticus) and to diseases (schizophrenia, depression, and anxiety). This work was designed to study the influence of drugs used to treat psychopathologies associated with cocaine abuse on cocaine-induced seizures and mortality

The influence of the benzodiazepine receptor antagonist flumazenil on the anxiolytic-like effects of CGP 37849 and ACPC in rats.

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In this paper we examined the effect of flumazenil (Ro 15-1788, 10 mg/kg), a benzodiazepine receptor antagonist, on the anticonflict activity of DL-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CGP 37849), a competitive N-methyl-D-aspartate (NMDA) receptor antagonist, and

The intrahippocampal administration of the neurosteroid allopregnanolone blocks the audiogenic seizures induced by nicotine.

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Allopregnanolone (AlloP), GABA(A) positive modulator, has efficacy as anticonvulsant. In contrast, nicotine and pregnenolone sulfate (PregS) act as potent convulsants. The present study aims to evaluate whether a promnesic dose of PregS and/or an anxiolytic dose of AlloP administered in the

Anxiolytic and anticonvulsant activity of a synthetic neuroactive steroid Co 3-0593.

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Endogeneously occurring neuroactive steroids, metabolites of progesterone and deoxycorticosterone, have been shown previously to interact with the GABAA receptor with great specificity in vitro and to have anticonvulsant, anxiolytic and sedative activity in vivo. However, these endogenously

Anticonvulsant, anxiolytic and hypnotic effects of aqueous bulb extract of Crinum glaucum A. chev (Amaryllidaceae): role of GABAergic and nitrergic systems.

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Crinum glaucum A. Chev (Amaryllidaceae) (CG) is a bulbous plant widely used in folk medicine in the treatment of cough, asthma and convulsions. This study was carried out to investigate the anticonvulsant, anxiolytic and hypnotic effects of the aqueous bulb extract of C. glaucum and its possible

[Study on the effect of selective serotonin reuptake inhibitor fluoxetine on seizures and inborn behavior of rats with different phenotype of the nervous system].

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Effects of increased levels of selective reuptake inhibitor fluoxetine were studied in Wistar male rats with different individual reactivity of the nervous system. Different behavioral models were used. In rats tolerant to audiogenic stress, drug administration led to a decrease in exploratory

Anxiolytic and sedative properties of BW A78U, a novel anticonvulsant adenine derivative.

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The anticonvulsant BW A78U, tested in a free mouse exploratory situation, reduced in a dose-dependent fashion the locomotion and the number of rearings, this sedative effect being significant up to a dose of 15 mg/kg (IP, 20 min before testing). In an unconditioned conflict test, the light/dark box

(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: II. In vivo characterization.

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(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418), an isoxazole analog of (-)-nicotine, is a potent agonist at the alpha-4/beta-2 subtype of neuronal nicotinic acetylcholine receptor (nAChR) that exists in mammalian brain (Arneric et al., 1994). Compared to (-)-nicotine, ABT 418 has

Design, synthesis and biological evaluation of 7-substituted 4-phenyl-6H-imidazo[1,5-a]thieno[3,2-f] [1,4]diazepines as safe anxiolytic agents

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A series of 4-phenyl-6H-imidazo[1,5-a]thieno[3,2-f][1,4]diazepine-7-carboxylate esters were synthesized and tested as central benzodiazepine receptor (CBR) ligands by the ability to displace [³H]flumazenil from rat cortical membranes. All the compounds showed high affinity with

Central action of ipsapirone, a new anxiolytic drug, on serotoninergic, noradrenergic and dopaminergic functions.

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Ipsapirone (TVX Q 7821, 2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-1,2-benzisothiazol-3- (2H)one-1, 1-dioxidehydrochloride), a new anxiolytic drug in respect of the evaluation of its effect on central 5-hydroxytryptamine (5-HT), noradrenaline and dopamine functions was studied. It was found that

Dietary and botanical anxiolytics.

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Drugs used to treat anxiety have many negative side effects including addiction, depression, suicide, seizures, sexual dysfunction, headaches and more. Anxiolytic medications do not restore normal levels of neurotransmitters but instead manipulate the brain chemistry. For example, selective

Psychogenic non-epileptic seizures in early Huntington's disease.

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Huntington's disease (HD) is a neurodegenerative condition characterised by motor dysfunction with involuntary movements and loss of voluntary control, cognitive deterioration and psychiatric problems. We report a 51-year-old man with early HD who experienced stereotyped episodes of repetitive,

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