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  • 1
    Electronic Resource
    Electronic Resource
    Nonsteroidal antiinflammatory agents. 2. Synthesis and biological activity of 2-chloroindolecarboxylic acids (1977)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 20 (1977), S. 1344-1346 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00220a023
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Pattern recognition applications in the biometrical science (1968)
    Springer
    Quality & quantity 2 (1968), S. 135-148 
    Details
    ISSN: 1573-7845
    Source: Springer Online Journal Archives 1860-2000
    Topics: Sociology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00234213
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Synergistic blockade of some dopamine-mediated behaviours by (−)-sulpiride and SCH 23390 in the rat (1989)
    Springer
    Psychopharmacology 98 (1989), S. 342-346 
    Details
    ISSN: 1432-2072
    Keywords: (−)-Sulpiride ; SCH 23390 ; Exploratory activity ; Apomorphine-induced stereotypy ; LY 171555-induced hypermotility
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Several studies have indicated that the D2 dopamine receptors mediate the antidopaminergic activity of the neuroleptics; nevertheless, the selective blocker (−)-sulpiride weakly inhibits dopamine-mediated behaviour. The present study investigated whether the concomitant injection of doses of the D1 antagonist SCH 23390, which by themselves are without effect, would enable (−)-sulpiride to express fully neuroleptic activity in the rat. The benzamide YM 09151-2 that strongly inhibits dopamine-mediated behaviour was also studied. Rats receiving different doses of (−)-sulpiride, YM 09151-2 and SCH 23390 given alone or in combination were tested for exploratory activity, apomorphine-induced stereotyped behaviour and hyperactivity elicited by the D2 agonist LY 171555. When given alone, (−)-sulpiride (10, 20 and 40 mg/kg IP) had no effect on exploratory activity and stereotypy. When (−)-sulpiride was administered in combination with an ineffective dose of SCH 23390 (5 μg/kg) both responses were significantly inhibited. The combined administration of subthreshold doses of (−)-sulpiride (2.5 mg/kg) and SCH 23390 (2.5 μg/kg) significantly inhibited hypermotility induced by LY 171555. Moreover, the combined administration of ineffective doses of YM 09151-2 with subthreshold doses of SCH 23390 strongly inhibited all the behavioural responses. The results indicate that SCH 23390 allowed (−)-sulpiride to exhibit a wider spectrum of neuroleptic activity and potentiated the antidopaminergic activity of YM 09151-2.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00451685
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Changes in behavioural responses to the combined administration of D1 and D2 dopamine agonists in normosensitive and D1 supersensitive rats (1988)
    Springer
    Psychopharmacology 95 (1988), S. 381-385 
    Details
    ISSN: 1432-2072
    Keywords: LY 171555 ; SKF 38393 ; Combined D1 and D2 stimulation ; SCH 23390 ; D1 supersensitivity ; Locomotor activity ; Grooming ; Stereotyped behaviour ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The selective D1 receptor stimulant SKF 38393 dose-dependently increased grooming time in rats without affecting locomotor activity or eliciting stereotyped behaviour. The selective D2 receptor agonist LY 171555 induced a dose-dependent increase in rat motility, a marked decrease in grooming time and a low occurrence of stereotyped behaviour. Concurrent administration of the two selective agonists induced high-degree stereotyped responses and reductions in locomotor and grooming behaviours. Rats withdrawn from repeated treatment with the selective D1 receptor blocker SCH 23390 (0.05 mg/kg twice daily for 21 days; 7 days of washout) did not exhibit any change of locomotor and grooming responses to threshold doses of LY 171555 and SKF 38393 given alone or in combination. On the contrary, a significantly greater occurrence of high-degree stereotyped responses to the combination of the two selective agonists was observed. The data support the view that D1 and D2 receptors have a cooperative role in the generation of stereotypies and suggest that D1 receptor supersensitivity needs D2 stimulation to be revealed.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00181952
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  • 5
    Electronic Resource
    Electronic Resource
    Effect of chronic treatment with dizocilpine (MK-801) on the behavioral response to dopamine receptor agonists in the rat (1992)
    Springer
    Psychopharmacology 107 (1992), S. 591-594 
    Details
    ISSN: 1432-2072
    Keywords: MK-801 induced hypermotility ; Repeated treatment ; SCH 23390 ; YM 09151 ; 2 ; LY 171555-induced hyperactivity ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The D2 or D1 dopamine receptor blockers (−)-sulpiride or SCH 23390 antagonized, in a dose dependent manner, the hypermotility induced by the N-methyl-d-aspartate (NMDA) receptor antagonist, MK-801 (0.25 mg/kg IP). MK-801 induced hyperactivity was not detected when rats were observed on days 7, 14 or 21 of 21 daily injections of MK-801. This lack of hyperactivity was also noted 5 days after the last administration of the repeated treatment with MK-801. The hypermotility induced by the D2 dopamine receptor agonist LY 171555 (0.3 mg/kg IP) was reduced 5 days following repeated treatment (21 days) with MK-801, while no change in the behavioral responses to the selective D1 agonist, SKF 38393, or the mixed D1/D2 agent apomorphine was detected. The results, although suggesting the involvement of dopaminergic pathways in the behavioral effect of MK-801, are conflicting with regard to the underlying mechanisms and to the adaptive changes of dopaminergic system following repeated NMDA receptor blockade.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02245275
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  • 6
    Electronic Resource
    Electronic Resource
    Behavioral differentiation between pharmacokinetic and pharmacodynamic components of the interaction of antidepressants or neuroleptics with methamphetamine (1986)
    Springer
    Psychopharmacology 90 (1986), S. 18-23 
    Details
    ISSN: 1432-2072
    Keywords: Antidepressants ; Neuroleptics ; Methamphetamine potentiation test ; Pharmacodynamic interaction ; Pharmacokinetic interaction ; Rat motility
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This study proposes a method capable of separating the pharmacodynamic from the pharmacokinetic component in the methamphetamine (MA) hyperactivity potentiation induced by antidepressants. Several antidepressants and neuroleptics, other centrally-acting drugs and the inhibitor of hepatic drug metabolism SKF 525-A were studied. The motility counts taken between 10 and 20 min after MA injection were considered as an index of pharmacodynamic interaction and the whole duration of the hyperactivity syndrome as an index of pharmacokinetic interaction. The duration of MA effect was prolonged by some of the drugs studied and left unchanged by the others regardless of their clinical classification. On the contrary, our evaluation of the intensity of MA effect produced a sharp differentiation between classical neuroleptics and typical antidepressants: the former antagonized and the latter potentiated MA peak intensity. Only the D-2 blocking neuroleptics sulpiride and tiapride potentiated MA intensity. Regarding the specificity of our model, none of the compounds known to be devoid of clinical antidepressant or antipsychotic activity interacted with MA in such a way as to be included in either category. As to the sensitivity of the test, two “false negatives” were obtained: the neuroleptic clozapine and the antidepressant mianserin. Such exceptions were discussed taking into account their peculiar mechanisms of action.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00172865
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  • 7
    Electronic Resource
    Electronic Resource
    Antidepressant versus neuroleptic activities of sulpiride isomers on four animal models of depression (1984)
    Springer
    Psychopharmacology 83 (1984), S. 28-33 
    Details
    ISSN: 1432-2072
    Keywords: Sulpiride isomers ; Imipramine ; Desipramine ; Haloperidol ; Apomorphine ; Hypomotility ; Hypothermia ; Behavioural despair ; Learned helplessness ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The atypical neuroleptic sulpiride is also prescribed for depression because of its activating effect. However, such an effect does not necessarily imply an action identical to that of classical antidepressants, and a laboratory comparison of the neuroleptic and antidepressant activities of sulpiride may contribute to a better definition of its psychotherapeutic profile. Sulpiride isomers were studied in the rat in four behavioural models of depression which are thought to be influenced by neuroleptics in different ways. Desipramine (imipramine) and haloperidol were employed in each test as a standard antidepressant and neuroleptic, respectively. The four tests were: 1) prevention of apomorphine-induced sedation: 2) antagonism of apomorphine-induced hypothermia; 3) behavioural despair (swim test); 4) learned helplessness (FR2 lever pressing escape). Desipramine ameliorated behaviour in all tests; haloperidol ameliorated the response to test 1, influenced that to test 2 in a neuroleptic-like way and worsened the responses to tests 3 and 4.(-)-Sulpiride worked in a similar way to haloperidol in all tests.(+)-Sulpiride significantly and dose-dependently ameliorated the responses to test 3 and was inactive in the others. No conclusion was drawn from test 1 owing to its lack of specificity; the results of the remaining tests indicated a neuroleptic profile of (-)-sulpiride and suggested a potential “antidepressant” activity of (+)-sulpiride which merits further investigation.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00427417
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  • 8
    Electronic Resource
    Electronic Resource
    Repeated treatment with (-)-sulpiride plus a low dose of SCH 23390 displays wider neuroleptic activity without inducing dopaminergic supersensitivity (1990)
    Springer
    Psychopharmacology 100 (1990), S. 560-562 
    Details
    ISSN: 1432-2072
    Keywords: (-)-Sulpiride ; SCH 23390 ; Repeated treatment ; Apomorphine-induced stereotypy ; Dopaminergic supersensitivity ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Combined treatment with (-)-sulpiride plus a low dose of the D1 receptor antagonist SCH 23390, unlike (-)-sulpiride given alone, blocked rat striatal dopaminergic transmission. Five days after the withdrawal of 21-day repeated administration of the combined treatment, no increase in apomorphine-induced stereotyped behaviour was observed. The results suggest that the combination of a D2 blocker and a low dose of a D1 blocker produces a wider spectrum of neuroleptic activity without an overt risk of inducing dopaminergic behavioural supersensitivity.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02244013
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  • 9
    Electronic Resource
    Electronic Resource
    Involvement of different dopamine receptors in rat diphasic motility response to apomorphine (1986)
    Springer
    Psychopharmacology 89 (1986), S. 265-268 
    Details
    ISSN: 1432-2072
    Keywords: DA receptor subtypes ; Apomorphine ; Motility ; Neuroleptics ; Rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract A critical dose of apomorphine (300 μg/kg SC) given immediately before placing rats into a novel environment produced a diphasic motility response (initial sedation followed by enhanced locomotion). Various neuroleptics having different clinical and/or pharmacological profiles were studied by using such a model. (−)-Sulpiride and sultopride preferentially antagonized apomorphine inhibition; haloperidol and tiapride antagonized both phases of apomorphine response at similar doses; chlorpromazine, fluphenazine, thioridazine, metoclopramide and SCH 23390 preferentially antagonized apomorphine stimulation. The results are discussed in terms of the dopamine receptor subtypes involved in the two phases of apomorphine effect. Apomorphine stimulation can be antagonized by D-1 as well as D-2 receptor blockade. A higher affinity for D-2 receptors seems a necessary requisite for the antagonism of apomorphine inhibition; moreover, the ability of neuroleptics to antagonize apomorphine inhibition seems to depend on the ratio of their presynaptic versus postsynaptic D-2 activity.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00174356
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