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  • 1
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 279 (1973), S. 371-380 
    ISSN: 1432-1912
    Schlagwort(e): Serotonin ; Dopamine ; Noradrenaline ; Alkaloids ; Synaptosomes ; Brain Chemistry
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The effect of some tetrahydroharmane derivatives on the synaptosomal uptake of monoamines was studied. 1,2,3,4-Tetrahydroharmane (TH), which can be viewed as an analog of tryptamine, inhibited 5-hydroxytryptamine (5-HT), noradrenaline (NA) and dopamine (DA) uptake, but TH was about 10 times less potent than tryptamine. 6-Hydroxy-1,2,3,4-tetrahydroharmane (6-HTH), a 5-HT analog, was slightly more potent an inhibitor of 5-HT uptake than TH, but as catecholamine uptake inhibitors these compounds were equipotent. Harmane-1,2,3,4-tetrahydro-3-carboxylic acid had no effect. Salsolinol and salsolidine, tetrahydroisoquinoline derivatives, were less potent than the harmane derivatives. It is to be concluded that also tetrahydroharmane derivatives have an affinity to the amine “pump” similarly to that of the tetrahydroisoquinolines, which are the corresponding analogs of catecholamines. These kinds of compounds are important because of the possibility that they may be formed in physiological conditions as condensation products of biogenic amines and aldehydes, e.g. acetaldehyde, which is an intermediate of ethanol metabolism.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 279 (1973), S. 361-370 
    ISSN: 1432-1912
    Schlagwort(e): Serotonin ; Histamine ; Blood Platelets ; Alkaloids
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The effect of 5-hydroxytryptamine (5-HT), tryptamine (T), 6-hydroxy-1,2,3,4-tetrahydroharmane (6-HTH), and 1,2,3,4-tetrahydroharmane (TH) on the accumulation of radioactive 5-HT and histamine, was studied in rabbit blood platelets. 6-HTH and TH inhibited the uptake of the labelled amine, but they were weaker inhibitors than 5-HT or T. All four compounds inhibited the accumulation of radioactive histamine in the granules as well as in the whole cells, but the latter effect is not the consequence of inhibition of granular accumulation. It is concluded that the methylene bridge, which is the most important structural difference between the harmanes and the tryptamines, does not abolish the affinity of the molecule to the uptake receptor at the platelet membrane. However, since the inhibitory potency was lower than that of the parent amines, one cannot be certain as to whether or not the conformation present in the harmane derivatives offers the best fit for the receptor.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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