| 产品描述: | LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM |
| 靶点: |
5-HT Receptor;5-HTReceptor |
| 体内研究: |
Following intravenous administration of LY334370 at 3 mg/kg (n=3) or 10 mg/kg (n=6) electrical stimulation evokes an increase in dural blood vessel diameter of 135±6% and 106±11%, respectively, which is not significantly different from the respective control values. LY334370 has no effect on dural blood vessel diameter per se because the actual dural blood vessel diameter is 43±4 arbitrary units before drug and 43±4 arbitrary units 15 min after injection of LY334370 (10 mg/kg). |
| 细胞实验: |
For in vitro studies, LY334370 is dissolved in buffer solution.Human cerebral artery is used in this study. Segments are prepared as previously described, but briefly they are placed in a buffer solution containing (mM) NaCl 119, NaHCo3 15, KCl 4.6, CaCl2 1.5, NaH2PO4 1.2, MgCl2 1.2, and glucose 5.5. Sections of vessel about 0.5 mm in diameter and 1 to 2 mm in length are mounted in a temperature-controlled tissue bath (37°C) containing buffer solution bubbled with 95% O2 and 5% CO2. The vessel segments are given a tension of 4 mN and allowed to stabilize at this tension for 1 to 1.5 h. Vessel reactivity is tested by exposure to 60 mM KCl. This is done twice for each segment and only if the response is similar to the segment used for LY334370 testing. Responses to LY334370 is calculated as a percentage of the maximum KC1 response. |
| 动物实验: |
LY334370 is dissolved in 0.9% saline and is administered at a volume of 1 mL/kg. Male Sprague-Dawley rats (300 to 400 g) are treated with LY334370 (3 or 10 mg/kg, iv.). |
| 参考文献: |
1. Shepheard S, et al. Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370. Cephalalgia. 1999 Dec;19(10):851-8. |
| 溶解性: |
Soluble in DMSO |
| 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 |
2.846 ml |
14.228 ml |
28.456 ml |
| 5 mM |
0.569 ml |
2.846 ml |
5.691 ml |
| 10 mM |
0.285 ml |
1.423 ml |
2.846 ml |
| 50 mM |
0.057 ml |
0.285 ml |
0.569 ml |
|
| 注意: |
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