Skip to main content
Clinical and Experimental Immunology logoLink to Clinical and Experimental Immunology
. 1977 Sep;29(3):436–441.

Blocking of histamine release from human basophils in vitro by the ATPase inhibitor, ethacrynic acid.

A M Magro
PMCID: PMC1541062  PMID: 73437

Abstract

Ethacrynic acid, a known inhibitor of both Na+--K+ and Mg2+-activated ATPases, effectively inhibits histamine release from antigen-challenged human basophils in vitro. Ouabain, an inhibitor specific for Na+--K+-activated ATPases, shows no effect upon the quantity of histamine released from the antigen-challenged basophils. Ethacrynic acid also effectively inhibits Ca2+--ionophore A23187-induced release, implying it inhibits the Ca2+-dependent secretory stage of the histamine-release process. Inhibition of ATPases and histamine release by ethacrynic acid both require the presence of the olefinic bond in the ethacrynic-acid molecule. Possible utilization of analogues of ethacrynic acid as anti-allergic drugs and as a device to investigate the ATPase system of histamine-releasing cells is suggested.

Full text

PDF
436

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. BLOCK J. B., BONTING S. L. SODIUM-POTASSIUM ACTIVATED ADENOSINETRIPHOSPHATASE AND CATION TRANSPORT IN NORMAL AND LEUKEMIC HUMAN LEUKOCYTES (STUDIES ON SODIUM-POTASSIUM ACTIVATED ADENOSINETRIPHOSPHATASE. 13). Enzymol Biol Clin (Basel) 1964;41:183–198. [PubMed] [Google Scholar]
  2. Bicking J. B., Holtz W. J., Watson S., Cragoe E. J., Jr (Vinylaryloxy)acetic acids. A new class of diuretic agents. 1. (Diacylvinylaryloxy)acetic acids. J Med Chem. 1976 Apr;19(4):530–535. doi: 10.1021/jm00226a017. [DOI] [PubMed] [Google Scholar]
  3. Bicking J. B., Robb C. M., Watson L. S., Cragoe E. J., Jr (Vinylaryloxy)acetic acids. A new class of diuretic agents. 2. (4-(3-Oxo-1-alkenyl)phenoxy)acetic acids. J Med Chem. 1976 Apr;19(4):544–547. doi: 10.1021/jm00226a020. [DOI] [PubMed] [Google Scholar]
  4. Foreman J. C., Mongar J. L., Gomperts B. D. Calcium ionophores and movement of calcium ions following the physiological stimulus to a secretory process. Nature. 1973 Oct 5;245(5423):249–251. doi: 10.1038/245249a0. [DOI] [PubMed] [Google Scholar]
  5. Ishizaka K., Ishizaka T. Identification of gamma-E-antibodies as a carrier of reaginic activity. J Immunol. 1967 Dec;99(6):1187–1198. [PubMed] [Google Scholar]
  6. KING T. P., NORMAN P. S. Isolation studies of allergens from regweed pollen. Biochemistry. 1962 Jul;1:709–720. doi: 10.1021/bi00910a027. [DOI] [PubMed] [Google Scholar]
  7. MONGAR J. L., SCHILD H. O. Cellular mechanisms in anaphylaxis. Physiol Rev. 1962 Apr;42:226–270. doi: 10.1152/physrev.1962.42.2.226. [DOI] [PubMed] [Google Scholar]
  8. MONGAR J. L., SCHILD H. O. The effect of calcium and pH on the anaphylactic reaction. J Physiol. 1958 Feb 17;140(2):272–284. doi: 10.1113/jphysiol.1958.sp005933. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Reed P. W., Lardy H. A. A23187: a divalent cation ionophore. J Biol Chem. 1972 Nov 10;247(21):6970–6977. [PubMed] [Google Scholar]
  10. SCHULTZ E. M., CRAGOE E. J., Jr, BICKING J. B., BOLHOFER W. A., SPRAGUE J. M. ALPHA, BETA-UNSATURATED KETONE DERIVATIVES OF ARYLOXYACETIC ACIDS, A NEW CLASS OF DIURETICS. J Med Pharm Chem. 1962 May;91:660–662. doi: 10.1021/jm01238a030. [DOI] [PubMed] [Google Scholar]
  11. SHORE P. A., BURKHALTER A., COHN V. H., Jr A method for the fluorometric assay of histamine in tissues. J Pharmacol Exp Ther. 1959 Nov;127:182–186. [PubMed] [Google Scholar]
  12. SKOU J. C. The influence of some cations on an adenosine triphosphatase from peripheral nerves. Biochim Biophys Acta. 1957 Feb;23(2):394–401. doi: 10.1016/0006-3002(57)90343-8. [DOI] [PubMed] [Google Scholar]
  13. Schultz E. M., Bicking J. B., Deana A. A., Gould N. P., Strobauge T. P., Watson L. S., Cragoe E. J., Jr (Vinylaryloxy)acetic acids. A new class of diuretic agents. 3. ((2-Nitro-1-alkenyl)aryloxy)acetic acids. J Med Chem. 1976 Jun;19(6):783–787. doi: 10.1021/jm00228a009. [DOI] [PubMed] [Google Scholar]
  14. Siraganian R. P. An automated continuous-flow system for the extraction and fluorometric analysis of histamine. Anal Biochem. 1974 Feb;57(2):383–394. doi: 10.1016/0003-2697(74)90093-1. [DOI] [PubMed] [Google Scholar]
  15. Woltersdorf O. W., Jr, Robb C. M., Bicking J. B., Watson L. S., Cragoe E. J., Jr (Vinylaryloxy)acetic acids. A new class of diuretic agents. 4. Various ((2-substituted and 2,2-disubstituted vinyl)aryloxy)acetic acids. J Med Chem. 1976 Jul;19(7):972–975. doi: 10.1021/jm00229a024. [DOI] [PubMed] [Google Scholar]

Articles from Clinical and Experimental Immunology are provided here courtesy of British Society for Immunology

RESOURCES