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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 318 (1981), S. 83-87 
    ISSN: 1432-1912
    Keywords: Release of noradrenaline ; Tyramine ; Dog saphenous vein ; Kinetic analysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Dog saphenous vein strips obtained from untreated or reserpine-pretreated animals were incubated with 1,4 μmol/l 3H-(−)noradrenaline for 60 min after inhibition of the noradrenaline-metabolizing enzymes and of extraneuronal uptake. At the end of the incubation period the strips were perifused during 200 min. Some strips were exposed to tyramine from the 100th to the 200th min of perifusion. A compartment analysis of spontaneous or tyramine-induced efflux of 3H-noradrenaline was made. The spontaneous efflux of strips obtained from untreated animals had a long half time (t/2=269 min), and most of the 3H-noradrenaline which accumulated in the strips did not participate in the efflux (“bound fraction”, representing 85% of tissue activity at the 100th min of perifusion). The strips were exposed to five concentrations of tyramine, ranging from 0.49–3,240 μmol/l. At all concentrations, tyramine mobilized only one noradrenaline compartment. The increase of tyramine concentration decreased the “bound fraction”, which became negligible for the highest concentration of tyramine. The half time of 3H-efflux induced by tyramine decreased from 278–106 min when the tyramine concentration was increased from 0.49–40 μmol/l. However, further increases of the concentration of tyramine up to 3240 μmol/l did not result in a significantly lower half time. Strips obtained from reserpine-pretreated animals were characterized by a low accumulation of 3H-noradrenaline (403 ng/g vs. 1,374 ng/g for strips obtained from unpretreated animals, at the 100th min of perifusion), the efflux had a half time of only 122 min and the “bound fraction” was smaller than in strips obtained from unpretreated animals (“bound fraction” representing 47% of tissue activity at the 100th min of perifusion). Reserpine-pretreated strips were exposed to 40 μmol/l tyramine. Under these experimental conditions there was no significant “bound fraction”. The 3H-efflux induced by tyramine decayed according to a two-compartment model, with half times of 8 and 50 min. The results support the view that in preparations from unpretreated animals the size of the noradrenaline pool available for release by tyramine is dependent on the concentration of the latter amine. Furthermore, the half time of the efflux evoked by tyramine in strips with intact vesicular stores is dependent on a rate-limiting process, probably of vesicular location.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 328 (1985), S. 248-252 
    ISSN: 1432-1912
    Keywords: Release of noradrenaline ; Dog saphenous vein ; Kinetic analysis ; Presynaptic α-adrenoceptors ; Electrical stimulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Dog saphenous vein strips were incubated with 1.4 μmol/l 3H-(-)-noradrenaline for 60 min, after inhibition of the noradrenaline-metabolizing enzymes and of extraneuronal uptake. At the end of the incubation period the strips were perifused for 150 min; cocaine (10 μmol/l) was added to the perifusion fluid from t=75 min onwards. In some experiments either phentolamine (10 μmol/l) or clonidine (0.1 μmol/l) was also added at this time. Some strips were subjected to electrical stimulation from t=100 to 150 min of perifusion (t=0 being the start of perifusion), with frequencies ranging from 0.5 to 13.5 Hz. A compartmental analysis of spontaneous or electrically-induced efflux of 3H-noradrenaline was made. The spontaneous efflux had a long half time (t/2=124 min) and most of the 3H-noradrenaline which had accumulated in the strips did not participate in the efflux (“bound fraction”, representing 90% of tissue activity at t=100 min of perifusion). Neither phentolamine nor clonidine modified the half time or the “bound fraction” observed for spontaneous efflux. Electrical stimulation (〉0.5 Hz) mobilized only one compartment of noradrenaline, which represented about 50% of the noradrenaline accumulated in the strips. The half time of 3H-efflux induced by electrical stimulation decreased when the frequency increased from 0.5 Hz up to 13.5 Hz. Phentolamine increased the rate of efflux for all frequencies of stimulation and decreased the half time of efflux. However, the releasable pool of noradrenaline was only increased by phentolamine at 0.5 Hz, but not at higher frequencies. Clonidine was used only at two frequencies of stimulation, 1.5 and 4.5 Hz. For the low frequency clonidine decreased the releasable pool, but no change was observed at 4.5 Hz. The results support the view that there is a norarenaline pool which is resistant to electrical stimulation and that its magnitude is not dependent on the activity of presynaptic α-adrenoceptors.
    Type of Medium: Electronic Resource
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