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  • 1
    ISSN: 1432-1041
    Keywords: Acipimox ; Skin flush ; healthy volunteers plasma level
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Facial skin flush is the most frequent adverse effect induced by acipimox (ACX), a nicotinic acid analogue used in the management of hyperlipidaemia. The aims of the study were to evaluate the frequency, magnitude and reproducibility of the ACX flush in previously unexposed healthy subjects and to assess any possible relationship with the dose and plasma level of ACX. Seventy four healthy subjects received, on two different mornings, ACX 250 mg and placebo (P), according to a single blind, randomized, cross-over design; 33 had a clear flush after ACX and not after P.25 of those subjects were retested on five different mornings, with P, and with ACX 31.2, 62.5, 125.0, 250.0 mg, according to a double blind, randomized, cross-over design. Any increase in the local skin temperature was recorded by a thermocouple fixed to the left check. Subjective and objective assessment of the flush were strongly correlated with thermographic recordings. They indicated that a 120 min flush occurred after doses of ACX 〉 62.5 mg. In 12 of the 25 subjects, 6 with the highest and 6 with the lowest thermographic recordings, plasma ACX levels were determined. Subjects with different thermographic records had superimposable plasma ACX levels after all doses of ACX. Only the 6 subjects with the highest skin temperatures showed a significant relationship between the thermographic record and the plasma ACX. The data indicate that flush is a frequent, reproducible and dose-related adverse effect of ACX.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 36 (1981), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: The inhibition of type A and B MAO in rat forebrain crude membrane preparation by MD780515. (3-{4-[(3-cyanophenyl)methoxy]phenyl)-5-(methoxymethyl)-2-oxazolidinone Centre de Recherche Delalande, France) has been investigated in vitro with 5-hydroxytryptamine and β-phenylethyl-amine as substrates. The inhibition of the high-affinity binding of [3H]harmaline, a specific marker of type A MAO, was also studied. In the experimental conditions used, MD780515 appeared to be a pure mixed MAO inhibitor (MAOI) of 5-HT deamination, both Km, and Vmax being altered [K1 (Dixon) =Ki, (slope) = 2 nM; Ki (intercept) = 12 nM]. Phenylethylamine oxidation could be considered to be noncompetitively inhibited by MD780515 (Ki (slope) = 78 nM; Ki, (intercept) = 103 nM). Dixon and intercept replots were hyperbolic, suggesting that, at high concentrations, PEA could be deaminated by both forms of MAO. This hypothesis was confirmed by biphasic inhibition curves of 80 μM-PEA obtained when MD780515, clorgyline, harmaline and deprenyl were used as MAOIs. MD780515 was a potent inhibitor (IC50= 1–2 nM) of [3H]harmaline binding. Comparatively, clorgyline, ‘cold’ harmaline and Lilly 51641 inhibited 3H ligand binding, with IC50 of 5, 7 and 40 nM respectively. In conclusion, MD780515 is a reversible, specific and potent type A MAOI.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 35 (1980), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: The activity of monoamine oxidase (MAO) was assayed in the brains of young adult (7–8 weeks old) and aging (95–104 weeks old) male Sprague-Dawley rats. When expressed per milligramme of tissue, total protein content was increased to a similar extent in whole brain and in all seven brain regions of the aging rat, whereas MAO A activity (assayed by using 5-hydroxytryptamine as substrate) was unchanged in whole brain but increased in the cerebellum, and fell in the brainstem, midbrain, hippocampus, and cortex; and MAO B activity (assayed by using β-phenylethylamine as substrate) increased in whole brain and all regions, except the brainstem. Age-related changes in total protein, MAO A, and MAO B were thus independent of each other. Kinetic studies indicated that the Vmax of MAO B was increased in aging rat brain, whereas the Km was unaltered. The increase in MAO B activity was restricted to the extrasynaptosomal mitochondrial fraction of the aging brain, whereas a reduction in MAO A activity was found in the intrasynaptosomal, but not the extrasynaptosomal mitochondrial fraction.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Journal of neural transmission 86 (1991), S. 191-203 
    ISSN: 1435-1463
    Keywords: Ageing ; rat brain ; amino acids
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Concentrations of the sulfur-containing amino acids methionine, homocysteic acid, cysteic acid and taurine were measured in brain structures of young and old Wistar rats in an attempt to etablish a possible link between the increase in oxidative stress with ageing and changes in tissue levels of these amino acids. Contrary to data reported by others, in all brain structures of young and old rats homocysteic acid levels could not be quantified. Compared with young rats, in old animals taurine and methionine concentrations significantly decreased in striatum and cortex; decreased taurine levels were also found in nucleus accumbens and cerebellum and lower concentrations of methionine were found in midbrain, hippocampus and pons-medulla. Cysteic acid levels either did not change or significantly increased in cortex and hippocampus. These results are discussed taking into account the biosynthesis of sulfur-containing amino acids in rat brain and the decrease in glutathione in relation to oxidative stress with ageing. Changes in aspartic acid, glutamic acid, serine, glutamine, glycine and GABA concentrations with ageing were also determined in the same brain structures and were in good agreement with those previously reported
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1435-1463
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Journal of neural transmission 1 (1989), S. 269-278 
    ISSN: 1435-1463
    Keywords: R and S salsolinol ; Parkinsonian patients ; L-dopa ; pyruvate ; acetaldehyde ; dopamine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Urinary salsolinol output had been shown to be lower in Parkinsonian patients than in controls and to increase largely after L-dopa therapy. It had also been established that the R enantiomer of salsolinol is either the predominant or the sole enantiomer present in the urine of healthy subjects. When Madopar was administered to Parkinsonians, the enantiomeric composition of urinary salsolinol showed an S/R ratio around 1. Considering brain and plasma concentrations in dopamine, acetaldehyde and pyruvate, it is suggested that, under physiological conditions, urinary salsolinol should have a central origin in humans. Conversely, urinary salsolinol in Madopar-treated Parkinsonian patients might be predominantly formed at the periphery.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1435-1463
    Keywords: MAO inhibitors ; moclobemide ; Ro 19-6327 ; amino acids ; aging
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary In a previous paper a possible relationship had been suggested to exist between age-induced changes in total MAO activity and amino acid levels in some rat brain areas. To further investigate the possible involvement of MAO activity in changes of brain amino acid levels with aging, moclobemide and Ro 19-6327, short acting MAO-A and MAO-B inhibitors, respectively, were administered to female Wistar rats for their whole life-span. Brain amino acid levels in animals treated with MAO inhibitors were compared to those of young and old nontreated rats. The age-induced changes in brain amino acid concentrations found in the present study were in good agreement with those previously reported. Treatment with both moclobemide and Ro 19-6327 was found to restore taurine and serine concentrations in cortex and glutamine concentrations in cerebellum, to the same values as in young rats, to decrease cerebellum concentrations of serine and to increase taurine concentrations in hypothalamus. Administration of moclobemide brought aspartate concentrations in accumbens and cortex back to the same values as in young rats. A similar effect was observed on hypothalamus glutamate concentrations in rats treated with Ro 19-6327. Some possible causes and consequences of the correction of age-induced brain amino acid levels by chronic administration of MAO inhibitors are discussed.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Journal of neural transmission 77 (1989), S. 47-53 
    ISSN: 1435-1463
    Keywords: R and S salsolinol ; food ; human urine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Salsolinol is present in human fluids and tissues as well as in some foods and beverages. It was found previously that the R enantiomer of salsolinol predominates in human urine whereas the S enantiomer predominates in Port wine. In this study a new methodology for measuring the proportion of the R and S salsolinol enantiomers in dried banana and human urine is described. In dried banana, a food particularly rich in salsolinol, the R/S ratio was found to be very near to 1. In urine from additional healthy volunteers, the presence of only the R enantiomer was detected. The origin of urinary salsolinol and its enantiomeric composition are discussed with respect to exogenous salsolinol.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 33 (1977), S. 1485-1486 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: summary The14C-labelled, substituted benzamide neuroleptic Tiapride has been found to accumulate transiently in the pituitary gland of the rat following a single dose, and a prolonged retention of the drug was observed in the pars intermedia.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 36 (1980), S. 818-820 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary In the rat, histamine metabolism is altered by some nonspecific inhibitors of monoamine oxidase (MAO) such as iproniazid, and, to a lesser extent, tranylcypromine. Type A MAO inhibitors, such as clorgyline and MD780515, do not seem to interfere with the metabolism of histamine. Deprenyl, a type B MAO inhibitor, shows some inhibition which is, however, much lower than that observed with iproniazid. The strong effect of iproniazid is probably due to its DAO inhibiting properties.
    Type of Medium: Electronic Resource
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