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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
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Bioorganic & Medicinal Chemistry Letters 2 (1992), S. 815-820 
    ISSN: 0960-894X
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1435-1463
    Keywords: SDZ PSD 958 ; D1 receptor antagonist ; catalepsy ; rearing ; stereotypy ; locomotion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary SDZ PSD 958, a novel benzo[g]quinoxaline derivative exhibits the properties of a potent orally active selective D1 receptor antagonist. It has high affinity for D1-like receptors (D1, D5; pKi=9.7–9.8) labelled by [3H]SCH23390 and is at least 400 fold less active at D2-like receptors (i.e. D2, D4) labelled by [3H]spiperone. Effects in functional tests are consistent with d1 receptor antagonist properties. SDZ PSD 958 inhibited apomorphine-induced rearing in mice and prevented prolongation of novelty-induced locomotion in rats elicited by the selective D1 receptor agonist CY 208-243. By contrast, SDZ PSD 958 did not induce catalepsy and only weakly inhibited apomorphine-induced stereotyped gnawing in rats. This suggests that SDZ PSD 958 preferentially inhibits responses mediated by dopamine systems innervating the limbic system.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1435-1463
    Keywords: SDZ GLC 756 ; octahydrobenzo[g]quinoline ; dopamine D1 receptor ; dopamine D2 receptor ; prolactin ; circling (rats) rearing (mice)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary SDZ GLC-756, a novel octahydrobenzo[g]quinoline derivative, is equipotent in displacing [3H]SCH23390 from dopamine D1 receptors and [3H]205–501 from dopamine D2 receptor binding sites. It blocks dopamine sensitive adenylate cyclase with the same potency as SCH23390, indicating antagonist properties at dopamine D1 receptors. On the other hand, SDZ GLC 756 inhibits electrically evoked acetylcholine release from rat striatal slices with the same potency as the selective dopamine D2 receptor agonist bromocriptine. This effect is blocked by spiperone suggesting that it is mediated by dopamine D2 receptor activation. The opposing action of SDZ GLC 756 on dopamine D1 and D2 receptors is also evident in vivo. SDZ GLC 756, like SCH23390, blocks apomorphine-induced rearing in mice. On the other hand, it inhibits prolactin secretion and produces circling in unilateral 6-OHDA-lesioned rats, which is compatible with stimulant properties at dopamine D2 receptors. This drug might be a new tool to study linkage between dopamine D1 and D2 receptors.
    Type of Medium: Electronic Resource
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  • 5
    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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  • 6
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: UV. -irradiation of the 11-oxo-δ14-5α-pregnene derivate 16 gives rise to a novel photochemical reaction. The preferential attack of the photochemically excited carbonyl on CH-8 furnishes the tertiary cyclopropanol compound 18 in high yield.
    Type of Medium: Electronic Resource
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