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  • 1
    Digitale Medien
    Digitale Medien
    Springer
    The journal of membrane biology 75 (1983), S. 179-192 
    ISSN: 1432-1424
    Schlagwort(e): epithelial ion transport ; apical Na channels ; frog skin ; fluctuation analysis ; extrinsic blockers ; extrinsic stimulators ; amiloride analogs ; PCMB ; TNBS
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie
    Notizen: Summary The stimulation of apical Na permeability caused by a number of reagents effective from the outer side of the membrane was investigated by fluctuation analysis. In the epidermis ofR. ridibunda, parachloromercuriphenyl sulfonate (PCMPS) and benzimidazolyl guanidine (BIG) increase the number (N 0) of conducting Na channels by releasing channels from Na self-inhibition. As a consequence, the apparent macroscopic affinity for amiloride is increased. 5-dimethyl amiloride and trinitrobenzene sulfonate (TNBS) also cause reversible stimulation by increasingN 0; here release from self-inhibition is less clear. With each of the four stimulators investigated, the Na channel current remained unaffected or was only marginally increased. In addition to its stimulatory effect, TNBS caused irreversible blockage of Na channels. Apart from their stimulatory effects, BIG and 5-dimethyl amiloride, both of which have a side-chain terminated with an amidino group, are high rate-blocking competitors of amiloride.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    ISSN: 1432-1424
    Schlagwort(e): epithelial transport ; apical Na permeability of frog skin ; fluctuation analysis ; extrinsic blockers ; amiloride analogs ; triamterene ; triaminopyrimidine ; dose-response curves ; competition kinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Chemie und Pharmazie
    Notizen: Summary Fluctuation analysis of Na current passing the apical membrane in the skin ofRana ridibunda was used to study the kinetics of Na-channel blocking by several organic cations present in the outer solution together with 60mm Na. The ratios of the apparent off-rate and on-rate constants (the microscopic inhibition constants) thus obtained for triamterene, triaminopyrimidine (TAP), 5,6-diCl-amiloride, 5H-amiloride and amiloride itself are found to be in the mean about sevenfold smaller than the corresponding inhibition constants obtained from macroscopic dose-response curves. The apparent discrepancy is explicable by competition of the organic blocker with the channel block by Na ions (the self-inhibition effect). The type of interaction between extrinsic blockage and self-inhibition may be purely competitive or mixed. However, in case of mixed inhibition the competitive component must dominate the noncompetitive component by at least seven to one.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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