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  • 1
    Electronic Resource
    Electronic Resource
    Synergism between 5-HT1B/1D and 5-HT1A receptor antagonists on turnover and release of 5-HT in guinea-pig brain in vivo (1999)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 359 (1999), S. 110-116 
    Details
    ISSN: 1432-1912
    Keywords: Key words 5-HT1B and 5-HT1A receptors ; 5-HT turnover ; 5-HT release ; Guinea pigs ; GR 127935 ; WAY-100635 ; Microdialysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects on 5-HT turnover (5-HIAA/5-HT ratio) and extracellular 5-HT and 5-HIAA levels (in vivo microdialysis in freely moving animals) were analysed in guinea-pig brains following the 5-HT1B receptor antagonist, GR 127935 {N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2’-methyl-4’-(5-methyl-1,2,4-oxadiazol-3-yl) [1,1-biphenyl]-4-carboxamide}, or the 5-HT1A receptor antagonist, WAY-100635 (N-{2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl}-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride), administered alone or in combination. GR 127935, injected alone, increased 5-HT turnover with maximal effects approximately 50% above the control levels in the four brain regions examined (hypothalamus, hippocampus, striatum and frontal cortex). GR 127935 significantly increased extracellular concentrations of 5-HT and 5-HIAA in frontal cortex (40%), whereas 5-HIAA, but not 5-HT, was elevated in striatum (20–30%). WAY-100635 did not significantly change 5-HT turnover but caused a small significant increase in the extracellular 5-HT and 5-HIAA concentrations in both striatum and frontal cortex. The combined treatment with GR 127935 and WAY-100635 resulted in an increased 5-HT turnover reaching maximal effects of 70–90% above the control values in all brain regions tested and produced a significant elevation of striatal and frontal cortex extracellular 5-HT (40% and 60%, respectively) and 5-HIAA (60% and 70%, respectively) concentrations. The synergistic effect of the two receptor antagonists on the 5-HT turnover and the terminal release of 5-HT indicate somatodendritic 5-HT release and stimulation of inhibitory 5-HT1A receptors at this level. Extracellular 5-HIAA seems to be a better marker than 5-HT itself for the evoked 5-HT release when the reuptake mechanism is intact.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/PL00005329
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Ability of obstructed bladders to empty is dependent on method of stimulation (1997)
    Springer
    Urological research 25 (1997), S. 291-298 
    Details
    ISSN: 1434-0879
    Keywords: Bladder ; Obstruction ; Stimulation ; Rabbit ; Function ; Work
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Purpose: To correlate pharmacologic changes that occur in the bladder after a partial outlet obstruction with the bladder's ability to perform work and empty. Methods: After 2 weeks of partial outlet obstruction, rabbit bladders were stimulated in vitro both isovolumetrically [field stimulation (FS)] and to empty (FS, bethanechol, and KCl). Results: The obstructed bladders were separated into two groups according to their ability to empty when stimulated with FS. Compensated bladders were those that could empty as much as controls. Decompensated bladders emptied significantly less than controls. With FS and bethanechol, the compensated obstructed bladders showed no difference from the control bladders in their ability to empty. In contrast, with Kcl, the compensated bladders generated significantly less pressure, performed less work, and emptied less than controls. When the decompensated bladders were stimulated with all three types of stimulation, all parameters, including emptying ability, were significantly decreased. Conclusions: The reduction in the response of compensated bladders to Kc1 stimulation suggested that the initial defects to the bladder after an outlet obstruction involved the interaction of smooth muscle proteins with calcium and ATP. In contrast, the response of decompensated bladders to all three forms of stimulation was equally reduced, suggesting that the degenerative processes were directly related to significant cellular damage to metabolic processes involved in energy synthesis, storage, and utilization.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00942101
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    Paper (German National Licenses)
    Fulltext
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