| 产品描述: | Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects. |
| 靶点: |
human 5-HT1B Receptor:1.7 nM (IC50); human 5-HT1D Receptor:1.3 nM (IC50); 5-HT1B Receptor:0.9 nM (Kd); 5-HT1D Receptor:1.2 nM (Kd) |
| 体外研究: |
The intraperitoneal administration of Alniditan ED50=9 μg/kg dose dependly reduces [125I]-BSA extravasation in the rat meninges when done 30 min before stimulation. Alniditan dose dependently attenuateds the neurogenic inflammation in vivo model of neurogenic inflammation[1]. |
| 体内研究: |
In vitro, Alniditan exhibits little vasoconstrictive effects on the rat basilar artery, although at a very high concentration 1 mM, Alniditan causes intensive constriction, most likely through a mechanism independent from 5-HT receptor activation. |
| 参考文献: |
1. Limmroth V, et al. Effects of alniditan on neurogenic oedema in the rat dura mater and on contraction of rat basilar artery. Eur J Pharmacol. 1999 Oct 8;382(2):103-9. 2. Lesage AS, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65. |
| 保存条件: |
2-8°C, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.664 ml |
13.321 ml |
26.643 ml |
| 5 mM |
0.533 ml |
2.664 ml |
5.329 ml |
| 10 mM |
0.266 ml |
1.332 ml |
2.664 ml |
| 50 mM |
0.053 ml |
0.266 ml |
0.533 ml |
|
| 注意: |
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