Studies on a new antiallergic pyridinecarboxamide TA-5707F and its sodium salt (TA-5707). II. Mechanism of antiallergic action of TA-5707.

  title={Studies on a new antiallergic pyridinecarboxamide TA-5707F and its sodium salt (TA-5707). II. Mechanism of antiallergic action of TA-5707.},
  author={K. Tsuzurahara and S. Ishikawa and Y. Ono and T. Murata and M. Kikuchi and S. Takeyama},
  journal={Japanese journal of pharmacology},
  volume={45 1},
Mechanism of the antiallergic action of 6-methyl-N-(1H-tetrazol-5-yl)-2-pyridinecarboxamide (TA-5707F) was studied using the water-soluble sodium salt (TA-5707). 1) TA-5707 administered p.o. at the dose ca. 3 times the ID50 for the PCA reaction did not inhibit capillary dye leakage induced on the rat skin by intracutaneous injection of histamine, serotonin, bradykinin and leukotriene D4 (LTD4). 2) TA-5707, at concentrations above 10(-7) M, inhibited antigen-induced histamine release and dye… Expand
1 Citations
The title compound, C20H14F4N4O2, has been synthesized as part of our ongoing investigations into three-dimensional supra­molecules or polymers with intriguing structural topologies and properties.Expand


Studies on a new antiallergic pyridinecarboxamide TA-5707F and its sodium salt (TA-5707). I. Inhibition of IgE-induced passive cutaneous anaphylaxis (PCA) in rats.
Both TA- 5707 and TA-5707F were found to be orally effective inhibitors of rat PCA and maximum activity by oral administration was obtained when they were administered 5 min before the challenge, and under these conditions were both approximately 1 mg/kg. Expand
Antiallergic action of 6-ethyl-3-(1h-tetrazol-5-YL) chromone (AA-344) on immediate hypersensitivity reaction in rats.
The results indicate that the inhibitory action of AA-344 on the immediate hypersensitivity reactions is due to prevention of the release of chemical mediators from the mast cells, by acting on some process in sequential events leading to the mediator release following antigen-antibody combination. Expand
Clinical pharmacological evaluation of a new anti-allergic agent, TA-5707, by skin and nasal provocation tests.
The clinical effect of a new orally active anti-allergic agent, coded TA-5707 and chemically designed as 6-methyl-N-(1H-tetrazol-5-y1)-2-pyridine carboxamide sodium salt, was investigated in 12 male patients with allergic rhinitis, finding the inhibitory effect was stronger after 2 hr of administration than after 1hr of administration. Expand
Antiallergic effects of the adrenergic beta-stimulant trimetoquinol in rats and guinea pigs.
Results indicate that TMQ and Iso inhibit the anaphylactic reactions by β-adrenergic mechanisms, probably of a β2-type. Expand
Increased vascular permeability during passive peritoneal anaphylaxis in the rat. The effects of disodium cromoglycate and a nitroindanedione.
Following intraperitoneal sensitisation of rats with rat serum containing reaginic antibody, intravenous injection of blue dye and intraperitoneal challenge with antigen caused a release ofExpand
Species difference in increased vascular permeability by synthetic leukotriene C4 and D4.
Results show that species difference is present in activity of LTC4 and LTD4 in vascular permeability, which was not affected after pretreatment with pyrilamine or bradykinin. Expand
Passive anaphylaxis in human lung fragments as a model for testing anti-allergic drugs: its variability and constraints.
Although theoretically a very appropriate model of allergic asthma, passive anaphylaxis in human lung fragments is quantitatively inconsistent and gives only a gross indication of drug efficacy. Expand
Inhibiting effect of desensitization on release of histamine from guinea pig lung by specific antigen.
Abstract Guinea pigs passively sensitized by intrathoracic injection of rabbit antiserum were subsequently desensitized by parenteral introduction of sublethal doses of antigen, and the amount ofExpand
Modulation of cyclic AMP in purified rat mast cells. I. Responses to pharmacologic, metabolic, and physical stimuli.
In these homogeneous single cell suspensions, cholinergic and beta adrenergic agents have opposing effects on cAMP levels, and the availability of highly purified mast cells and the identification of agents which either decrease or increase cAMP content allows a direct examination of the role of cAMP in histamine release. Expand
A method for the fluorometric assay of histamine in tissues.
Gross dissection of brain showed no marked localization of brain histamine and a sensitive and specific fluorometric method for the estimation of histamine in tissues was described. Expand