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Effect of sulfhydryl-reactive ATPase inhibitors upon mast cell and basophil activation.
Int Arch Allergy Appl Immunol. 1983; 72(1):41-5.IA

Abstract

Ethacrynic acid is an inhibitor of Ca2+-Mg2+-activated ATPases which also inhibits histamine release. By testing analogs of ethacrynic acid, the molecular structural requirements for ATPase inhibition and for inhibition of histamine release were compared. The results indicated that effective inhibition involves several structural features of the molecule. Analogs void of chlorine atoms were ineffective as inhibitors of histamine release and ATPase activity. Inhibition of both ATPase and histamine release requires a sulfhydryl-reactive olefinic bond, but sulfhydryl reactivity alone is not sufficient, as certain analogs which have a high capacity to react with sulfhydryl moieties were not active. Replacement of carboxy by highly ionized moieties like sulfo, rendered the molecules ineffective as an inhibitor of histamine release. Compounds which did not inhibit ATPase activity did not inhibit histamine release. The data indicate that mast cells and basophils require an intact ATPase system for histamine release, and raises the question of whether both ecto and endo ATPases are essential.

Authors

Magro AM
No affiliation info available
Cragoe EJ
No affiliation info available
Hurtado I
No affiliation info available
Rudofsky UH
No affiliation info available

MeSH

Adenosine TriphosphatasesAnimalsBasophilsEnzyme InhibitorsEthacrynic AcidHistamine ReleaseMast CellsRatsRats, Inbred Strains

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

6192095

Citation

Magro, A M., et al. "Effect of Sulfhydryl-reactive ATPase Inhibitors Upon Mast Cell and Basophil Activation." International Archives of Allergy and Applied Immunology, vol. 72, no. 1, 1983, pp. 41-5.
Magro AM, Cragoe EJ, Hurtado I, et al. Effect of sulfhydryl-reactive ATPase inhibitors upon mast cell and basophil activation. Int Arch Allergy Appl Immunol. 1983;72(1):41-5.
Magro, A. M., Cragoe, E. J., Hurtado, I., & Rudofsky, U. H. (1983). Effect of sulfhydryl-reactive ATPase inhibitors upon mast cell and basophil activation. International Archives of Allergy and Applied Immunology, 72(1), 41-5.
Magro AM, et al. Effect of Sulfhydryl-reactive ATPase Inhibitors Upon Mast Cell and Basophil Activation. Int Arch Allergy Appl Immunol. 1983;72(1):41-5. PubMed PMID: 6192095.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of sulfhydryl-reactive ATPase inhibitors upon mast cell and basophil activation. AU - Magro,A M, AU - Cragoe,E J,Jr AU - Hurtado,I, AU - Rudofsky,U H, PY - 1983/1/1/pubmed PY - 2001/3/28/medline PY - 1983/1/1/entrez SP - 41 EP - 5 JF - International archives of allergy and applied immunology JO - Int Arch Allergy Appl Immunol VL - 72 IS - 1 N2 - Ethacrynic acid is an inhibitor of Ca2+-Mg2+-activated ATPases which also inhibits histamine release. By testing analogs of ethacrynic acid, the molecular structural requirements for ATPase inhibition and for inhibition of histamine release were compared. The results indicated that effective inhibition involves several structural features of the molecule. Analogs void of chlorine atoms were ineffective as inhibitors of histamine release and ATPase activity. Inhibition of both ATPase and histamine release requires a sulfhydryl-reactive olefinic bond, but sulfhydryl reactivity alone is not sufficient, as certain analogs which have a high capacity to react with sulfhydryl moieties were not active. Replacement of carboxy by highly ionized moieties like sulfo, rendered the molecules ineffective as an inhibitor of histamine release. Compounds which did not inhibit ATPase activity did not inhibit histamine release. The data indicate that mast cells and basophils require an intact ATPase system for histamine release, and raises the question of whether both ecto and endo ATPases are essential. SN - 0020-5915 UR - https://www.unboundmedicine.com/medline/citation/6192095/Effect_of_sulfhydryl_reactive_ATPase_inhibitors_upon_mast_cell_and_basophil_activation_ L2 - https://www.lens.org/lens/search/patent/list?q=citation_id:6192095 DB - PRIME DP - Unbound Medicine ER -