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  • Haloperidol  (4)
  • Dopamine receptors  (2)
  • Polymer and Materials Science  (2)
Materialart
Erscheinungszeitraum
  • 1
    Digitale Medien
    Digitale Medien
    Springer
    Psychopharmacology 73 (1981), S. 219-222 
    ISSN: 1432-2072
    Schlagwort(e): Aging ; Catalepsy ; Haloperidol ; Maturation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Male Sprague-Dawley rats were evaluated between ages 18 and 825 days for responses to doses of haloperidol (0 and 0.05–10 mg/kg, IP). Catalepsy, ptosis, and inhibition of general motor activity showed steady decreases in sensitivity to the drug with age during the first 1.5 years of maturation, while rats older than 1.5 years had strikingly increased sensitivity to the activity-inhibiting and cataleptic effects of the drug. The efficacy of haloperidol on all tests in 110-day old rats was indistinguishable whether food was available continuously, or restricted to reduce body weight by 55%, indicating that the effects of maturation are due to aging and not to increasing body weight. The effects may be due to altered drug metabolism or altered sensitivity of the central nervous system to neuroleptic agents. Clinical impressions too, indicate that immature and elderly patients are more sensitive to these and other psychotropic drugs than are young adults.
    Materialart: Digitale Medien
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    Psychopharmacology 77 (1982), S. 150-155 
    ISSN: 1432-2072
    Schlagwort(e): Catalepsy ; Chronopharmacology ; Circadian rhythms ; Haloperidol
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Circadian changes in behavioral responses to haloperidol were evaluated in rats under normal and altered lighting cycles. There was a 5.5-fold change in ED50 between the maximum (4 PM) and minimum (4 AM) cataleptic response to the drug under normal lighting (lights on 7 AM-7 PM). The rhythm was present whether the same rats were tested repeatedly, or fresh rats were used at each time to avoid drug effects which persist for at least several days. Under normal lighting, the maximum cataleptic effect of haloperidol corresponded closely to the light-phase minimum of spontaneous motor activity in untreated rats. Measures of sedation (ptosis and motor inhibition) induced by haloperidol yielded small circadian rhythms under normal lighting and were highly dependent on the baseline level of arousal. A month of constant light or dark, or reversed dark-light cycles had small effects on the sedative actions of haloperidol, although inhibition of locomotion tended to phase-shift with general arousal; these changes did not alter the catalepsy rhythm. While the circadian rhythm of spontaneous activity underwent a complete reversal within 1 month (t 1/2=17 days) of reversed lighting cycles, the catalepsy rhythm changed very gradually (t 1/2=82 days) and required nearly 6 months for complete reversal. Thus, catalepsy is a robust endogenously regulated circadian response that is only slowly influenced by altered lighting conditions which dissociate this rhythm of neuroleptic response from that of spontaneous general arousal. Endogenous neurobiologic and pharmacokinetic factors may contribute to circadian changes in neuroleptic responses.
    Materialart: Digitale Medien
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  • 3
    ISSN: 1432-2072
    Schlagwort(e): Apomorphine ; Butyrophenones ; Dopamine receptors ; Duration of drug action ; Droperidol ; Haloperidol ; Neuroleptics ; Stereotypy
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Rats were treated once with doses of haloperidol or of droperidol below and above the acute ID50 vs the dopamine agonist apomorphine; they were later challenged with an acute dose of apomorphine (0.3mg/kg, SC) and rated for stereotyped behavioral responses. The two neuroleptics were similar in acute anti-apomorphine potency (ID50=0.12 and 0.18mg/kg for haloperidol and droperidol, respectively). The antidopaminergic effects of droperidol persisted for nearly 1 week and those of haloperidol lasted for 20–40 days, depending on the dose given. The computed half-time of disappearance of their antidopaminergic effects was 7.6±1.0 days and 0.59±0.17 days for haloperidol and droperidol, respectively, following a dose of 0.3 mg/kg, and these indices of duration of action did not vary significantly at doses between 0.1 and 1.0mg/kg. Haloperidol reduced the acute entry of 3H-apomorphine into brain by 21.5% 1 week later. Treatment with apomorphine alone just prior to haloperidol (both at 0.3 mg/kg) prevented the prolonged antidopaminergic effects of the neuroleptic evaluated 1 week later. These results indicate that some neuroleptics may have very prolonged activity or retention in tissue at sites of action, even after moderate, single doses. Caution is recommended in the interpretation of studies which assume “neuroleptic-free” conditions of subjects previously exposed to a neuroleptic agent.
    Materialart: Digitale Medien
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  • 4
    ISSN: 1432-2072
    Schlagwort(e): Haloperidol ; Brain levels ; Bromperidol ; Chlorpromazine ; Fluphenazine
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract After a single dose of the butyrophenone neuroleptic haloperidol, behavioral effects and detectable drug levels in rat brain can last for several weeks. To determine if such persistence is a general property of neuroleptics, we compared drug levels and effects after IP administration of two butyrophenones (haloperidol and bromperidol), a high potency (fluphenazine) and a low potency (chlorpromazine) phenothiazine. Drug levels in brain tissue were measured by high pressure liquid chromatography and behavioral effects monitored as inhibition of apomorphine-induced stereotypy. Estimated near terminal elimination half-lives (t1/2) from brain for acutely administered chlorpromazine (20 mg/kg) and fluphenazine (1 mg/kg) were 0.41 and 0.62 days, respectively, and neither drug was detectable after 4 days. Fluphenazine given daily for 5 days showed an only slightly slower elimination (t1/2=1.1 days). In contrast, near-terminal elimination half-lives from brain for haloperidol and bromperidol (both at 1 mg/kg, IP) were much longer (6.6 and 5.8 days, respectively), and each was detectable for 21 days after dosing. Inhibition of apomorphine-induced stereotypy correlated highly (r=0.95) with brain levels of haloperidol. For fluphenazine, given once or repeatedly, early inhibition was replaced within 1 week by supersensitivity to apomorphine which persisted for up to 3 weeks. These findings, indicating marked differences in clearance and recovery times after dosing with butyrophenones and phenothiazines, have clear implications for studies of the effects of neuroleptic drugs in rats. While there are limits to the extrapolation of these findings to other species, our results and those from studies in human subjects suggest similarly persistent drug levels and effects may be seen when patients are withdrawn from neuroleptic drugs.
    Materialart: Digitale Medien
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  • 5
    ISSN: 1432-2072
    Schlagwort(e): R(-) and S(+) apomorphine ; Dopamine receptors ; Locomotion ; Limbic system ; R(-) and S(+) N-propylnorapomorphine
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract The optical isomers of apomorphine (APO) and N-n-propylnorapomorphine (NPA) were evaluated behaviorally in the rat. Both R(-) isomers induced motor-excitatory effects and strong stereotyped sniffing, licking, and gnawing, as has been reported previously. The S(+) isomers selectively inhibited locomotor activity and did not induce stereotypy or catalepsy. These actions of the S(+) aporphines were selective against locomotor activity stimulated by low doses of R(-) isomers. (+)NPA (ID50=0.2 mg/kg) was 20 times more potent than (+)APO (ID50=4 mg/kg) in antagonizing the locomotor arousal-inducing effects of (-)APO (at ED50=0.3 mg/kg). (+)NPA also inhibited spontaneous locomotor activity much more potently (ID50=3.0 mg/kg) than did (+)APO (ID50〉50 mg/kg). Neither S(+) aporphine had a significant effect against stereotypy induced by the R(-) isomers, even at high doses (up to 30 mg/kg). Inhibition of the effects of (-)APO by (+)NPA appeared not to be due to altered uptake of (-)APO into brain. These results suggest that S(+)NPA or its congeners and analogs may have selective antidopaminergic actions in limbic rather than striatal areas of mammalian brain.
    Materialart: Digitale Medien
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  • 6
    Digitale Medien
    Digitale Medien
    New York, NY [u.a.] : Wiley-Blackwell
    Journal of Applied Polymer Science 8 (1964), S. 1007-1014 
    ISSN: 0021-8995
    Schlagwort(e): Chemistry ; Polymer and Materials Science
    Quelle: Wiley InterScience Backfile Collection 1832-2000
    Thema: Chemie und Pharmazie , Maschinenbau , Physik
    Notizen: An easily constructed, cheap and compact stress relaxometer has been designed for aging tests on elastomers. Its construction is such as to allow it to fit inside a multicavity metal block oven commonly used for aging tests. The instrument works well on continuous and intermittent cycles and its action is illustrated by a brief examination of the stress relaxation properties of vulcanized nitrile rubber/PVC blends. The presence of PVC increases the initial (physical) relaxation both at high and normal temperatures under conditions of continuous stress. The rate of relaxation thereafter increase with increase in PVC content. Under intermittent conditions the PVC seems to encourage a crosslinking reaction, as does carbon black.
    Zusätzliches Material: 5 Ill.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 7
    Digitale Medien
    Digitale Medien
    Hoboken, NJ : Wiley-Blackwell
    Journal of Biomedical Materials Research 10 (1976), S. 583-594 
    ISSN: 0021-9304
    Schlagwort(e): Chemistry ; Polymer and Materials Science
    Quelle: Wiley InterScience Backfile Collection 1832-2000
    Thema: Medizin , Technik allgemein
    Notizen: Polyacrylonitrile fabric (Orlon) may be oxidized by heating in air, when it becomes black and carbonized. During the heat treatment, the fibers shrink; this shrinkage allows components such as diaphrams to be shaped around molds. Oxidation reduces the tensile strength by about 25% and also reduces the stiffness of the material.The oxidized Orlon was screened in tissue culture for possible cytotoxic effects. Finding none, patches of the material were sutured into the right atrium of dogs and examined after 48 hr. Because of encouraging results, 10 atrial patches, consisting of Dacron velour and oxidized Orlon side-by-side, were implanted into the right atrium of dogs. Five patches were backed with Silastic to render them impervious, and five with segmented polyurethane. The atrial patches were examined after 48 hr, and in all instances the oxidized Orlon part of the patch was coated with a thinner and smoother fibrin layer than was the Dacron velour half.A left ventricular bypass pump was fabricated from oxidized Orlon and spraycoated on the nonblood surface with segmented polyurethane. After 48 hr implantation in the chest cavity of a calf, pumping without systemic anticoagulation, the pump was found covered by a thin, smooth, firmly attached layer of fibrin.
    Zusätzliches Material: 10 Ill.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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