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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 332 (1986), S. 8-15 
    ISSN: 1432-1912
    Keywords: Perfused rat kidney ; 5-Hydroxytryptamine ; 5-Hydroxytryptamine agonists ; 5-Hydroxytryptamine antagonists ; 5-Hydroxytryptamine receptors ; Prejunctional 5-HT1-like receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The present study has identified a receptor for 5-hydroxytryptamine (5-HT) which functions to inhibit the stimulus-induced release of [3H] noradrenaline following sympathetic periarterial nerve stimulation to the isolated perfused rat kidney. In addition to 5-HT (IC30=4.5×10−8 mol/l), both 5-carboxamidotryptamine (IC30=8×10−9 mol/l) and 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl) indole (RU-24969, IC30=2.5×10−7 mol/l) acted as agonists whereas 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) was inactive. The inhibitory effect of 5-HT on the electrically-evoked release of tritium was antagonized in a concentration-dependent manner by methiothepin (IC50=4×10−9 mol/l), metergoline (IC50=4×10−8 mol/l) and methysergide (IC50=1.3×10−7 mol/l) but not by cyproheptadine, ketanserin, mesulergine, (−)-propranolol, (±)-pindolol, (±)-cyanopindolol, metoclopramide or phentolamine. It is concluded that the receptor to 5-HT conforms to general criteria defining 5-HT1-like receptors but at the present time the receptor site cannot be fitted to the designated 5-HT1A, 5-HT1B or 5-HT1C subtypes.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1912
    Keywords: 5-Hydroxytryptamine ; Serotonin receptors ; 5-Hydroxykynuramine ; Alpha1-adrenoceptors ; Perfused rat kidney
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Kynuramines are endogenously occurring diamines derived from tryptophan. In the present study, we have compared the pharmacological actions of 5-hydroxykynuramine (5-OH-K) with kynuramine and 5-hydroxytryptamine (5-HT) on vascular resistance changes and responsiveness to adrenergic stimuli in the isolated perfused rat kidney. 5-OH-K was found to mimic the actions of 5-HT in that it produced vasoconstriction, potentiation of alpha1-adrenoceptor-mediated responses to norepinephrine (NE) and periarterial nerve stimulation and displaced specific [3H]spiroperidol binding from rat cortical membranes. With regard to all parameters measured, 5-OH-K was about 15-times less active than 5-HT. Vascular responses to 5-OH-K and 5-HT were inhibited noncompetitively by ketanserin and cyproheptadine. Unlike 5-OH-K, kynuramine, failed to evoke vasoconstriction and Inhibited vascular responses to NE via alpha1-adrenoceptors. Thus, kynuramine lacks serotonin receptor agonist activity but possesses alphaI-adrenoceptor blocking properties. In contrast, 5-OH-K potentiates NE and acts as a serotonin agonist. The present results raise the possibility that kynuramine and 5-OH-K might act as endogenous modulators of serotonergic and adrenergic mechanisms in the renal vascular bed.
    Type of Medium: Electronic Resource
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