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Characterization of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic acid Na] on histamine release from rat peritoneal mast cells induced by antigen, compound 48/80 and A 23187.
Agents Actions. 1985 Oct; 17(1):10-3.AA

Abstract

We studied the in vitro effects of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic acid Na] on histamine release from rat peritoneal mast cells. These cells exposed to ascaris antigen, compound 48/80 or the ionophore A 23187 concentration-dependently released histamine. About a 30-40% histamine release was obtained by 1 X 10(-4) g/ml of antigen, 1 X 10(-7) g/ml of compound 48/80 and A 23187. FPL-52694 (10(-9)-10(-4) g/ml) concentration-dependently inhibited the histamine release from mast cells in response to antigen (1 X 10(-4) g/ml) and compound 48/80 (1 X 10(-7) g/ml), but only slightly inhibited the histamine release induced by A 23187 (1 X 10(-7) g/ml). Similar results were obtained with disodium cromoglycate (DSCG), in the same dose ranges. However, the inhibitory activity of FPL-52694 on histamine release by antigen and compound 48/80 was approximately 10 times more potent than that of DSCG at certain concentrations. Tachyphylaxis was observed when these two agents were preincubated with mast cells for 10 min. These results show FPL-52694 to be a novel mast cell stabilizer.

Authors

Takeuchi K
No affiliation info available
Ohtsuki H
No affiliation info available
Nakagawa S
No affiliation info available
Okabe S
No affiliation info available

MeSH

AnimalsAntigensAscarisCalcimycinChromonesCromolyn SodiumDose-Response Relationship, DrugHistamine ReleaseIn Vitro TechniquesMaleMast CellsPeritoneal CavityRatsRats, Inbred Strainsp-Methoxy-N-methylphenethylamine

Pub Type(s)

Journal Article

Language

eng

PubMed ID

2417456

Citation

Takeuchi, K, et al. "Characterization of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic Acid Na] On Histamine Release From Rat Peritoneal Mast Cells Induced By Antigen, Compound 48/80 and a 23187." Agents and Actions, vol. 17, no. 1, 1985, pp. 10-3.
Takeuchi K, Ohtsuki H, Nakagawa S, et al. Characterization of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic acid Na] on histamine release from rat peritoneal mast cells induced by antigen, compound 48/80 and A 23187. Agents Actions. 1985;17(1):10-3.
Takeuchi, K., Ohtsuki, H., Nakagawa, S., & Okabe, S. (1985). Characterization of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic acid Na] on histamine release from rat peritoneal mast cells induced by antigen, compound 48/80 and A 23187. Agents and Actions, 17(1), 10-3.
Takeuchi K, et al. Characterization of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic Acid Na] On Histamine Release From Rat Peritoneal Mast Cells Induced By Antigen, Compound 48/80 and a 23187. Agents Actions. 1985;17(1):10-3. PubMed PMID: 2417456.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characterization of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic acid Na] on histamine release from rat peritoneal mast cells induced by antigen, compound 48/80 and A 23187. AU - Takeuchi,K, AU - Ohtsuki,H, AU - Nakagawa,S, AU - Okabe,S, PY - 1985/10/1/pubmed PY - 1985/10/1/medline PY - 1985/10/1/entrez SP - 10 EP - 3 JF - Agents and actions JO - Agents Actions VL - 17 IS - 1 N2 - We studied the in vitro effects of FPL-52694 [5-(2-hydroxypropoxyl)-8-propyl-4-oxo-4H-benzopyran-2-carboxylic acid Na] on histamine release from rat peritoneal mast cells. These cells exposed to ascaris antigen, compound 48/80 or the ionophore A 23187 concentration-dependently released histamine. About a 30-40% histamine release was obtained by 1 X 10(-4) g/ml of antigen, 1 X 10(-7) g/ml of compound 48/80 and A 23187. FPL-52694 (10(-9)-10(-4) g/ml) concentration-dependently inhibited the histamine release from mast cells in response to antigen (1 X 10(-4) g/ml) and compound 48/80 (1 X 10(-7) g/ml), but only slightly inhibited the histamine release induced by A 23187 (1 X 10(-7) g/ml). Similar results were obtained with disodium cromoglycate (DSCG), in the same dose ranges. However, the inhibitory activity of FPL-52694 on histamine release by antigen and compound 48/80 was approximately 10 times more potent than that of DSCG at certain concentrations. Tachyphylaxis was observed when these two agents were preincubated with mast cells for 10 min. These results show FPL-52694 to be a novel mast cell stabilizer. SN - 0065-4299 UR - https://www.unboundmedicine.com/medline/citation/2417456/Characterization_of_FPL_52694_[5__2_hydroxypropoxyl__8_propyl_4_oxo_4H_benzopyran_2_carboxylic_acid_Na]_on_histamine_release_from_rat_peritoneal_mast_cells_induced_by_antigen_compound_48/80_and_A_23187_ DB - PRIME DP - Unbound Medicine ER -