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Benzalkonium chloride: selective inhibitor of histamine release induced by compound 48/80 and other polyamines.
J Pharmacol Exp Ther. 1979 Dec; 211(3):711-5.JP

Abstract

Benzalkonium chloride (BAC) is a mixture of quaternary benzyldimethylalkylammonium chlorides which was found to inhibit histamine release induced by polyamines (48/80, ATP, bradykinin, curare, guanethidine, polylysine, polymyxin B, poly-THIQ, protamine, stilbamidine or substance P), but not that caused by antigens, concanavalin A, dextran, lonophores (A23187 or X-537A), enzymes (chymotrypsin or phospholipase C), monoamines (dextromethorphan, meperidine or chlorpromazine) or detergents (decylamine, Triton X-100 or a fire ant venom alkylpiperidine). Inhibition by 1.5 and 3 microgram of BAC per ml caused parallel shifts of the 48/80 dose-response curves to the right with no loss of efficacy, indicating that the antagonism was surmountable. Phospholipase C was partially inhibited by BAC, but Triton X-100 also inhibited phospholipase C (but not 48/80), indicating that the inhibition of phospholipase C by BAC was probably a nonspecific, detergent effect. BAC caused histamine release by itself at concentrations over 5 microgram/ml. Heat inactivation (50 degrees C for 15 min) of the mast cells did not prevent this release, suggesting a lytic mechanism for this action. Structure-activity relations studies on various members of the BAC family for their ability to inhibit 48/80-induced histamine release indicated that benzyldimethyltridecylammonium chloride was the most potent.

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Publisher Full Text

Authors

Read GW
No affiliation info available
Kiefer EF
No affiliation info available

MeSH

AnimalsBenzalkonium CompoundsFemaleHistamine ReleaseMaleMast CellsPolyaminesPolyethylene GlycolsRatsType C Phospholipasesp-Methoxy-N-methylphenethylamine

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, Non-P.H.S.

Language

eng

PubMed ID

92563

Citation

Read, G W., and E F. Kiefer. "Benzalkonium Chloride: Selective Inhibitor of Histamine Release Induced By Compound 48/80 and Other Polyamines." The Journal of Pharmacology and Experimental Therapeutics, vol. 211, no. 3, 1979, pp. 711-5.
Read GW, Kiefer EF. Benzalkonium chloride: selective inhibitor of histamine release induced by compound 48/80 and other polyamines. J Pharmacol Exp Ther. 1979;211(3):711-5.
Read, G. W., & Kiefer, E. F. (1979). Benzalkonium chloride: selective inhibitor of histamine release induced by compound 48/80 and other polyamines. The Journal of Pharmacology and Experimental Therapeutics, 211(3), 711-5.
Read GW, Kiefer EF. Benzalkonium Chloride: Selective Inhibitor of Histamine Release Induced By Compound 48/80 and Other Polyamines. J Pharmacol Exp Ther. 1979;211(3):711-5. PubMed PMID: 92563.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Benzalkonium chloride: selective inhibitor of histamine release induced by compound 48/80 and other polyamines. AU - Read,G W, AU - Kiefer,E F, PY - 1979/12/1/pubmed PY - 1979/12/1/medline PY - 1979/12/1/entrez SP - 711 EP - 5 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 211 IS - 3 N2 - Benzalkonium chloride (BAC) is a mixture of quaternary benzyldimethylalkylammonium chlorides which was found to inhibit histamine release induced by polyamines (48/80, ATP, bradykinin, curare, guanethidine, polylysine, polymyxin B, poly-THIQ, protamine, stilbamidine or substance P), but not that caused by antigens, concanavalin A, dextran, lonophores (A23187 or X-537A), enzymes (chymotrypsin or phospholipase C), monoamines (dextromethorphan, meperidine or chlorpromazine) or detergents (decylamine, Triton X-100 or a fire ant venom alkylpiperidine). Inhibition by 1.5 and 3 microgram of BAC per ml caused parallel shifts of the 48/80 dose-response curves to the right with no loss of efficacy, indicating that the antagonism was surmountable. Phospholipase C was partially inhibited by BAC, but Triton X-100 also inhibited phospholipase C (but not 48/80), indicating that the inhibition of phospholipase C by BAC was probably a nonspecific, detergent effect. BAC caused histamine release by itself at concentrations over 5 microgram/ml. Heat inactivation (50 degrees C for 15 min) of the mast cells did not prevent this release, suggesting a lytic mechanism for this action. Structure-activity relations studies on various members of the BAC family for their ability to inhibit 48/80-induced histamine release indicated that benzyldimethyltridecylammonium chloride was the most potent. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/92563/Benzalkonium_chloride:_selective_inhibitor_of_histamine_release_induced_by_compound_48/80_and_other_polyamines_ L2 - https://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=92563 DB - PRIME DP - Unbound Medicine ER -