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  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 53 (1989), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: [3H]Zacopride displayed regional saturable specific binding to homogenates of human brain tissues, as defined by the inclusion of BRL43694 [endo-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-l-methylindazole-3-carboxamide] in the incubation media. Scatchard analysis of the saturation data obtained from amygdaloid and hippocampal tissues identified the binding as being of high affinity and to a homogeneous population of binding sites (KD= 2.64 ± 0.75 and 2.93 ± 0.41 nmol/L and Bmax= 55 ± 7 and 44 ± 9 fmol/ mg of protein in the amygdala and hippocampus, respectively). 5-Hydroxytryptamine3 (5-HT3) receptor agonists and antagonists competed for the [3H]zacopride binding site, competing with up to 40% of total binding with a similar rank order of affinity in both tissues; agents acting on various other neurotransmitter receptors failed to inhibit binding. Kinetic data revealed a fast association that was fully reversible (k+1= 6.61 × 105 and 7.65 × 105/mol/L/s and k-1= 3.68 × 10−3 and 3.45 × 10−3/s in the amygdala and hippocampus, respectively). It is concluded that [3H]zacopride selectively labels with high affinity 5-HT3 recognition sites in human amygdala and hippocampus and, if these binding domains represent 5-HT3 receptors, may provide the opportunity for 5-HT3 receptor antagonists to modify 5-HT function in the human brain
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 160 (1969), S. 0 
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 338 (1989), S. 762-763 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Release of [3H]acetylcholine from rat entorhinal cortex pre-loaded with [3H] choline was stimulated by potassium. Previous studies have shown that the tritium released is [3H]acetylcholine, and that the release is calcium-dependent13. 5-HT (2 p,M) or the selective 5-HT3 receptor agonist, ...
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 342 (1990), S. 17-21 
    ISSN: 1432-1912
    Keywords: 5-Hydroxytryptamine3 receptor recognition sites ; Ferret ; Brainstem ; Emesis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The distribution of [3H]zacopride (1.0 nM) to putative 5-HT3 receptor recognition sites in the ferret hindbrain was assessed using autoradiography. Specific binding (defined by the inclusion of granisetron, 1.0 μM) was heterogeneously distributed with highest density within the dorsal vagal complex (area postrema, nucleus tractus solitarius and dorsal motor nucleus of the vagus nerve). Lower densities were detected in the spinal trigeminal nerve complex whilst no other significant specific binding was detected ventral to the dorsal vagal complex. The location of 5-HT3 receptor recognition sites within the dorsal vagal complex may provide sites of action for zacopride and other 5-HT3 receptor antagonists to inhibit the emesis induced by cancer chemotherapeutic agents and x-radiation.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-1912
    Keywords: Sigma recognition sites ; Human cerebellum ; Rat cerebellum ; [3H]haloperidol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The radioligand binding characteristics of [3H]haloperidol (in the presence of spiperone, 25 nmolL−1) were investigated in rat and human cerebellar membranes. In both rat and human cerebellar membrane preparations saturation studies with [3H]haloperidol (non-specific binding defined by pentazocine, 10 μmolL−1) demonstrated high affinity saturable specific binding to a homogenous population of binding sites (rat, Bmax 6693 ± 1242 fmol mg−1 protein, pKD 8.33 ± 0.08; human, Bmax 2550 ± 437 fmol mg−1 protein, pKD 8.59 ± 0.11; mean ± SEM, n = 3–6). Competition studies employing a wide range of structurally diverse competing compounds displayed that the [3H]haloperidol binding site was pharmacologically similar in both preparations and comparable to sigma recognition sites previously identified in various tissues originating from different species. In addition, with reference to the potential subtypes of sigma recognition sites, the labelling of these sites by low nanomolar concentrations of [3H]haloperidol provides evidence that they belong to the sigma-1 recognition site subtype. The present findings suggest that the pharmacology of the rat and human cerebellar sigma recognition site are directly comparable and provides further supporting evidence towards the use of [3H]haloperidol radioligand binding studies in the rat to detect sigma receptor ligands with potential therapeutic activity.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 169 (1952), S. 345-347 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] AMONG the group of compounds often referred to as organo-phosphorus insecticides, active search continues for members more effective as insecticides and less injurious to mammals than tetra-ethyl pyrophosphate (TEPP), p-nitrophenyl diethyl thiophosphate (Parathion, .E7.6O5) or octa methyl ...
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 248 (1974), S. 711-711 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Given as solutions in glycerol formal by the intravenous route, the lethal dose of NRDC 156 was 6 to 8 mg kg^1 and of NRDC 161, 2 to 2.5 mg kg'"1. Orally, as solutions in arachis oil, an LDso could not be computed, but the rats showed severe toxic effects, with some deaths in the dose range 80 to ...
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 209 (1966), S. 90-90 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] In our original experiments to examine the toxicity of groundnut meal we reported two definite adenocarcinomas. of the stomach while a third animal had multiple meta-stases from a histologically similar adenocarcinoma These experiments were started when the rats were about 5 weeks old and the ...
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 202 (1964), S. 1016-1016 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] In March 1962, Dr. P, C. Spensley, of the Tropical Products Institute, supplied us with 30 mg of aflatoxin batch GOB. On subsequent analysis this was shown to contain 80 per cent aflatoxin of which nearly all was aflatoxin Bx and Gl9 with Gx present in rather greater amounts than Bt (ref. 7). This ...
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] IN 1949 maleic hydrazide (1), 1 : 2-dihydro-pyridazine-3 : 6-dione, was introduced as a plant growth regulator and has since found a number of important commercial uses as a selective weed killer and as a depressant of plant growth in a variety of circumstances. The mode of action of maleic ...
    Type of Medium: Electronic Resource
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