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Effects of thiazinamium chloride on histamine release from rat peritoneal mast cells and on phosphodiesterase activity in guinea pig lung.
Int Arch Allergy Appl Immunol. 1986; 81(4):348-50.IA

Abstract

The effect of thiazinamium Cl (TCl) on histamine release from rat peritoneal mast cells (RPMC) was investigated. Although TCl inhibited compound 48/80-induced histamine release moderately (IC50 value 40 microM), the drug was a weaker inhibitor of ovalbumin-induced histamine release (100 microM, -21%). In contrast, promethazine HCl (PHCl) was more effective against antigen-induced histamine release (IC50 value 13 microM) than against compound 48/80-induced histamine release (100 microM, -53%). Disodium cromoglycate (DSCG) was effective against both antigen and compound 48/80-induced release of histamine with IC50 values of 7 and 1 microM, respectively. Neither TCl nor DSCG at 1 mM increased spontaneous release of histamine from RPMC, whereas PHCl induced spontaneous release by over 50% at 1 mM. TCl did not inhibit phosphodiesterase (PDE) activity in guinea pig lung at 1 mM, whereas theophylline and DSCG inhibited PDE with IC50 values of 1.1 and 0.32 mM, respectively. These data suggest that high local concentrations of TCl may reduce histamine release during an asthmatic attack and improve its effectiveness as a bronchoprotectant.

Authors

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Pub Type(s)

Journal Article

Language

eng

PubMed ID

2430893

Citation

Carlson, R P., et al. "Effects of Thiazinamium Chloride On Histamine Release From Rat Peritoneal Mast Cells and On Phosphodiesterase Activity in Guinea Pig Lung." International Archives of Allergy and Applied Immunology, vol. 81, no. 4, 1986, pp. 348-50.
Carlson RP, O'Neill-Davis L, Chang J, et al. Effects of thiazinamium chloride on histamine release from rat peritoneal mast cells and on phosphodiesterase activity in guinea pig lung. Int Arch Allergy Appl Immunol. 1986;81(4):348-50.
Carlson, R. P., O'Neill-Davis, L., Chang, J., & Lewis, A. J. (1986). Effects of thiazinamium chloride on histamine release from rat peritoneal mast cells and on phosphodiesterase activity in guinea pig lung. International Archives of Allergy and Applied Immunology, 81(4), 348-50.
Carlson RP, et al. Effects of Thiazinamium Chloride On Histamine Release From Rat Peritoneal Mast Cells and On Phosphodiesterase Activity in Guinea Pig Lung. Int Arch Allergy Appl Immunol. 1986;81(4):348-50. PubMed PMID: 2430893.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of thiazinamium chloride on histamine release from rat peritoneal mast cells and on phosphodiesterase activity in guinea pig lung. AU - Carlson,R P, AU - O'Neill-Davis,L, AU - Chang,J, AU - Lewis,A J, PY - 1986/1/1/pubmed PY - 1986/1/1/medline PY - 1986/1/1/entrez SP - 348 EP - 50 JF - International archives of allergy and applied immunology JO - Int Arch Allergy Appl Immunol VL - 81 IS - 4 N2 - The effect of thiazinamium Cl (TCl) on histamine release from rat peritoneal mast cells (RPMC) was investigated. Although TCl inhibited compound 48/80-induced histamine release moderately (IC50 value 40 microM), the drug was a weaker inhibitor of ovalbumin-induced histamine release (100 microM, -21%). In contrast, promethazine HCl (PHCl) was more effective against antigen-induced histamine release (IC50 value 13 microM) than against compound 48/80-induced histamine release (100 microM, -53%). Disodium cromoglycate (DSCG) was effective against both antigen and compound 48/80-induced release of histamine with IC50 values of 7 and 1 microM, respectively. Neither TCl nor DSCG at 1 mM increased spontaneous release of histamine from RPMC, whereas PHCl induced spontaneous release by over 50% at 1 mM. TCl did not inhibit phosphodiesterase (PDE) activity in guinea pig lung at 1 mM, whereas theophylline and DSCG inhibited PDE with IC50 values of 1.1 and 0.32 mM, respectively. These data suggest that high local concentrations of TCl may reduce histamine release during an asthmatic attack and improve its effectiveness as a bronchoprotectant. SN - 0020-5915 UR - https://www.unboundmedicine.com/medline/citation/2430893/Effects_of_thiazinamium_chloride_on_histamine_release_from_rat_peritoneal_mast_cells_and_on_phosphodiesterase_activity_in_guinea_pig_lung_ DB - PRIME DP - Unbound Medicine ER -