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  • 1
    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
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  • 2
    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
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 35 (1979), S. 1677-1678 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Prolactin secretion inhibition and changes in striatal dopamine metabolism in rats were compared after the administration of 8a-amino-ergoline CH 29-717 and 2 derivates. CQ 32-084 was similar to but less potent than CH 29-717. while 32-085, the 1-methyl derivative, showed delayed dopaminomimetic effects.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 34 (1978), S. 1330-1332 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary In rats, CH 29-717 inhibits basal and physiologically or chemically stimulated prolactin secretion. It is more potent than the standard bromocriptine.
    Type of Medium: Electronic Resource
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