Structure-activity relationship of amiloride analogs as blockers of epithelial Na channels: I. Pyrazine-ring modifications

The Journal of Membrane Biology

Volumn 83, Issue 1-2, 1985, Pages 45-56

  Li, J H Y ^a,b   Cragoe Jr , E J ^a,b   Lindemann, B ^a,b  

^a 2nd Department of Physiology ^*  (Germany)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

amiloride; blocking kinetics; fluctuation analysis; frog skin; Na channels; structure activity relationship

Indexed keywords

AMILORIDE DERIVATIVE;

ANIMAL CELL; DRUG COMPARISON; DRUG MECHANISM; DRUG SCREENING; EPITHELIUM CELL; NONHUMAN; PRIORITY JOURNAL; SKIN; SODIUM CHANNEL; STRUCTURE ACTIVITY RELATION;

AMILORIDE; ANIMAL; EPITHELIUM; HYDROGEN-ION CONCENTRATION; ION CHANNELS; KINETICS; MODELS, BIOLOGICAL; PYRAZINES; RANA RIDIBUNDA; SKIN; SODIUM; STRUCTURE-ACTIVITY RELATIONSHIP; SUPPORT, NON-U.S. GOV'T; THERMODYNAMICS;

EID: 0021926330     PISSN: 00222631     EISSN: 14321424     Source Type: Journal    
DOI: 10.1007/BF01868737     Document Type: Article

References (48)

1. Estimation of the density of sodium entry sites in frog skin epithelium from the uptake of3H-benzamil
2. Amiloride, a molecular probe of sodium transport in tissues and cells
3. Sodium flux ratio through the amiloride-sensitive entry pathway in frog skin
4. Irreversible inhibition of sodium entry sites in frog skin by a photosensitive amiloride analog
5. Effect of amiloride and some of its analogues on cation transport in isolated frog skin and thin lipid membranes
6. Pyrazine diuretics. I. N-Amidino-3-amino-6-halo-pyrazinecarboxamides
7. Pyrazine diuretics. III. 5- and 6-Alkyl,-cycloalkyl and-aryl derivatives of N-amidino-3-amino-pyrazinecarboxamides
8. Fluctuation analysis of short-circuit current in a warm-blooded sodium-retaining epithelium: Site current, density, and interaction with triamterene
9. Irreversible inhibition of sodium transport by the toad urinary bladder following photolysis of amiloride analogs
10. Structure activity relationships in the amiloride series
11. Pyrazine diuretics. II. N-Amidino-3-amino-5-substituted 6-halopyrazinecarboxyamides
12. Importance of guanidinium groups for blocking sodium channels in epithelia
13. Sodium entry step in transporting epithelia: Results of ligand-binding studies
14. Effects of some pyrazine carboxamides on sodium transport in frog skin
15. Irreversible inhibition of epithelial sodium channels by ultraviolet irradiation
16. Characteristics of the entry process for sodium in transporting epithelia as revealed with amiloride
17. Competitive blocking of apical Na channels in epithelia
18. Current voltage curve of sodium channels and concentration dependence of sodium permeability in frog skin
19. Feedback inhibition of sodium uptake in K-depolarized toad urinary bladder
20. Voltage dependence of channel currents and of channel densities in the apical membrane of toad urinary bladder
21. Pyrazine diuretics. V. N-Amidino-3-aminopyrazinecarboxamidines and analogues 2,4-diaminopteridimes
22. Kinetic aspects of structure-activity relations: The binding of sulphonamides by carbonic anhydrase
23. Inhibitory and stimulatory effects of amiloride analogues on sodium transport in frog skin
24. Blockage of epithelial Na-channels by amiloride analogues: Dependence of rate constants on drug structure
25. pH dependence of apical Na transport in frog skin
26. Chemical stimulation of Na transport through amiloride blockable channels of frog skin epithelium
27. Competitive blocking of epithelial Na channels by organic cations: The relationship between macroscopic and microscopic inhibition constants
28. Fluctuation analysis of sodium channels in epithelia
29. Sodium-specific membrane channels of frog skin are pores: Current fluctuations reveal high turnover
30. The mechanism of Na uptake through Na-selective channels in the epithelium of frog skin
31. Structure and function of the epidermis
32. An extended table of Hammett substituent constants based on the ionisation of substituted benzoic acids
33. Na-transport and flux ratio through apical Na-channels in toad bladder
34. Proton magnetic resonance study of intramolecular hydrogen bonding in halophenols
35. 3,5-Diamino-6-chloropyrazinecarboxylic acid “active esters” and their reactions
36. Activated esters of substituted pyrazinecarboxylic acids
37. Pyrazine diuretics, VI. (Pyrazinecarboxamido)guanidines
38. Proton, carbon-13, and nitrogen-15 nuclear magnetic resonance and CNDO/2 studies on the tautomerism and conformation of amiloride, a novel acylguanidine
39. The active ion transport through the isolated frog skin in the light of tracer studies
40. Concentration dependence of currents through single sodium-selective pores in frog skin
41. Blockage of Na-channels in frog skin by titration with protons and by chemical modification of COO−-groups