Structure-activity relationship of amiloride analogs as blockers of epithelial Na channels: II. Side-chain modifications

The Journal of Membrane Biology

Volumn 95, Issue 2, 1987, Pages 171-185

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

^a SAARLAND UNIVERSITY   (Germany)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

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

Indexed keywords

AMILORIDE; AMILORIDE DERIVATIVE; BENZAMIL; TRIAMTERENE;

ANIMAL CELL; BIOLOGICAL MODEL; DRUG COMPARISON; DRUG SCREENING; DRUG STABILITY; EPITHELIUM; FROG; NONHUMAN; PRIORITY JOURNAL; SKIN; SODIUM CHANNEL; STRUCTURE ACTIVITY RELATION;

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

EID: 0023112928     PISSN: 00222631     EISSN: 14321424     Source Type: Journal    
DOI: 10.1007/BF01869162     Document Type: Article

References (63)

1. Autoregulation of apical membrane Na+ permeability of tight epithelia. Noise analysis with amiloride and CGS 4270
2. Uptake of (3H)-benzamil at different sodium concentrations. Inferences regarding the regulation of sodium permeability
3. Estimation of the density of sodium entry sites in, frog skin epithelium from the uptake of (3H)-benzamil
4. Application of the theory of diffusion controlled reactions to enzyme kinetics
5. On the crossreactivity of amiloride and 2,4,6-triaminopyrimidine (TAP) for the cellular entry and tight junctional cation permeation pathways in epithelia
6. Amiloride: A molecular probe of sodium transport in tissues and cells
7. Effect of amiloride and some of its analogs on cation transport in isolated frog skin and thin lipid membranes
8. Pyrazine diuretics. I. N-Amidino-3-amino-6-halopyrazinecarboxamides
9. Ground states of molecules. XXV. MINDO/3. An improved version of the MINDO semiempirical SCF-MO method
10. Fluctuation analysis of short-circuit current in a warm-blooded sodium-retaining epithelium: Site current, density, and interaction with triamterene
11. Structure activity relationships in the amiloride series
12. Pyrazine diuretics. II. N-amidino-3-amino-5-substituted 6-halopyrazinecarboxamides
13. Importance of guanidinium groups for blocking sodium channels in epithelia
14. Sodium entry step in transporting epithelia: Results of ligand-binding studies
15. Effects of some pyrazine carboxamides on sodium transport in frog skin
16. Rate constants of proteolytic reactions in aqueous solution
17. Some applications of modern rate theory to physiological systems
18. Inhibition of short-circuit current by triaminopyrimidine in isolated toad urinary bladder
19. Competitive blocking of apical sodium channels in epithelia
20. Current voltage curve of sodium channels and concentration dependence of sodium permeability in frog skin
21. Phenamil: An irreversible inhibitor of sodium channels in the toad urinary bladder
22. The tetrodotoxin and saxitoxin binding site of voltage-dependent sodium channels is negatively charged and distant from the permeation pathway
23. Single channel recordings from the amiloride-sensitive epithelial Na+ channel
24. Relaxation spectrometry of biological systems
25. Kinetic mapping of the antibody combining site by chemical relaxation spectrometry
26. The receptor for tetrodotoxin and saxitoxin
27. Triamterene-induced sodium current fluctuations in frog skin
28. Effect of sodium on amiloride-and triamterene-induced current fluctuations in isolated frog skin
29. Pyrazine diuretics. V. N-amidino-3-aminopyrazinecarboxamidines and analogs 2,4-diaminopteridines
30. Active groups of saxitoxin and tetrodotoxin as deduced from actions of saxitoxin analogs on frog muscle and squid axon
31. Kinetic aspects of structure-activity relations: The binding of sulphonamides by carbonic anhydrase
32. Structure-activity relationship of amiloride analogs as blockers of epithelial Na channels: I. Pyrazine-ring modifications
33. Blockage of epithelial Na-channels by amiloride analogs: Dependence of rate constants on drug structure
34. pH dependence of apical Na transport in frog skin
35. Chemical stimulation of Na transport through amiloride blockable channels of frog skin epithelium
36. Competitive blocking of epithelial Na channels by organic cations: The relationship between macroscopic and microscopic inhibition constants
37. The beginning of fluctuation analysis of epithelial ion transport
38. Fluctuation analysis of sodium channels in epithelia
39. Sodium-specific membrane channels of frog skin are pores: Current fluctuations reveal high turnover
40. The mechanism of Na uptake through Na-selective channels in the epithelium of frog skin
41. Dependence of the blocking rate constants of amiloride on the mucosal Na concentration
42. Blockage of cation permeability across the tight junction of gallbladder and other leaky epithelia
43. Displacement of TTX from Na channels by Na+, Li+, K+ ions
44. Voltage dependence of amiloride inhibition of apical membrane Na conductance in toad urinary bladder
45. Interactions of amiloride and other blocking cations with the apical Na channel in the toad urinary bladder
46. Amiloride-blockable Na-channels observed after fusion of membrane vesicles from toad urinary bladder to planar phospholipid bilayers
47. The amiloride-sensitive sodium channel
48. 3,5-Diamino-6-chloropyrazinecarboxylic acid active esters' and their reactions
49. Activated esters of substituted pyrazinecarboxylic acids
50. Pyrazine diuretics. VI (Pyrazine-carboxamido) guanidines
51. Proton, carbon-13, and nitrogen-15 nuclear magnetic resonance and CNDO/2 studies on the tautomerism and conformation of amiloride, a novel acylguanidin
52. The MNDOC method, a correlated version of the MNDO model
53. Voltage dependence of Na channel blockage by amiloride: Relaxation effects in admitance spectra
54. Voltage dependence of the blocking rate constants of amiloride at apical Na channels
55. The influence of 2,4,6-triaminopyrimidine on Na transport in frog skin
56. Chemical stimulation of Na current through the outer surface of frog skin epithelium