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  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 45 (1985), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: Both alprazolam and triazolam displaced clonazepam (but not Ro 5–4864) from rat brain membranes with high affinity, showing them to act at central but not peripheral benzodiazepine receptors. At 0°C, 10 μMγ-aminobutyric acid (GABA) increased the ability of alprazolam, but not of triazolam, to displace ethyl-β-carboline-3-carboxylate (β-CCE) and Ro 15–1788 from these receptors. At 37°C, GABA increased the affinity of the receptors for both drugs, with a +GABA/–GABA ratio of 1.5 for each in promoting Ro 15–1788 binding displacement. As both triazolam and alprazolam act as anxiolytics in vivo, the results at 37°C would be compatible with the hypothesis that GABA causes an increase in affinity of drugs that act in this way, but the results at 0°C would not be compatible. At 37°C, alprazolam had a higher IC50 for the benzodiazepine receptor than at 0°C, whereas triazolam showed the reverse effect. The relative IC50 values in vitro at 37°C correlated better with the potency in vivo than those obtained at 0°C. At 0°C, both drugs showed Hill plots with slopes of 0.9–1 with β-CCE and Ro 15–1788. At 37°C, the slopes with triazolam were much reduced, indicating that the drug may have a selective action on a subclass of central benzodiazepine receptors. In the studies reported here, alprazolam behaved like other benzodiazepines, whereas triazolam showed several anomalous properties. It would be of interest if these properties could be related either to the drug's use as a hypnotic or to the side effects it sometimes induces.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1433-8491
    Keywords: Phenylethylamine ; Phenylacetic acid ; Schizophrenia ; CSF ; Phenyläthylamin ; Phenylessigsäure ; Schizophrenie ; CSF
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Phenyläthylamin (PEA) ist eine endogene Substanz mit amphetaminähnlichen, stimulierenden Eigenschaften, die auch im menschlichen Organismus vorkommt. Wegen dieser Wirkungen ist ein veränderter PEA Stoffwechsel bei bestimmten Formen von Schizophrenie zu vermuten. In der vorliegenden Studie wurde bei 28 schizophrenen Patienten und 15 psychisch gesunden Kontrollpersonen PEA und Phenylessigsäure (PAA) gemessen. Im Liquor cerebrospinalis unbehandelter und behandelter Patienten mit paranoider Schizophrenie sowie gesunder Kontrollen wurden keine signifikant unterschiedlichen PEA Konzentrationen gefunden. Allerdings zeigten die zwei Patienten mit den höchsten Psychosescores in der Brief Psychiatric Rating Scale extrem hohe PEA Werte im Liquor. Dagegen war die unkonjugierte Phenylessigsäure (PAA), der Hauptmetabolit des PEA, signifikant bei unbehandelten Schizophrenen erniedrigt (P〈0.05). Da PEA vermutlich neuromodulatorische Wirkungen hat, kann angenommen werden, daß schon äußerst geringe und spezifisch lokalisierte Veränderungen im PEA Stoffwechsel (wie in der erniedrigten PAA und der partiellen Erhöhung von PEA zum Ausdruck kommt) veränderte zentrale Neurotransmission in bestimmten Schizophrenieformen bewirken.
    Notes: Summary Phenylethylamine (PEA) is an endogenous substance with amphetamine-like stimulant properties. On the basis of this ability an abnormal brain PEA metabolism has been proposed as an etiological factor in some forms of schizophrenia. In the present study 28 schizophrenic patients and 15 healthy controls were investigated. No significant difference from control values was found in PEA concentration in cerebrospinal fluid (CSF) of either untreated or neuroleptic-treated schizophrenics. However, 2 schizophrenics with highest BPRS scores had extremely high PEA concentrations. Free phenylacetic acid (PAA), the major metabolite of PEA, was significantly decreased in ummedicated but not in drug-treated schizophrenics. Because of the assumed neuromodulatory properties of PEA, it is suggested that lowered PAA concentrations and the tendency for PEA to be elevated may imply that altered central neurotransmission occurs in certain forms of schizophrenia.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    New York, NY [u.a.] : Wiley-Blackwell
    Cell Biochemistry and Function 4 (1986), S. 89-97 
    ISSN: 0263-6484
    Keywords: Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Medicine
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1052-9306
    Keywords: Chemistry ; Analytical Chemistry and Spectroscopy
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: When melatonin is reacted with pentafluoropropionic anhydride for selected ion monitoring or electron capture gas chromatographic analysis a volatile product results. Examination of the product by combined gas chromatography mass spectrometry has established that the molecular weight of 360 corresponds to the addition of one molecule of pentafluoropropionic acid followed by dehydration. Further spectroscopic and chemical examination using mass spectrometry and nuclear magnetic resonance with isotopic labelling has established that the product is a 3,3-spirocyclic indole derivative. Several analogous compounds were also examined and their mass spectra studied.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
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