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  • 1
    ISSN: 1573-6903
    Schlagwort(e): Muscarinic ; M3 receptors ; HSDM1C1 cells ; PI turnover ; [3H]4-DAMP binding ; Receptor binding
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: 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.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    Journal of optimization theory and applications 53 (1987), S. 461-474 
    ISSN: 1573-2878
    Schlagwort(e): Nonlinear time-lag systems ; linear control constraints ; nonlinear terminal inequality constraints ; feasible direction methods ; accumulation points ; relaxed controls ; relaxed control problems ; necessary conditions for optimality
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Mathematik
    Notizen: Abstract In this paper, we consider a class of time-lag optimal control problems involving control and terminal inequality constraints. A feasible direction algorithm has been obtained by Teo, Wong, and Clements for solving this class of optimal control problems. It was shown that anyL ∞ accumulation points of the sequence of controls generated by the algorithm satisfy a necessary condition for optimality. However, suchL ∞ accumulation points need not exist. The aim of this paper is to prove a convergence result, which ensures that the sequence of controls generated by the algorithm always has accumulation points in the sense of control measure, and these accumulation points satisfy a necessary condition for optimality for the corresponding relaxed problem.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 3
    Digitale Medien
    Digitale Medien
    Springer
    Journal of optimization theory and applications 46 (1985), S. 295-317 
    ISSN: 1573-2878
    Schlagwort(e): Nonlinear time-lag systems ; linear control constraints ; nonlinear terminal inequality constraints ; conditional gradient methods ; feasible direction methods ; control parametrization ; initial feasible control ; computational schemes ; finite convergence
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Mathematik
    Notizen: Abstract A computational algorithm for a class of time-lag optimal control problems involving control and terminal inequality constraints is presented. The convergence properties of the algorithm is also investigated. To test the algorithm, an example is solved.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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