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YM158 free base

CAS No. : 179102-65-9

MCE 站：YM158 free base

产品活性：YM158 free base 是一种有效的选择性 LTD₄ 和 TXA₂ 受体拮抗剂, pA₂ 值分别为 8.87 和 8.81。

研究领域：GPCR/G Protein

作用靶点：Leukotriene Receptor  |  Prostaglandin Receptor

In Vitro: YM158 antagonizes leukotriene (LT) D₄ ａnd thromboxane (TX) A₂ receptors. Functional assays in vitro show that YM158 exhibits competitive dual antagonism of LTD₄ ａnd TXA₂ receptor-mediated contraction of isolated guinea pig tracheae, with pA₂ values of about 8.87 ａnd 8.81, respectively. Its antagonistic activity for the LTD₄ receptor is approximately 6.5 times less potent than that of Montelukast, ａnd that for the TXA₂ receptor is 2.5 times more potent than that of Seratrodast. YM158 also inhibits PGD₂- ａnd PGF_2α -induced tracheal contractions. YM158 antagonizes the stable TXA₂ analog U46619-induced aggregation of both guinea pig ａnd human platelets ａnd inhibits the LTD₄-induced contraction of guinea pig ileum. YM158 produces a concentration-dependent inhibition of guinea pig ileum contraction induced by 1 nM LTD₄ with an IC₅₀ value of 0.58 nM.

In Vivo: YM158, an orally active dual antagonist for LTD₄ ａnd TXA₂ receptors, is expected to have a stronger antiasthmatic efficacy in a broader class of asthmatic patients than single antagonistic drugs.The effect of YM158 is examined on these asthmatic responses in mediator-controlled ａnd passively sensitized guinea pigs. Because the inhibitory effects of YM158 on increase in the airway resistance induced by LTD₄ or U46619 are shown to be dose-dependent when p.o. administered 1 h before LTD₄ or U46619 injection, with ED₅₀ values of 8.6 ａnd 14 mg/kg, respectively, the antagonistic activities of p.o. YM158 for LTD₄ ａnd TXA₂ receptors are exhibited at the same dose range. Oral YM158 shows significant effects, approximately the same as the combination of Pranlukast ａnd Daltroban on antigen-induced response under various conditions; namely, where LTD₄ is predominant, TXA₂ is predominant; or where both mediators participated equally. In groups not treated with Indomethacin, administration of Daltroban (10 mg/kg), a combination of Pranlukast (30 mg/kg) ａnd Daltroban (10 mg/kg), or YM158 (30 mg/kg) significantly prolongs the onset time for asthmatic response ａnd significantly suppresses symptoms.

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