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  • 1
    Electronic Resource
    Electronic Resource
    Evidence for common pharmacological properties of [3H]5-hydroxytryptamine binding sites, presynaptic 5-hydroxytryptamine autoreceptors in CNS and inhibitory presynaptic 5-hydroxytryptamine receptors on sympathetic nerves (1983)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 324 (1983), S. 116-124 
    Details
    ISSN: 1432-1912
    Keywords: [3H]5-HT binding sites ; 5-HT autoreceptors ; Presynaptic receptors ; Rat cerebral cortex ; Canine saphenous vein
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The affinities of 16 5-hydroxytryptamine (5-HT) receptor agonists (indole derivatives) and 7 5-HT receptor antagonists for [3H]5-hydroxytryptamine ([3H]5-HT) binding sites in rat cerebral cortex membranes were determined. In addition, the potencies of the agonists for inhibiting the electrically induced tritium overflow from rat brain cortex slices preincubated with [3H]5-HT and from canine saphenous veins preincubated with [3H]noradrenaline were measured. Furthermore, the potencies of the indole derivatives for inducing contractile responses of canine saphenous veins were recorded. In addition, the interaction of the antagonists with unlabelled 5-HT at the 5-HT autoreceptor was studied in rat brain cortex slices. There was a good correlation between the binding affinities of the indole derivatives for the [3H]5-HT sites of rat brain cortex membranes and their potencies for inhibiting the evoked tritium overflow from both rat brain cortex slices and strips of canine saphenous vein. Comparison of the inhibition constants derived from the overflow experiments in both tissues again revealed a high correlation coefficient while there was only weak correlation between the binding affinities in rat brain cortex and the contractile potencies of the drugs in canine saphenous vein strips. When 5-HT receptor antagonists were investigated, metitepin and metergoline showed moderate affinities for the 5-HT autoreceptors in rat brain cortex slices, whereas quipazine had only weak affinity, and ketanserin, metoclopramide, cinanserin and cyproheptadine exhibited no antagonistic property. In binding experiments, the competition curves of most 5-HT receptor antagonists were biphasic, suggesting that the [3H]5-HT binding sites are heterogeneous. The affinities of the antagonists to the low affinity binding sites were roughly in accordance with their affinities for the 5-HT autoreceptors determined in release experiments. It is concluded that [3H]5-HT binding sites, presynaptic 5-HT autoreceptors in the rat brain cortex and inhibitory presynaptic 5-HT receptors on sympathetic nerve endings in the canine saphenous vein possess common pharmacological properties. In the rat brain cortex, the 5-HT1 sites are not homogeneous. Part of the [3H]5-HT binding sites (low affinity sites rather than high affinity sites) may be localized on the serotoninergic neurones and, hence, be identical with the serotonin autoreceptors. The results are also compatible with the suggestion that there may exist even more than two subtypes of [3H]5-HT1 binding sites in the rat brain cortex.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00497016
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  • 2
    Electronic Resource
    Electronic Resource
    Sucrose promotes the functional activity of blood vessels after cryopreservation in DMSO-containing fetal calf serum (1992)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 345 (1992), S. 594-597 
    Details
    ISSN: 1432-1912
    Keywords: Cryopreservation ; Blood vessels ; DMSO ; Sucrose
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The cryoprotective effect of sucrose has been investigated using 3 different vascular smooth muscle preparations, namely canine saphenous veins and arteries and porcine circumflex coronary arteries following storage in liquid nitrogen (at −196°C). Contractile responses to noradrenaline, 5-HT, prostaglandin F2α and KCl and relaxant responses to substance P and 5-HT were determined on fresh tissues and after cryostorage in fetal calf serum (FCS) containing either 1.8 M dimethyl sulfoxide (DMSO), or 0.1 M sucrose or both agents combined. The data demonstrate that the addition of sucrose to the DMSO-containing cryomedium promotes the preservation of both contractile and relaxant activity of cryostored blood vessels, though sucrose alone did not confer any noticeable protection.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00168954
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacological actions of the main metabolites of dihydroergotamine (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 699-705 
    Details
    ISSN: 1432-1041
    Keywords: dihydroergotamine metabolites ; man ; mammals ; pharmacological action ; venoconstriction ; varicose veins
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Dihydroergotamine (DHE) and 5 of its main metabolites, namely 8′-hydroxy-dihydroergotamine (8′-OH-DHE), 8′,10′-dihydroxy-dihydroergotamine (8′,10′-OH-DHE), 2,3seco,N(1)formyl,3-keto,8′-hydroxy-dihydroergotamine (8′-OH,N(1)formyl-DHE), dihydrolysergic acid amide (DH-LSA) and dihydrolysergic acid (DH-LS) were investigated on human and canine veins in vitro, on canine veins in situ, and in the ganglion-blocked rat in vivo. Like DHE, the metabolites 8′-OH-DHE, 8′,10′-OH-DHE and DH-LSA caused contriction of human varicose veins and only weak α-adrenoceptor blockade. On canine femoral vein strips the same compounds produced predominantly α-adrenoceptor blockade and only negligible stimulation. 8′-OH,N(1)formyl-DHE and DH-LS were largely inactive. The same compounds, which were agonists on human vein strips in vitro, induced dose-dependent reduction of venous compliance when infused locally into the dog saphenous vein in situ. In the ganglion-blocked rat, only 8′-OH-DHE and 8′,10′-OH-DHE besides the parent drug produced an increase in diastolic blood pressure when injected intravenously. It is concluded that DHE metabolites with considerable venoconstrictor activity may contribute to the selective therapeutic action of DHE.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00541928
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    Paper (German National Licenses)
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