Back to Search
Start Over
Synthesis, properties and biological activity of tritiated N-benzylamidino-3,5-diamino-6-chloro-pyrazine carboxamide -- a new ligand for epithelial sodium channels.
- Source :
-
The Journal of pharmacy and pharmacology [J Pharm Pharmacol] 1979 Jun; Vol. 31 (6), pp. 382-6. - Publication Year :
- 1979
-
Abstract
- 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.
- Subjects :
- Amiloride analogs & derivatives
Amiloride chemical synthesis
Animals
Anura
Chromatography, Thin Layer
Drug Stability
Electrophoresis, Paper
Epithelium metabolism
In Vitro Techniques
Ion Channels metabolism
Ligands
Rana temporaria
Amiloride pharmacology
Ion Channels drug effects
Pyrazines pharmacology
Sodium metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0022-3573
- Volume :
- 31
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- The Journal of pharmacy and pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 39137
- Full Text :
- https://doi.org/10.1111/j.2042-7158.1979.tb13528.x