Studies on the Metabolism of γ-Guanidinobutyric Acid (HL 521) and its Amide (HL 523)

M. F. Beeson; A. L. J. Buckle; H. E. H. Jones

doi:10.1055/s-0028-1094154

Hormone and Metabolic Research, Table of Contents

Horm Metab Res 1971; 3(3): 188-192
DOI: 10.1055/s-0028-1094154

Originals

Studies on the Metabolism of γ-Guanidinobutyric Acid (HL 521) and its Amide (HL 523)

M. F. Beeson [*] , A.L. J. Buckle [**] , H.E. H. Jones [***]

Beecham Research Laboratories, Orchard Lea, Winkfield, Windsor, Berks., England

Abstract

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Abstract

The tissue distribution and metabolism of γ-guinidinobutyramide (HL 523), a hypoglycemic agent of low toxicity, have been studied. After intravenous administration to the rabbit, the compound was very rapidly removed from the bloodstream.

In vitro HL 523 was strongly taken up by vascular tissue and also retained well by kidney, liver and other organs. This finding was confirmed by autoradiography which showed that salivary glands had a very high affinity for the drug, and that it was rapidly excreted into the urine. When dosed orally, 95% of the recovered compound was found unchanged in the urine; the remainder was mostly excreted as the free acid, γ-guanidinobutyric acid (HL 521). Mice dosed with HL 521 excreted this compound unchanged except for a 14% conversion to urea.

Key words

γ-Guanidinobutyramide - Glycemia - Tissue Distribution - Excretion - γ-Guanidinobutyric Acid - Glycocyamine - Urea - Arginine

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References

1 Present address: Beecham Research Laboratories, Chemotherapeutic Research Centre, Brockham Park, Betchworth, Surrey, England.

2 Present address: Guy's Hospital Medical School, London Bridge, S.E. 1.

3 Present address: Glaxo Research Ltd., Greenford, Middlesex, England.