AS-35

AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.

Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor

Research Areas >> Inflammation/Immunology

LTE4:3 nM (IC50, In isolated guinea pig ileum)

LTD4:4 nM (IC50, In isolated guinea pig ileum)

LTC4:8 nM (IC50, In isolated guinea pig ileum)

In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively. In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC50 values of 10 nM and 20 nM, respectively. However, AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate[1].

AS-35 (0.0375 to 0.3 mg/kg, i.v.) dose-dependently antagonizes bronchoconstriction induced by i.v.-injection of LTC4 and LTD4 in anesthetized guinea pigs, but does not inhibit histamine-induced bronchoconstriction. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig[1].

[1]. Kasai H, et al. Peptide leukotriene antagonistic activity of AS-35, a new antiallergic drug. Jpn J Pharmacol. 1992 Apr;58(4):347-55.

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