| 产品描述: | H1 受体选择性抑制剂| 激动剂 | 拮抗剂;H1 receptor Selective Inhibitors | Agonists | Antagonists;;InformationEmedastine is a potent, high affinityhistamine H1-receptor-selectiveantagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).TargetsH1 receptor (Cell-free assay) 1.3 nM(Ki)In vitroEmedastine is capable of potently inhibiting histamine-induced cytokine release as well as the chemotaxis of eosinophils, thereby influencing factors contributing to the inhibition of the signs and symptoms of allergic diseases.In vivoIn human, the half-life of emedastine, when administered as slow release capsules is of about 6±7 h. |
| 体内研究: |
Emedastine (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg. Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B. Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs. Emedastine inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM). |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.307 ml |
16.534 ml |
33.068 ml |
| 5 mM |
0.661 ml |
3.307 ml |
6.614 ml |
| 10 mM |
0.331 ml |
1.653 ml |
3.307 ml |
| 50 mM |
0.066 ml |
0.331 ml |
0.661 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |