Characteristics of sodium channels in transporting epithelia

  • A. W. Cuthbert
Chapter
Part of the Biological Council book series

Abstract

One of the most interesting drugs which has become available for investigating the properties of sodium channels in epithelia which transport this ion is amiloride, a material discovered in the search for new diuretic drugs. Chemically it is an N-amidino pyrazine carboxamide, the formula of which is given in Fig. 1. The guanidine moiety is essential for the activity of this compound, and indeed guanidine itself has been shown to have some actions similar to those of amiloride, although it is much less potent (Bentley, 1968). The activities of a great number of analogues of amiloride have been measured by their effects on the urinary sodium-potassium ratio in DOCAtreated rats. Using this criterion it can be concluded that halogenation in position 6 is essential for activity, with the chloro compounds the most active. Substitution on the 5-amino group invariably leads to a reduction in activity, while very varied substitution on the terminal amino group of the guanidine residue can be made without affecting potency (Cragoe, Woltersdorf, Bicking, Kwong & Jones, 1967).
Fig. 1.

Structural formula of amiloride

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Copyright information

© Institute of Biology Endowment Trust Fund 1973

Authors and Affiliations

  • A. W. Cuthbert
    • 1
  1. 1.Department of PharmacologyUniversity of CambridgeCambridgeEngland

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