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  • 1
    Electronic Resource
    Electronic Resource
    A pharmacokinetic study of CGS-8216, a benzodiazepine receptor ligand, in the rat (1984)
    Springer
    Psychopharmacology 84 (1984), S. 420-422 
    Details
    ISSN: 1432-2072
    Keywords: CGS-8216 ; Benzodiazepine ; Plasma ; Pharmacokinetics ; Rat ; Brain
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract A rapid and sensitive method is described for the determination of CGS-8216 (a pyrazoloquinoline that displaces benzodiazepines from their binding sites in the brain but which reverses some of the behavioural actions of the benzodiazepines) in plasma using high-performance liquid chromatography with ultraviolet detection. CGS-9896 serves as the internal standard. The method is applied to a pharmacokinetic study of CGS-8216 in the rat. CGS-8216 was not detectable in plasma 24 h after a single IP administration of a 10 mg/kg dose. Animals treated with five once-daily injections of CGS-8216 had plasma concentrations 30 min after the final injection that were approximately four-times those observed 30 min after a single treatment. This suggests that caution must be used in the interpretation of results from experiments using multiple administrations of CGS-8216. The compound could not be detected in brain tissue at any of the time points studied.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00555224
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    A late-appearing benzodiazepine-induced hypoactivity that is not reversed by a receptor antagonist (1986)
    Springer
    Psychopharmacology 88 (1986), S. 520-524 
    Details
    ISSN: 1432-2072
    Keywords: Benzodiazepine ; Sedation ; Locomotor activity ; Exploration ; Withdrawal ; Benzodiazepine antagonist ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The activity of rats in a holeboard test is reduced 30, 90, and 240 min after treatment with a single dose of lorazepam. The administration of a benzodiazepine antagonist (RO 15-1788) 20 min before the holeboard test (i.e., 10, 70, or 220 min after lorazepam administration) reverses the hypoactivity of animals tested 30 min after treatment with lorazepam, partially reverses the hypoactivity of animals tested 90 min after receiving lorazepam, but is without effect on the hypoactivity observed 240 min after treatment with the benzodiazepine. If, however, RO 15-1788 is given at the same time as lorazepam then it reverses the hypoactivity seen 4 h later. The results of these experiments demonstrate that a benzodiazepine can exert a behavioral effect at a time when it no longer appears to be acting at central benzodiazepine receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00178518
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
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