产品描述: | Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine. IC50: Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) Receptor Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems |
靶点: |
5-HT1B Receptor;5-HT1D Receptor;5-HTReceptor |
参考文献: |
1. Bou J , et al. Pharmacological characterization of almotriptan: an indolic 5-HT receptor agonist for the treatment of migraine. Eur J Pharmacol, 2000. 410(1): p. 33-41. 2. Gras J, et al. Safety profile of almotriptan, a new antimigraine agent. Effects on central nervous system, renal function and respiratory dynamics. Arzneimittelforschung, 2001. 51(9): p. 726-32. |
溶解性: |
DMSO : 100 mg/mL (212.97 mM; Need ultrasonic) H2O : 33.33 mg/mL (70.98 mM; Need ultrasonic) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.13 ml |
10.648 ml |
21.297 ml |
5 mM |
0.426 ml |
2.13 ml |
4.259 ml |
10 mM |
0.213 ml |
1.065 ml |
2.13 ml |
50 mM |
0.043 ml |
0.213 ml |
0.426 ml |
|
注意: |
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