YM 264
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- CAS号:
- 131888-54-5
- 英文名:
- YM 264
- 英文别名:
- Y-264;YM 264;YM 264,YM264
- 中文名:
- YM 264
- 中文别名:
- 化合物 YM-264;化合物 T13369
- CBNumber:
- CB01360020
- 分子式:
- C24H32N4OS.C4H4O4
- 分子量:
- 540.681
- MOL File:
- 131888-54-5.mol
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YM 264化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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YM 264性质、用途与生产工艺
YM-264 是一种有口服活性的、血小板活化因子 (PAF) 的有效选择性拮抗剂,其在兔子血小板膜上的 pKi 值为 8.85。
pKi: 8.85 (PAF, rabbit platelet membranes).
The anti-platelet-activating factor effect of YM-264 is examined in vitro. YM-264 inhibits [
3
H] platelet-activating factor binding to rabbit platelet membranes with a pK
i
value of 8.85. YM-264 inhibits the platelet-activating factor-induced human, rabbit and guinea-pig platelet aggregation with pA2 values of 8.68, 8.33 and 8.14, respectively.
There are no significant differences in baseline airway responsiveness between control and YM-264 treated groups. Airway hyperresponsiveness induced by antigen exposure is significantly inhibited by the administration of YM-264. The baseline Rrs is 0.40 (0.02) cm H
2
O/mL/s in the control group (n=6). In the YM-264 treated groups, the baseline Rrs is 0.39 (0.01) and 0.36 (0.01) cm H
2
O/mL/s at a doses of 1 mg/kg (n=5) and 3 mg/kg (n=6), respectively. The Rrs during the IAR significantly increase from baseline to 0.92 (0.10) cm H
2
O/mL/s in control (p=0.0002), 0.81 (0.12) in YM-264 1 mg/kg (p=0.01), and 1.06 (0.29) in YM-264 3 mg/kg (p=0.048). Reelevation of Rrs in the late phase is observed in the control group after antigen challenge. At this phase, Rrs significantly increase to 0.72 (0.10) cm H
2
O/mL/s (p=0.0101) from the baseline (0.40) at 6 h after the exposure of antigen. In contrast, YM-264 at the doses of 1 and 3 mg/kg show significant inhibition of reelevation of Rrs as compared with control. YM-264 inhibit the eosinophil infiltration dose dependently.
YM 264
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上游原料
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131888-54-5, YM 264 相关搜索:
- 抑制剂
- 化合物 YM-264
- 化合物 T13369
- 131888-54-5
- YM 264,YM264
- Y-264
- YM 264