| 产品描述: | Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects. |
| 靶点: |
5-HT1A Receptor;5-HT1A Receptor:24 nM (EC50) |
| 体外研究: |
Flesinoxan acts as a partial agonist at postsynaptic and as a full agonist at presynaptic 5-HT1A receptors. The capacity of Flesinoxan to antagonize the effect of 5-HT on CA3 pyramidal neurons was similar to that of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT). The intravenous administration of Flesinoxan suppresses the firing activity of both CA3 pyramidal neurons and dorsal raphe 5-HT neurons. The acute brain penetration of [3H]Flesinoxan and [3H]8-OH-DPAT are determined. Nine minutes after intravenous administration, [3H]8-OH-DPAT reached significantly greater brain concentration than [3H]Flesinoxan. Subcutaneous administration of Flesinoxan and 8-OH-DPAT produce a dose-dependent hypothermia. The Flesinoxan-induced hypothermia is significantly attenuated by prior administration of the non-selective 5-HT1A antagonist pindolol and the 5-HT1/2 antagonist methysergide. Similar degrees of hypothermia are achieved with 3 mg/kg of Flesinoxan and 0.5 mg/kg of 8-OH-DPAT. The maximal effect of Flesinoxan occurs 30 min later than that of 8-OH-DPAT and fades more slowly. |
| 参考文献: |
1. Hadrava V, et al. Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study. Neuropharmacology. 1995 Oct;34(10):1311-26. |
| 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 |
2.407 ml |
12.035 ml |
24.07 ml |
| 5 mM |
0.481 ml |
2.407 ml |
4.814 ml |
| 10 mM |
0.241 ml |
1.203 ml |
2.407 ml |
| 50 mM |
0.048 ml |
0.241 ml |
0.481 ml |
|
| 注意: |
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