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  • 1
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract: The mechanism by which two D3 receptor-preferring agonists, 7-hydroxydipropylaminotetralin (7-OH-DPAT) and quinelorane, modulate cocaine reinforcement was examined by monitoring nucleus accumbens dopamine levels with in vivo microdialysis while rats intravenously self-administered the following four different drug solutions consecutively: (1) cocaine; (2) a combination of cocaine plus a low dose of either agonist; (3) either agonist alone; and finally, (4) a physiological saline solution. Both 7-OH-DPAT (4 µg/infusion) and quinelorane (0.25 µg/infusion) decreased cocaine (0.25 mg/infusion) intake in a manner indicating an enhancement of cocaine reinforcement and simultaneously decreased the cocaine-induced elevations in nucleus accumbens dopamine levels by 〉50%. Subsequent self-administration of either 7-OH-DPAT (4 µg/infusion) or quinelorane (0.25 µg/infusion) alone resulted in significant, but stable, increases in drug intake, with a concurrent decrease in nucleus accumbens dopamine levels to ∼50% below nondrug baseline levels. These findings indicate that postsynaptic D3 receptor stimulation in the nucleus accumbens enhances the reinforcing properties of cocaine. In a second experiment, local application of 7-OH-DPAT via reverse dialysis (30 and 100 nM perfusate concentrations) dose-dependently decreased nucleus accumbens dopamine efflux to 76 ± 3.9 and 61 ± 6.3% of baseline, respectively, whereas there was no effect of this agonist on dopamine efflux in the ipsilateral striatum of these same animals. Coperfusion with the D3 receptor-preferring antagonist nafadotride dose-dependently blocked the effect of 7-OH-DPAT on nucleus accumbens dopamine efflux. These results suggest that, at low concentrations, 7-OH-DPAT selectively activates D3 receptors in vivo.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract— Radioimmunoassays (RIAs) selective for methionine-enkephalin (Met-ENK) and leucineenkephalin (Leu-ENK) have been developed using competition towards binding of 10 pM 125I-enkephalins to antibodies raised in rabbits against ENKs coupled to ovalbumin with carbodiimide. The high sensitivity of the RIAs (IC50 0.57 nm and 0.55 nm for Met- and Leu-ENK, respectively) allowed estimation of the enkephalin content in extracts of all rat brain regions. Regional levels are compared with those determined on the same extracts by a radioreceptor assay (RRA) using competition towards binding of 5 nm [3H]Leu-ENK to rat striatal membranes. Optimal conditions for killing the animals and extracting the endorphins have been carefully investigated: killing by rapid microwave irradiation was not found necessary as long as brain regions were homogenized into 0.1 n-HCl before deproteinization.Marked differences both in total endorphins (RRA) and ENKs (RIA) between regions are observed with similar ranking of the various regions: highest levels are found in striatum and hypothalamus and lowest in cerebellum and hippocampus. In each region the total ENK levels (RIA) represent only 2–13% of the total endorphins (RRA) suggesting the presence of large amounts of endorphins other than the ENKs.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 30 (1978), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Abstract— Different agents have been investigated for their effects on [C3H]glycogen synthesized in mouse cortical slices. Of these noradrenaline, serotonin and histamine induced clear concentration-dependent glycogenolysis.[C3H]Glycogen hydrolysis induced by noradrenaline appears to be mediated by beta-adrenergic receptors because it is completely prevented by timolol, while phentolamine is ineffective. It seems to involve cyclic AMP because it is potentiated in the presence of isobutylmethylxanthine; in addition dibutyryl cyclic AMP (but not dibutyryl cyclic GMP) promotes glycogenolysis.Lower concentrations of noradrenaline were necessary for [C3H]glycogen hydrolysis (EC50= 0.5μM) than for stimulation of cyclic AMP accumulation (EC50= 8μM).After subchronic reserpine treatment the concentration-response curve to noradrenaline was significantly shifted to the left (EC50= 0.09 ± 0.02 μM as compared with 0.49 ± 0.08 μM in saline-pretreated mice) without modifications of either the basal [C3H]glycogen level, maximal glycogenolytic effect, or the dibutyryl cAMP-induced glycogenolytic response.In addition to noradrenaline, clear concentration-dependent [3H]glycogen hydrolysis was observed in the presence of histamine or serotonin. In contrast to the partial [3H]glycogen hydrolysis elicited by these biogenic amines, depolarization of the slices by 50 mM K+ provoked a nearly total [C3H)glycogen hydrolysis.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Journal of neurochemistry 26 (1976), S. 0 
    ISSN: 1471-4159
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: —Histidine decarboxylase activity is found in all parts of the hippocampal formation (subiculum, CA1, CA3 and area dentata), and a major portion of the enzyme is localized in a subcellular fraction containing the nerve terminal particles. The almost complete disppearance of HD (and histamine) after deafferentation of the hippocampal formation suggests that histamine synthesis in this region resides in terminals of extrinsic fibres. The results after selective lesions indicate that these alleged histaminergic fibres enter the hippocampus, like the monaminergic fibres, through a dorsal route (comprising fimbria, fornix superior and cingulum) as well as through a ventral route (via the amygdaloid area). The former was tentatively estimated to represent about 60% of the total hippocampal supply of alleged histaminergic fibres.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Science Ltd
    European journal of neuroscience 10 (1998), S. 0 
    ISSN: 1460-9568
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: By screening an olfactory bulb cDNA library using dopamine receptor probes, we isolated the cDNA coding for the rat counterpart of an orphan receptor known as Edg-2, homologous to G protein-coupled receptors. In situ hybridization analysis showed that Edg-2 mRNA expression is restricted to myelinated structures, e.g. corpus callosum or peripheral nerves. A weaker expression in various peripheral organs was also detected in newborns. A 3.8-kb transcript was found at high levels in highly myelinated brain structures and sciatic nerve, and, at lower levels, in poorly myelinated peripheral organs, consistent with its occurrence in Schwann cells in the peripheral nervous system. One hundred percent of Edg-2 mRNA-containing cells in the brain also expressed mRNA encoding myelin-basic-protein, a marker of oligodendrocytes. This restricted olygodendrocytes localization was confirmed by the absence of cellular colocalization of Edg-2 and glial fibrillary acidic protein, an astrocytic marker. During prenatal development, Edg-2 mRNA expression was high in the cortical neuroepithelium and meningeal layer at E16, extended later to other neuroepithelia, and disappeared shortly after birth. During brain postnatal development, Edg-2 mRNA expression in myelinated structures followed a caudo-rostral gradient, similar to that of myelination. Thus, Edg-2 is the first G protein-coupled receptor found to be selectively expressed in myelin-forming cells in the nervous system and its temporal expression pattern is consistent with a dual role (i) in neurogenesis, during embryonic development, and (ii) in myelination and myelin maintenance, during postnatal life.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 274 (1978), S. 603-605 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] The presence of opiate receptors on noradrenergic nerve terminals was investigated by measuring 3H-naloxone binding in brain regions receiving noradrenergic inputs, after chemical destruction of noradrenergic cell bodies. For 15-40 d after the slow unilateral infusion of 6-hydroxydopamine (6-OHDA) ...
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 56 (1978), S. 233-234 
    ISSN: 1432-2072
    Keywords: Stereotyped behaviour ; Apomorphine ; Dopamine receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Mice treated with apomorphine tend to adopt a vertical position in a stereotyped manner. A quantal evaluation of this behaviour, taking into account its frequency and duration, leads to a biphasic dose-response curve that reveals opposite actions of the dopamine agonist.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 308 (1979), S. 231-237 
    ISSN: 1432-1912
    Keywords: 3H-Domperidone ; Dopamine receptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 3H-Domperidone, a potent antagonist of dopamine but less lipophilic than neuroleptic drugs, was studied as a potential ligand for cerebral dopamine receptors. It labeled with high affinity an apparently homogeneous population of non-interacting sites in a particulate fraction of mouse striatum. Association occurred rapidly and dissociation was relatively slow (t1/2≃4min); this allowed extensive washing of membranes which reduced the non-specific binding to values as low as 5% of the total binding. Consistent Kd values of 0.7 nM were obtained by analysing by various methods either the kinetics of binding or the saturation of binding sites at equilibrium. The relative potencies of various dopamine receptor agonists or antagonists to inhibit 3H-domperidone binding, paralleled their pharmacological activity. On the other hand, a variety of non-dopaminergic agents failed to inhibit 3H-domperidone binding. The findings indicate that striatal dopamine receptors are selectively labeled by this 3H-ligand. In various non-striatal regions of mouse brain the saturable binding of 3H-domperidone was almost entirely inhibited by apomorphine indicating its selectivity for dopamine receptors in spite of the low density of the latter. This was not the case for the binding of 3H-spiperone, evaluated on the same preparations, indicating that 3H-domperidone probably represents the most selective ligand presently available.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 268 (1977), S. 745-747 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] 3H-Leu-enkephalin binds to a particulate fraction from rat striatum and the saturation kinetics at equilibrium evidence two distinct sites; the first one, exhibiting a high affinity (K& around 3 nM) and recognised by morphine or naloxone, has been identified as the 'opiate receptor' whereas the ...
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    [s.l.] : Nature Publishing Group
    Nature 276 (1978), S. 523-526 
    ISSN: 1476-4687
    Source: Nature Archives 1869 - 2009
    Topics: Biology , Chemistry and Pharmacology , Medicine , Natural Sciences in General , Physics
    Notes: [Auszug] Enkephalin-hydrolysing activity exhibits a considerable heterogeneity in rat brain subtractions8. Starting from the hypothesis that a specific peptidase involved in the control of enkephalin concentration in the synaptic cleft should be membrane-bound and should exhibit a high affinity for the ...
    Type of Medium: Electronic Resource
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