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  • 1
    Electronic Resource
    Electronic Resource
    Pharmacodynamic profile of CQP 201-403, a novel 8α-amino-ergoline (1988)
    Springer
    Cellular and molecular life sciences 44 (1988), S. 431-436 
    Details
    ISSN: 1420-9071
    Keywords: CQP 201-403 ; 8α-amino-ergolines ; ergot pharmacology ; D-2 agonist ; endocrine ; CNS ; cardiovascular actions
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary The profile of action in animals of CQP 201-403, a novel 8α-amino-ergoline, is in most aspects that of a very potent dopaminomimetic, both as a prolactin secretion inhibitor, and at the levels of the CNS and the cardiovascular system. Qualitatively CQP 201-403 differs slightly from bromocriptine and apomorphine in its effects on the CNS (no influence on serotonin metabolism in the rat cortex; induction of masculine mounting behavior in rats) and the cardiovascular system of the dog (reflex tachycardia in response to a blood-pressure fall). In man the new compound proved to be highly active in lowering prolactin serum levels and to be more potent than bromocriptine (Parlodel®).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01940539
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  • 2
    Electronic Resource
    Electronic Resource
    Biochemical, behavioural, and endocrine effects of CK 204-933, a novel 8β-ergolene (1987)
    Springer
    Journal of neural transmission 69 (1987), S. 179-199 
    Details
    ISSN: 1435-1463
    Keywords: Ergoline ; dopamine ; noradrenaline ; serotonin ; rat brain
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary CK 204-933 displaces [3H]dopamine and [3H]spiperonene with high affinity from D-1 and D-2 recognition sites in membranes of calf caudate. Results from functionalin vitro tests suggest that it is a partial agonist at D-1 receptors and an antagonist at D-2 receptors. These opposite effects at dopamine receptor subtypes are also expressedin vivo. For instance, in 6-hydroxydopamine lesioned rats, CK 204-933 induces contralateral rotations which are antagonised by SCH 23390 but not by sulpiride. On the other hand, CK 204-933 induces a long lasting increase of dopamine turnover in rat striatum and antagonises apomorphine-induced gnawing behaviour in rats. CK 204-933 increases prolactin serum levels in rats after subcutaneous administration, whereas after oral administration a moderate decrease of prolactin serum levels was seen. The latter effect is probably due to the formation of active metabolites. CK 204-933 exhibits also a high affinity to [3H]prazosin binding sites and antagonises serotonin-mediated stimulation of adenylate cyclase in rat hippocampus. On the other hand, CK 204-933 has no effect of only very weak effects on noradrenaline and serotonin release from rat cerebral cortex slices, which is consistent with its weak effects on noradrenaline- and serotonin-turnover in rat brain. Based on these properties it is suggested that CK 204-933 could be of therapeutic value in brain diseases associated with disturbances of monoaminergic neurotransmission.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01244340
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    [3H]Ketanserin labels 5-HT2 receptors and α1-adrenoceptors in human and pig brain membranes (1987)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 335 (1987), S. 226-230 
    Details
    ISSN: 1432-1912
    Keywords: [3H]Ketanserin ; 5-HT2 receptors ; [125I]BE 2254 ; α1-Adrenoceptors ; Human and pig brain cortex
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1) The binding characteristics of [3H]ketanserin (a reported selective radioligand for serotonin 5-HT2 receptors) and [125I]BE 2254 (which labels selectively α1-adrenoceptors) were characterized in brain frontal cortex membranes of pig and man. 2) Saturation experiments indicated that both radioligands label apparently a homogeneous class of binding sites in human and pig fontal cortex membranes. 3) Competition experiments with [125I]BE 2254 using 17 agonists and antagonists showed monophasic and steep curves in human and pig frontal cortex membranes. The pharmacological profile of these sites is typical of α1-adrenoceptors. 4) In competition experiments with [3H]ketanserin, most of the tested compounds displayed shallow or biphasic curves. In particular, α1-adrenoceptor-selective antagonists (prazosin, WB 4101, BE 2254...) displaced with nanomolar affinity about 15 and 40% of the specific [3H]ketanserin binding in human and pig frontal cortex membranes, respectively. 5) The minor component of [3H]ketanserin binding correlated highly significantly with [125I]BE 2254 binding in both membrane preparations. 6) The major component of [3H]ketanserin binding to pig and human frontal cortex membranes correlated significantly with [3H]ketanserin binding in rat brain cortex membranes (which is essentially to 5-HT2 receptors). 7) The present data demonstrate that [3H]ketanserin in nanomolar concentrations binds significantly to α1-adrenoceptors in human and pig frontal cortex membranes; this suggests a rather limited degree of selectivity of ketanserin for 5-HT2 receptors in pig and human tissues.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00172788
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  • 4
    Electronic Resource
    Electronic Resource
    Die Struktur von Panepoxydon und verwandten Pilzmetaboliten (1970)
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 53 (1970), S. 1577-1597 
    Details
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: The structure of panepoxydone (1) and some related products, produced by two species of Panus (basidiomycetes), are proposed on the basis of chemical transformations and physical measurements.The absolute configurations of the main products are deduced by the interpretation of CD. studies and compared with those of the structurally related compounds epoxydone (10), terreic acid (11) and terremutin (12).
    Additional Material: 6 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/hlca.19700530704
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    Paper (German National Licenses)
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