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  • 1
    Electronic Resource
    Electronic Resource
    Palo Alto, Calif. : Annual Reviews
    Annual Review of Pharmacology 23 (1983), S. 279-301 
    ISSN: 0362-1642
    Source: Annual Reviews Electronic Back Volume Collection 1932-2001ff
    Topics: Medicine , Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] THIS article reports the discovery of tetramisole (R 8299 (I)), a new, potent broad spectrum anthelmintic, which is at present undergoing large-scale clinical trials in several countries. In the course of our routine screening programme for anthelmintic activity the aminothiazol derivative (II) ...
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 35 (1979), S. 1538-1539 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary The construction and use of a specially designed electrode to measure gastric pH in the conscious rat is described. Measurement of gastric hydrogen ion activity with this device is rapid and reproducible in starved rats. A doserelated increase of gastric pH was obtained after s.c. injection of the anticholinergic isopropamide.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Levocabastine, selected from a series of cyclohexylpiperidine derivatives protects rats from compound 48/80-induced anaphylactic shock for at least 16 h at the oral dose of 0.0015 mg/kg. At the same dose histamine skin reactions and at slightly higher doses passive cutaneous anaphylactic reactions are inhibited. Blockade of passive cutaneous anaphylactic reactions is obtained with levocabastine, despite absence of peripheral serotonin antagonism and any other known non-specific action that may facilitate inhibition of passive anaphylaxis. In dogs allergic reactions are inhibited at oral doses 40 times lower than ketotifen. In guinea-pigs orally and topically administered levocabastine are remarkably effective against allergic conjunctivitis.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 205 (1965), S. 1018-1019 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Experiments with goldfish have been carried out in 101 aerated aquaria kept at 19 ± 2 C. Concentrations of R7464: 1/1.6, 1/4, 1, 4, 16 and 64 p.p.m., were tested at various immersion times, 1/64, 1/16, 1/4, 1, 4 and 16 h. Recovery from anaesthesia was effected by transferring the fish into ...
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1432-2072
    Keywords: Risperidone ; Haloperidol ; Antipsychotics ; Behaviour ; Activity meter ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Risperidone, a new antipsychotic agent, was studied for its effects on spontaneous motor activity in rats in comparison with haloperidol. Motor activity was recorded via the optical scanning technique (horizontal and vertical activity) and via a recently developed technique based on the piezo-electric principle which, in contrast to optical scanning, is very sensitive to small, stationary movements (piezo activity). Risperidone and haloperidol at low doses depressed both vertical activity (ED50s: 0.062 and 0.038 mg/kg, respectively) and horizontal activity (0.18 and 0.060 mg/kg, respectively). With increase of dose, motor activity decline was significantly faster with haloperidol than with risperidone. Moreover, haloperidol also rapidly depressed piezo activity (ED50: 0.085 mg/kg) whereas risperidone depressed this component of motor behaviour at much higher doses only (ED50: 2.80 mg/kg). Visual inspection did not reveal abnormal behavioural movements following the test compounds. Risperidone, therefore, preserves normal small movements over a much larger dose interval than haloperidol; this effect may be related to its relatively low cataleptogenic activity and potentially also to a reduced EPS liability. The present results further confirm that the piezo technique may complement the optical scanning method, and thereby enhance the information on the extent that test compounds modify behaviour.
    Type of Medium: Electronic Resource
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  • 7
    ISSN: 1432-2072
    Keywords: Motor activity ; Locomotion ; Behaviour ; Methods ; Haloperidol ; Apomorphine ; Amphetamine ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Spontaneous and drug-induced (haloperidol, apomorphine, and amphetamine) motor activity of rats was measured simultaneously via two distinct and independent methods: the classical optical scanning technique and a new procedure based on the piezo-electric principle. The latter procedure measured animal-induced mechanical vibrations of a flexible cage floor which were transduced into electric signals via piezo-electricity. The piezo method appeared to be relatively more sensitive in recording the small, stereotyped motor movements induced by apomorpine (0.63–≧10 mg/kg) and high doses of amphetamine (2.5–≧20 mg/kg). The optical scanning technique, on the other hand, was more sensitive in recording horizontal displacements across the cage such as induced by low doses of amphetamine (0.31–2.5 mg/kg). Both methods showed comparable sensitivity in recording the depression of behaviour induced by haloperidol (0.04–≧1.25 mg/kg) or low doses of apomorphine (0.04–0.16 mg/kg). The piezo method may complement the optical scanning procedure, and thereby enhance the information on the extent that test compounds modify animal behaviour.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1432-2072
    Keywords: Risperidone ; Antipsychotics ; 5-HT2 antagonism ; D2 antagonism ; Pharmacology ; Receptor binding ; Biochemistry ; Review
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract This review reports on the pharmacodynamics of the new antipsychotic risperidone. The primary action of risperidone is serotonin 5-HT2 receptor blockade as shown by displacement of radioligand binding (Ki: 0.16 nM), activity on isolated tissues (EC50:0.5 nM), and antagonism of peripherally (ED50: 0.0011 mg/kg) and centrally (ED50:0.014 mg/kg) acting 5-HT2 receptor agonists in rats. Risperidone is at least as potent as the specific 5-HT2 receptor antagonist ritanserin in these tests. Risperidone is also a potent dopamine D2 receptor antagonist as indicated by displacement of radioligand binding (Ki: 1.4 nM), activity in isolated striatal slices (IC50: 0.89 nM), and antagonism of peripherally (ED50: 0.0057 mg/kg in dogs) and centrally acting D2 receptor agonists (ED50: 0.056–0.15 mg/kg in rats). Risperidone shows all effects common to D2 antagonists, including enhancement of prolactin release. However, some central effects such as catalepsy and blockade of motor activity occur at high doses only. Risperidone is 4–10 times less potent than haloperidol as a central D2 antagonist in rats and it differs from haloperidol by the following characteristics: predominant 5-HT2 antagonism; LSD antagonism; effects on sleep; smooth dose-response curves for D2 antagonism; synergism of combined 5-HT2/D2 antagonism; pronounced effects on amphetamine-induced oxygen consumption; increased social interaction; and pronounced effects on dopamine (DA) turnover. Risperidone displays similar activity at pre- and postsynaptic D2 receptors and at D2 receptors from various rat brain regions. The binding affinity for D4 and D3 receptors is 5 and 9 times weaker, respectively, than for D2 receptors; interaction with D1 receptors occurs only at very high concentrations. The pharmacological profile of risperidone includes interaction with histamine H1 and α-adrenergic receptors but the compound is devoid of significant interaction with cholinergic and a variety of other types of receptors. Risperidone has excellent oral activity, a rapid onset, and a 24-h duration of action. Its major metabolite, 9-hydroxyrisperidone, closely mimics risperidone in pharmacodynamics. Risperidone can be characterized as a potent D2 antagonist with predominant 5HT2 antagonistic activity and optimal pharmacokinetic properties.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 16 (1969), S. 175-182 
    ISSN: 1432-2072
    Keywords: Neuroleptics ; Conditioning ; Extinction ; IRT's ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The effects of seven neuroleptic drugs on conditioned behaviour were studied in rats by means of a lever-press shock-avoidance procedure (shock-shock 20 sec; response-shock 20 sec) with alternate reinforcement and extinction periods. All seven drugs inhibited the lever-press response and the shock-avoidance rate; their order of potency was trifluperidol 〉 droperidol 〉 haloperidol 〉 pimozide 〉 fluanisone 〉 chlorpromazine 〉 pipamperone. For all seven drugs, the response rate during the extinction periods was a more sensitive indicator of drug effect than the response rate during the reinforcement periods. Analysis of the temporal distribution of the IRT's shows that IRT's of 0–5″ and of 6–15″ were more sensitive to drug effects than IRT's of 16–20″ and of 〉 20″. The introduction of extinction periods together with the analysis of IRT's rendered the Sidman avoidance procedure the most sensitive test available for the quantitative evaluation of the potency of neuroleptic drugs in rats. The qualitative differences between the neuroleptics studied were less pronounced. There is some indication, however, that specific neuroleptics (e.g. pimozide) inhibit the response rate to about the same extent during both reinforcement and extinction periods, while aspecific neuroleptics (e.g. pipamperone) are more active inhibitors of the responses during extinction than during the corresponding reinforcement periods.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 34 (1974), S. 265-274 
    ISSN: 1432-2072
    Keywords: Amphetamine ; Rats ; Self-Stimulation ; Medial Forebrain Bundle ; Monopolar Electrodes ; Various Stimulus Parameter Combinations
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects of various subcutaneous doses (0.16, 0.31, 0.63, 1.25 and 2.50 mg/kg) of amphetamine on self-stimulation in rats, with monopolar nichrome electrodes, implanted in the medial forebrain bundle at the level of the lateral hypothalamus, were studied. Six different stimulus parameter combinations (SPC), inducing different predictable response rates, were used. Response stimulation as well as response inhibition were measured at the same dose levels in the same rats and during the same experimental session. At each dose level of amphetamine response stimulation was more pronounced than response depression. The response depression was dose-related and the response stimulation reached a peak at 0.63 mg/kg. The response depression was directly related and the response stimulation inversely related to the control response rate, obtained with the different SPC's. It is assumed that amphetamine enhanced self-stimulation by lowering the threshold at the synaptic level and by increasing catecholamine release at neurons mediating motivational properties and reinforcement. Inhibition of the response rate at high doses of amphetamine can be attributed to non-specific motor stimulation interfering with performance efficiency.
    Type of Medium: Electronic Resource
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