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Journal of Pharmacology And Experimental Therapeutics, Vol. 106, Issue 3, 291-302, 1952
Copyright © 1952 by American Society for Pharmacology and Experimental Therapeutics

ENZYMATIC DEAMINATION AND VASODEPRESSOR EFFECTS OF ADENOSINE ANALOGS

Donald A. Clarke 1, John Davoll 1, Frederick S. Philips 1, and George Bosworth Brown 1

1 Divisions of Experimental Chemotherapy and Protein Chemistry, Sloan-Kettering Institute for Cancer Research, New York, New York

1. Adenosine analogs with substitutions in the 2-position have been shown to elicit adenosine-like vasodepression in the cat. Several of these analogs were found more potent than adenosine; all caused hypotension of greater duration than that produced by the parent riboside.

2. The relatively transient nature of the hypotension induced by adenosine in the cat has been attributed to the activity of adenosine deaminase. Persistence of vasodepression, characteristic of the 2-substituted congeners, has been attributed to failure of the enzyme to deaminate these analogs.

3. A manometnic method has been described which was employed to study the adenosine deaminase activity of various tissues of cats, rats and rabbits and to ascertain the relative susceptibility of adenosine and its analogs to enzymatic degradation.

4. The influence of molecular alteration on the vasodepressor activity of purine nibosides has been discussed.

Submitted on July 7, 1952




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