Effects of Thiazinamium Chloride on Histamine Release from Rat Peritoneal Mast Cells and on Phosphodiesterase Activity in Guinea Pig Lung
| Autor: | Richard P. Carlson, Lynn O’Neill-Davis, Alan J. Lewis, Joseph Chang |
|---|---|
| Rok vydání: | 1986 |
| Předmět: |
medicine.medical_specialty
Immunology Histamine Release Promethazine Guinea pig chemistry.chemical_compound Theophylline Cricetinae Internal medicine Cromolyn Sodium medicine Animals Immunology and Allergy Mast Cells Histamine H4 receptor Lung IC50 business.industry Phosphodiesterase General Medicine Mast cell Endocrinology medicine.anatomical_structure chemistry 3' 5'-Cyclic-AMP Phosphodiesterases Liberation business Histamine medicine.drug |
| Zdroj: | International Archives of Allergy and Immunology. 81:348-350 |
| ISSN: | 1423-0097 1018-2438 |
| DOI: | 10.1159/000234161 |
| Popis: | 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 μM), the drug was a weaker inhibitor of ovalbumin-induced histamine release (100 μM, ––21 %). In contrast, promethazine HCl (PHCl) was more effective against antigen-induced histamine release (IC50 value 13 μM) than against compound 48/80-induced histamine release (100 μM, ––53%). Disodium cromoglycate (DSCG) was effective against both antigen and compound 48/80-induced release of histamine with IC50 values of 7 and 1 μM, 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. |
| Databáze: | OpenAIRE |
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