Anti-Allergic Activities of a New Benzopyranopyridine Derivative Y-12,141 in Rats

Abstract

Passive cutaneous anaphylaxis (PCA) mediated in rats by IgE-like antibodies against egg albumin or the benzylpenicilloyl determinant was inhibited in a dose-dependent manner by intravenous treatment with Y-12,141; the ED50 was 0.09–0.2 mg/kg. The inhibitory effect of Y-12,141 on PCA was about 5 times as potent as that of disodium cromoglycate (DSCG). Oral treatment with Y-12,141 resulted in the inhibition of PCA, showing an ED₅₀ of 2.5 mg/kg. This action of Y-12,141 on PCA was considered to be due to the inhibition of the release of allergic mediators from mast cells in a manner similar to DSCG. The present results suggest that Y-12,141 may have an anti-allergic activity.

Anti-anaphylactic activities of a new benzopyranopyridine derivative Y-12,141 in rats and guinea pigs.

“…In addition, we found that Y-12,141 did not inhibit the antigen-antibody reaction (20). In these respects, Y-12,141 is different from DSCG and mepyramine.…”

Stimulation of phagocytic activity of leukocytes and macrophages by traxanox sodium in mice and rats.

“…In addition, traxanox sodium has anti asthmatic activity (1,2). In adult chronic asthmatics, prednisolone can decrease the airway resistance and theophylline and iso proterenol can improve the arterial oxygen tension (18,19).…”

“…A new synthetic compound, traxanox (9 chloro-5-oxo-7-(1 H-tetrazol-5-yl)-5H [1 ] benzopyrano- [2,3-b]pyridine) sodium penta hydrate has been shown to possess anti anaphylactic effects (1,2). This agent has also been shown to enhance the production of spleen and thymus-rosette forming cells in C57BL/6 mice (3), a lower responder to sheep red blood cells (SRBC), and to inhibit that in BALB/c mice (4), a higher responder mice to SRBC.…”

Traxanox augments immune response to lipopolysaccharide in inbred mice: Role of macrophages.

“…In the previous papers, we have reported that Y-1 2,141 (9-chloro-5-oxo-7-(1 H tetrazol-5-yl)-5H- [1 ]benzopyrano [2,3-b] pyridine sodium salt pentahydrate, traxanox sodium pentahydrate**)…”

“…The anti anaphylactic effect of this agent was sug gested to be due to an inhibition of release of allergic mediators such as histamine and slow reacting substance of anaphylaxis (1)(2)(3). Traxanox sodium has been suggested to have a capacity to suppress the IgE production in the BN rat (4) and to potentiate immune responses in dd mice immunized with low doses of sheep red blood cells (SRBC) (5).…”