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  • 11
    Electronic Resource
    Electronic Resource
    M3 muscarinic receptors on murine HSDM1C1 cells: Further functional, regulatory, and receptor binding studies (1995)
    Springer
    Neurochemical research 20 (1995), S. 61-68 
    Details
    ISSN: 1573-6903
    Keywords: Muscarinic ; M3 receptors ; HSDM1C1 cells ; PI turnover ; [3H]4-DAMP binding ; Receptor binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In the present studies, the pharmacology and regulation of the functional muscarinic receptors on HSDM1C1 cells were probed using phosphoinositide (PI) turnover assays. In addition, the receptor binding of the putative M3-selective radioligand, [3H]4-DAMP, to cell homogenates was characterized. Carbachol (EC50=9 μM), (+)muscarine (EC50=4.5 μM) and cis-dioxolane (EC5=0.72 μM) were full agonists which stimulated PI turnover by 13.3±1.0 fold above basal values. The potencies of numerous agonists in this assay system were relatively similar to their affinities in receptor binding assays. Exposure of HSDM1C1 cells to 10 nM–10 μM muscarine during the last 24h of [3H]myo-inositol-labeling resulted in a concentration-dependent reduction in the cisdioxolane affinity and maximal PI response induced by subsequent treatment with cis-dioxolane. pertussis toxin (5–2000 ng/ml) caused a partial reduction in the cis-dioxolane-induced PI turnover. Likewise, exposure of the HSDM1C1 cells to an active phorbol ester (TPA) resulted in a partial inhibition of the cis-dioxolane-induced (100 μM) PI turnover. The half-maximal effect of TPA was produced at 1.8±0.3 nM. [3H]4-DAMP binding to cell homogenates was of high affinity (Kd=0.19±0.04 nM) and moderate capacity (Bmax=201±22 fmol/mg protein). The pharmacological specificity (4-DAMP〉p-FHHSiD〉dicyclomine〉pirenzepine〉methoctramine〉AFDX-116 〉gallamine) resembled that for [3H]NMS binding and correlated well with that observed for inhibition of PI turnover. These studies further support the identification of M3 receptors on HSDM1C1 cells. These receptors have been shown to be influenced by pertussis toxin, an active phorbol ester and to exhibit desensitization.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00995154
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    Paper (German National Licenses)
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  • 12
    Electronic Resource
    Electronic Resource
    Quantitative autoradiography demonstrates selective modulation of rat brain regional dopamine (D1 and D2) receptor subtypes after chronic manipulation of dietary salt (1995)
    Springer
    Neurochemical research 20 (1995), S. 121-128 
    Details
    ISSN: 1573-6903
    Keywords: Dopamine receptors ; autoradiography ; hypertension ; schizophrenia ; Parkinson's disease
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects of chronic dietary sodium chloride (NaCl) consumption on renal function and brain dopamine receptors were studied in adult, male normotensive rats. Compared to rats maintained on the normal NaCl (0.33%) diet, animals maintained on the low NaCl (0%) diet for 4 weeks exhibited significant increases in plasma aldosterone, chloride and changes in urinary electrolyte excretion. In contrast, rats maintained on the high NaCl (8%) diet for 4 weeks demonstrated significant increases in urine volume and urinary sodium, chloride and dopamine excretions and water intake. Rats fed the high NaCl diet displayed a 42–59% decrease (p〈0.001–0.05) in D1 binding in the nucleus accumbens (NA), olfactory tubercle (OT) and the striatum (STM), without any effects on D2 binding in these brain regions. Rats maintained on the low NaCl diet also demonstrated decreased D1 binding in the ventral (24%, p〈0.02) and lateral (29%, p〈0.01) STM, but not in the OT, NA, entopeduncular nucleus and substantia nigra. Rats fed low or high NaCl diets exhibited a 35–180% increase (p〈0.01–0.05) in D2 binding in several mid-brain areas (e.g. hypothalamus, thalamus and hippocampus) and hindbrain regions (e.g. superior colliculus and nucleus tractus solitarius) without affecting the D1 binding. These data indicate that chronic modification of dietary salt intake profoundly affects the renal handling of sodium/water excretion and leads to selective up- and/or down-regulation of DA receptor subtypes in different areas of the brain. These findings may have relevance to centrally-mediated hypertension, Parkinson's disease, schizophrenia and other brain disorders involving dopamine and dopamine receptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00970535
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  • 13
    Electronic Resource
    Electronic Resource
    Neurochemical, pharmacological, and developmental studies on cerebellar receptors for dicarboxylic amino acids (1984)
    Springer
    Neurochemical research 9 (1984), S. 81-101 
    Details
    ISSN: 1573-6903
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Specific binding ofl-[3H]glutamate ([3H]Glu) andl-[3H]asparate ([3H]Asp) to cerebellar membranes represented a time-, temperature- pH- and protein-dependent interaction which was both saturable and reversible. Binding sites for both radioligands appeared maximally enriched in synaptosomal fractions isolated by gradient centrifugation. Kinetically derived dissociation constant (K off/K on=K d) for [3H]Glu binding to this fraction indicated high-affinity (443 nM). Competition experiments employing analogs of excitatory amino acids, including new antagonists, helped identify binding sites for [3H]Glu and [3H]Asp as receptors with differential pharmacological, specificities. Membrane freezing reduced numbers of both receptor types, but binding activity could be recovered partially by incubation at 37°C. Glu receptors exhibited a pronounced deleterious sensitivity to thiol modifying reagents andl-Glu (50–1000 μM) provided protection, against these compounds during co-incubation with cerebellar membranes. It is suggested that cold storage may induce partially reversible receptor inactivation by promoting sulfhydryl group/bond modification. Rat cerebellar glutamatergic function (endogenous Glu content, Glu uptake and receptor sites) exhibited an apparent ontogenetic peak between days 8–12 postpartum with a plateauing profile from day 30 to adulthood. The accelerated development (days 8–12) coincides with the first demonstrable Glu release and kainic acid neurotoxicity, as described previously.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00967661
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    Paper (German National Licenses)
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