PMID: 39137Jun 1, 1979

Synthesis, properties and biological activity of tritiated N-benzylamidino-3,5-diamino-6-chloro-pyrazine carboxamide -- a new ligand for epithelial sodium channels

The Journal of Pharmacy and Pharmacology
A W Cuthbert, J M Edwardson


A method is described for the synthesis and purification of tritiated N-benzylamidino-3,5-diamino-6-chloro-pyrazine carboxamide (benzamil). The tritium was inserted at the meta position of the benzyl ring, from which it apparently does not exchange with solvent hydrogen. When stored in ethanol at -4 degrees C the radioligand remains stable for at least 15 months. The pharmacology of benzamil is very similar to that of amiloride in terms of its effects on sodium transporting epithelia except that it has a higher affinity. The affinity of benzamil for sodium channels in amphibian epithelia in the absence of sodium is approximately 10(9) M-1. The new ligand can be used to label sodium channels in epithelia, and may be useful in channel isolation procedures.


Jun 17, 1975·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·A W Cuthbert, W K Shum
Jan 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·W A Catterall, C S Morrow
May 1, 1978·British Journal of Pharmacology·A W Cuthbert, G M Fanelli
Feb 1, 1973·The Journal of Physiology·A W Cuthbert
Jan 1, 1967·Journal of Medicinal Chemistry·E J CragoeJ H Jones


Feb 1, 1982·Pflügers Archiv : European journal of physiology·A W CuthbertE Skadhauge
Oct 1, 1988·The Journal of Membrane Biology·T R Kleyman, E J Cragoe

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