3-Piperidynemethyl-5-chlorobenzoxazolinone-2 (PMB). Pharmacological estimation of the central action.
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Biomedical subjects
Publications and source records attributed to K Kolasa.
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Infant feeding practices and beliefs of 54 women in one rural community in the Sierra of Ecuador are described. Breastfeeding was nearly universal, with a mean duration of 16.9 months: males were weaned gradually, which was significantly different from the sudden weaning of females. Infants' diets were supplemented at a mean 9.7 months; first food included soup, meat broth, oats, and grains. Males' diets were supplemented significantly earlier than females. Mothers reported 16 months as the best weaning age. The best age to begin supplementing breast or bottle was 8.8 months. Milk, soup, meat, oats, "all foods," and vitamins were believed to help produce breastmilk. Most mothers said they would give a bottle if they were unable to produce breastmilk.
Buspirone, a novel psychotropic anxioselective agent, produced a dose-dependent decrease in the level of acetylcholine in the striatum of the rat. The maximum effect of about 25-30% was produced at the dose of 20 mg kg-1. A smaller decrease of 10% was also found in the n. accumbens-olfactory tubercle while other brain regions were unaffected. The drug did not alter striatal choline acetyltransferase or acetylcholinesterase activities and was feeble in displacing [3H]dexetimide from its specific muscarinic binding sites. The effect of buspirone in lowering acetylcholine content was more marked and longer lasting in the striatum of female than male rats. Buspirone proved to be weak as a blocker of the dopamine receptor agonist, apomorphine, and it appears that only a small proportion of the decrease in striatal acetylcholine content can be attributed to the blockade of dopamine receptors. Rapid homologous tolerance to an acute challenge with buspirone on striatal acetylcholine was achieved within seven days of its chronic administration, and, unlike clozapine, a cross tolerance of buspirone to chronic haloperidol treatment was also observed. Other data indicating that the drug differed from haloperidol both qualitatively and quantitatively on dopaminergic neurochemical parameters, and the fact that it is not cataleptogenic, suggest that buspirone cannot be considered a typical neuroleptic agent. The possibility that buspirone may act as an agonist at certain presynaptic dopamine receptors, which could translate into a fall in striatal acetylcholine content, is discussed.
Prostacyclin (PGI2) injected ivc in doses of 25 and 100 micrograms/rat increased body temperature, decreased spontaneous locomotor activity and amphetamine-induced locomotor hyperactivity in Wistar rats, in a dose of 100 micrograms inhibited apomorphine-induced stereotypy and potentiated haloperidol-induced catalepsy. PGI2 in both doses decreased noradrenaline level, in a dose of 100 micrograms it increased the cerebral level of dopamine but did not influence the utilization of these amines in the rat brain. PGI2 in a dose of 100 micrograms also increased the concentration of serotonin, but did not change the cerebral 5-hydroxyindoloacetic acid concentration.
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Fifty-nine elderly women interviewed about their food behavior, health, and laxation showed mean dietary fiber (DF) intakes of 14 gm. per day (range 3 to 34 gm. per day). DF intakes were lower for those in poor health and those with a tendency to constipation who took laxatives than for those who did not take laxatives or had no tendency to constipation. Factors not related to DF intake included age, participation in a meal program, living arrangements, understanding of fiber, and functional health. Cooked vegetables and bread added most to DF intakes.
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Out of 12 oximes and amidoximes (3 of which were new to the literature) the following showed a distinct antilethal effect in DFP poisoning: RA14 (1-methylbenzimidazole-2-aldoxime methiodide), RA14 (pyridine-4-aldoxime dodecyl bromide), and RA24 (pyridine-2-aldoxime dodecyl bromide). These compounds also reactivated acetylcholinesterase (AChE) in vitro, but had no effect on this enzyme in vivo. Moreover, addition of the dodecyl chain to pyridinealdoxtimes, or in a less degree replacement of the pyridine ring with benzimidazole in aldoximes, distinctly increased acute toxicity and lipophilicity when compared with the parent pyridine compounds, along with protective action in DFP poisoning.
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An immunoblotting method using prefrontal cortical and hippocampal membranes from control and Alzheimer disease postmortem brains was employed to detect three subtypes of Galphao protein. In the membranes from control subjects, the density of Galphao1 in hippocampus and cortex was the highest, whereas the density of Galphao2 was the lowest and that of Galphao3 was intermediate. In the Alzheimer disease membranes from hippocampus, the density of total Galphao and all three subtype forms was not changed significantly when compared with control values. There were statistically significant alterations in Galphao in cortical membranes from Alzheimer disease when compared with controls. The density of Galphao1 was decreased by approximately 85%, density of Galphao3 was decreased by approximately 95%, and total Galphao density was decreased by approximately 84% of control value. However, Galphao2 density was decreased by approximately 44% but was found not to be statistically different from controls.
Propranolol (100mug) ivc together with phentolamine (60 mug) decreased spontaneous locomotor activity and weakened post-nialamide locomotor activity in rat. When applied separately in the above doses, neither of the two compounds had this action. Depression of amphetamine-induced locomotor activity was observed after propranolol (250 mug) together with phetolamine (60 mug). Phentolamine alone, had hypothermic action but when applied together with propranolol, it increased after 4 hrs body temperature. The tested compounds prolonged hexobarbital-induced sleeping time but did not affect noradrenaline or dopamine levels in rat's brain.
Methionine given ivc or ip to rats and ic to mice acts only slightly on the central nervous system of these animals; it has either stimulating or inhibiting action, depending on the test applied.
Pharmacological studies on the central action of novel benzylidene-imidazothiazolone derivatives were carried out on mice and rats. The highest activity showed two compounds: a chloro- and a methoxy- derivative. They produced analgesic, anticonvulsant, anti-anxiety and "antidepressant" effects in mice.
Newly synthesized derivatives of 1-diphenylacetamide-2-butanol were investigated pharmacologically for their central properties in mice and rats. The most active were 2 compounds: racemic (RS) and enantiomer S (+) form of N-diphenylacetamide-2-butanol which produced hypothermia in normothermic mice, showed anxiolytic action in the four-plate test and reversed reserpine-induced hypothermia.