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Immunopharmacological studies on TBX, a new antiallergic drug (2). Inhibitory effects on histamine release from peritoneal mast cells and lung fragments of rats.
Jpn J Pharmacol. 1988 Sep; 48(1):103-12.JJ

Abstract

The ability of 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one potassium salt (TBX) to inhibit histamine release from both peritoneal exudate cells (PEC) containing mast cells and lung fragments of rats was investigated in vitro. Low concentrations of TBX dose-dependently inhibited IgE-mediated histamine release from PEC of passively sensitized animals; its IC50 was 5.1 x 10(-9) g/ml. When TBX was added simultaneously with the antigen challenge, the highest inhibition was obtained. In contrast, extension of preincubation time with the agent resulted in a marked decrease in the inhibition of histamine release. The potent inhibition of histamine release by TBX was observed equally in glucose-free as well as complete Tyrode's solution, whereas TBX reduced its inhibitory action in Ca2+-free or D2O-supplemented medium. In addition, TBX inhibited compound 48/80- but not calcium ionophore A23187-induced histamine release from normal PEC. With regard to the intracellular cyclic AMP level in normal PEC, it was significantly enhanced by a high concentration of TBX (10(-3) g/ml). TBX also inhibited antigen-induced histamine release from lung fragments of actively immunized animals. Interestingly, TBX displayed non-competitive inhibition of cyclic AMP-dependent phosphodiesterase derived from lung homogenates; its K1 value was 8.70 x 10(-4) M.

Authors+Show Affiliations

Clinical Research Center for Allergy, National Sagamihara Hospital, Kanagawa, Japan.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

2462073

Citation

Yanagihara, Y, et al. "Immunopharmacological Studies On TBX, a New Antiallergic Drug (2). Inhibitory Effects On Histamine Release From Peritoneal Mast Cells and Lung Fragments of Rats." Japanese Journal of Pharmacology, vol. 48, no. 1, 1988, pp. 103-12.
Yanagihara Y, Kasai H, Shida T. Immunopharmacological studies on TBX, a new antiallergic drug (2). Inhibitory effects on histamine release from peritoneal mast cells and lung fragments of rats. Jpn J Pharmacol. 1988;48(1):103-12.
Yanagihara, Y., Kasai, H., & Shida, T. (1988). Immunopharmacological studies on TBX, a new antiallergic drug (2). Inhibitory effects on histamine release from peritoneal mast cells and lung fragments of rats. Japanese Journal of Pharmacology, 48(1), 103-12.
Yanagihara Y, Kasai H, Shida T. Immunopharmacological Studies On TBX, a New Antiallergic Drug (2). Inhibitory Effects On Histamine Release From Peritoneal Mast Cells and Lung Fragments of Rats. Jpn J Pharmacol. 1988;48(1):103-12. PubMed PMID: 2462073.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Immunopharmacological studies on TBX, a new antiallergic drug (2). Inhibitory effects on histamine release from peritoneal mast cells and lung fragments of rats. AU - Yanagihara,Y, AU - Kasai,H, AU - Shida,T, PY - 1988/9/1/pubmed PY - 1988/9/1/medline PY - 1988/9/1/entrez SP - 103 EP - 12 JF - Japanese journal of pharmacology JO - Jpn J Pharmacol VL - 48 IS - 1 N2 - The ability of 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one potassium salt (TBX) to inhibit histamine release from both peritoneal exudate cells (PEC) containing mast cells and lung fragments of rats was investigated in vitro. Low concentrations of TBX dose-dependently inhibited IgE-mediated histamine release from PEC of passively sensitized animals; its IC50 was 5.1 x 10(-9) g/ml. When TBX was added simultaneously with the antigen challenge, the highest inhibition was obtained. In contrast, extension of preincubation time with the agent resulted in a marked decrease in the inhibition of histamine release. The potent inhibition of histamine release by TBX was observed equally in glucose-free as well as complete Tyrode's solution, whereas TBX reduced its inhibitory action in Ca2+-free or D2O-supplemented medium. In addition, TBX inhibited compound 48/80- but not calcium ionophore A23187-induced histamine release from normal PEC. With regard to the intracellular cyclic AMP level in normal PEC, it was significantly enhanced by a high concentration of TBX (10(-3) g/ml). TBX also inhibited antigen-induced histamine release from lung fragments of actively immunized animals. Interestingly, TBX displayed non-competitive inhibition of cyclic AMP-dependent phosphodiesterase derived from lung homogenates; its K1 value was 8.70 x 10(-4) M. SN - 0021-5198 UR - https://www.unboundmedicine.com/medline/citation/2462073/Immunopharmacological_studies_on_TBX_a_new_antiallergic_drug__2___Inhibitory_effects_on_histamine_release_from_peritoneal_mast_cells_and_lung_fragments_of_rats_ L2 - https://joi.jlc.jst.go.jp/JST.Journalarchive/jphs1951/48.103?from=PubMed DB - PRIME DP - Unbound Medicine ER -