JPET xPharm- The Comprehensive Pharmacology Reference

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Harvey, S. C.
Right arrow Articles by Nickerson, M.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Harvey, S. C.
Right arrow Articles by Nickerson, M.
Journal of Pharmacology And Experimental Therapeutics, Vol. 112, Issue 3, 274-290, 1954
Copyright © 1954 by American Society for Pharmacology and Experimental Therapeutics

REACTIONS OF DIBENAMINE AND SOME CONGENERS WITH SUBSTANCES OF BIOLOGICAL INTEREST IN RELATION TO THE MECHANISM OF ADRENERGIC BLOCKADE

Stewart C. Harvey 1 and Mark Nickerson 1

1 Department of Pharmacology, University of Utah College of Medicine, Salt Lake City

Dibenamine, Dibenzyline, two adrenergically inactive mono-beta-chloroethylamines and a nitrogen mustard were found to react readily in vitro with sulfhydryl groups. In contrast to Dibenamine and Dibenzyline the three adrenergically inactive compounds did not react as completely in unbuffered media as in buffered media. A Dibenamine-cysteine product was isolated.

Data on the effects of Dibenzyline on liver sulfhydryl in vivo were equivocal. However, the molar disparity between the amount of drug tolerated and the total body sulfhydryl precluded obtaining meaningful data. Dibenamine reacted readily with both free and fixed liver sulfhydryl in vitro.

All five drugs were found to react in vitro with fifteen amino compounds and to form esters with fourteen carboxyl compounds, but the reactions were not as complete as with sulfhydryl. Reactions with phosphates and carbohydrateswere slight or absent.

Various of the drugs were found to react with amino and carboxyl groups of bovine serum albumin and with carboxyl groups of zein. The biological activities of insulin and Pitressin and the oxygen-carrying capacity of hemoglobin were reduced by Dibenamine.

Problems relating to the mechanism of action of Dibenamine and a possible chemical-biological correlation are discussed. It is concluded that alkylation of sulfhydryl by Dibenamine and its congeners provides a generally satisfactory mechanism for the production of adrenergic blockade.

Submitted on July 12, 1954




This article has been cited by other articles:


Home page
 J. Physiol.Home page
S. M. Hamza and S. Kaufman
Splenorenal reflex modulates renal blood flow in the rat
J. Physiol., July 1, 2004; 558(1): 277 - 282.
[Abstract] [Full Text] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1954 by the American Society for Pharmacology and Experimental Therapeutics.