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Strana 1 od 16 výsledky
The sigma receptor ligand 1,3-di(2-tolyl)guanidine is anticonvulsant in the rat prepiriform cortex.
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Unilateral focal injection of 1,3-di(2-tolyl)guanidine (DTG) caused a dose-dependent and potent (ED50 = 5.25 nmol, 95% confidence limits 1.1 to 25.0 nmol) suppression of generalized motor seizures induced by (-)-bicuculline methiodide in the rat prepiriform cortex. These findings indicate that DTG
Monoamine oxidase inhibition by substituted benzylideneamino guanidines and their CNS activities.
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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)
Diagnosis and treatment of botulism in lions.
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Six circus lions (Panthera leo) showed neurological and gastrointestinal signs after consuming casualty broiler chickens. Signs included ataxia, hindlimb paralysis and recumbency. Neurological examination of two affected males showed paralysis of extraocular muscles, fixed dilated pupils and
2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives: novel, potent and selective sigma1 receptor ligands.
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A series of original 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were evaluated for their affinity at sigma1 and sigma2 receptor subtypes in competition binding experiments, using [3H](+)-pentazocine or [3H]1,3-di-o-tolyl-guanidine (DTG) in the presence of 100 nM
[Ictal syncopes. Cardiac sympathetic innervation disorder as the etiology?].
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We report 3 cases of an ictal sinus arrest. All patients suffered from temporal lobe epilepsy (TLE). Seizures were monitored with simultaneous video-eeg during preoperative epilepsy diagnosis. One patient with cortical dysplasia, who frequently suffered from long lasting syncopes, had a nearly
Safety evaluation of cimetidine: 54 month interim report on long-term study in dogs.
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Cimetidine [N"-cyano-N-methyl-N'-2[(5-methylimidazol-4-yl)methylthio]ethyl guanidine] was administered orally to eight male and four female beagle dogs at a dose level of 144 mg per kg bodyweight per day. Four males and two females received placebo tablets. Dosing began in March 1976. During the
Biochemistry and neurotoxicology of guanidino compounds. History and recent advances.
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Guanidino compounds are known to have important biological roles, such as the participation of arginine in ureagenesis, and of creatine in muscular contraction. On the other hand, the high toxicity of guanidino compounds, such as methylguanidine and guanidine, has been under study for quite a long
A role for guanidino compounds in the brain.
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Guanidino compounds of guanidinoethanesulfonic acid, guanidinoacetic acid, guanidinosuccinic acid, N-acetylarginine, beta-guanidinopropionic acid, creatinine, gamma-guanidinobutyric acid, arginine, guanidine, methylguanidine, homoarginine and alpha-guanidinoglutaric acid are present in the mammalian
Guanidino compounds in serum and brain of audiogenically sensitive rats.
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The levels of 12 guanidino compounds were determined in serum and brain of audiogenically sensitive rats with and without seizures. During audiogenic seizures the serum levels of creatine are significantly decreased, while those of guanidinoacetic acid, N-alpha-acetylarginine, creatinine,
Guanidino compounds inhibit acetylcholinesterase and butyrylcholinesterase activities: effect neuroprotector of vitamins E plus C.
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Hyperargininemia is a metabolic disorder biochemically characterized by tissue accumulating of arginine and other guanidino compounds. Convulsions, lethargy and psychomotor delay or cognitive deterioration are predominant clinical features of this disease. Although neurologic symptoms predominate in
Convulsive action and toxicity of uremic guanidino compounds: behavioral assessment and relation to brain concentration in adult mice.
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Four guanidino compounds that are known to accumulate in uremia, namely creatinine, guanidine, guanidinosuccinic acid and methylguanidine, were administered intraperitoneally and intracerebroventricularly to adult albino mice and the compounds epileptogenic and toxic properties were behaviorally
Synthesis, Anticonvulsant, Antimicrobial and Analgesic activity of Novel 1,2,4-Dithiazoles.
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A series of 1,2,4-dithiazole were synthesized from 1,2,4-thiadiazoles in the presence of CS(2) and evaluated for their antimicrobial, anticonvulsant, analgesic and neurotoxicity potential. The compounds provided significant protection against maximal electroshock-induced seizures and seizures
Design, synthesis, and pharmacological evaluation of conformationally constrained analogues of N,N'-diaryl- and N-aryl-N-aralkylguanidines as potent inhibitors of neuronal Na+ channels.
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In the present investigation, the rationale for the design, synthesis, and biological evaluation of potent inhibitors of neuronal Na+ channels is described. N,N'-diaryl- and N-aryl-N-aralkylguanidine templates were locked in conformations mimicking the permissible conformations of the flexible
Guanidino compound levels in brain regions of non-dialyzed uremic patients.
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Guanidino compounds have been suggested to contribute to the complex neurological complications associated with uremia. Several of them have previously been reported to accumulate in physiological fluids of renal insufficient subjects. We report on guanidino compound levels in 28 brain regions in
Potential anticonvulsant activity of novel VV-hemorphin-7 analogues containing unnatural amino acids: synthesis and characterization.
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Herein, some new analogues of VV-hemorphin-7, modified at position 4 and 7 by the unnatural amino acids followed the structure Val-Val-Tyr-Xxx-Trp-Thr-Yyy-Arg-Phe-NH2, where Xxx is Ac5c (1-aminocyclopentanecarboxylic acid) or Ac6c (1-aminocyclohexane carboxylic acid) and Yyy is Dap
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