| 名称 | LY334370 |
| 描述 | LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM |
| 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. |
| 激酶实验 | AlphaScreen Assay: All reagents are diluted in 50 mM HEPES, 0.1% BSA, pH 7.5 supplemented with 0.01% Tween20 and allowed to equilibrate to room temperature prior to addition to plates. Catalytic turnover assays are run in 10 μL volumes in lowvolume 384-well plates at RT. The reaction consisted of enzyme (5 nM), biotinylated substrate peptide (30 nM), Fe(II) (1 μM), ascorbate (100 μM), 2OG (10 μM) and run at RT. For PHD2, the reaction consisted of enzyme (5 nM), biotinylated substrate peptide (60 nM), Fe(II) (20 μM), ascorbate (200 μM), 2OG (2 μM) and run at RT. EDTA is used to quench the reaction (5 μL), AlphaScreen donor (Streptavidin-conjugated) and acceptor (Protein A-conjugated) beads preincubated with peptide product antibodies are added (5 μL). Plates are foil-sealed to protect from light, incubated at room temperature for 60 minutes and read on a PHERAstar FS plate reader using an AlphaScreen 680 excitation/570 emission filter set. The final bead concentration in 20 μL reaction is 20 μg/mL. IC50 values are calculated in Prism 6 after normalisation against corresponding DMSO controls. |
| 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.). |
| 体外活性 | LY334370在体外对人脑动脉不表现出血管收缩效应，直至剂量达到10^-5 M，此时可触发8.5±5.7%的收缩率，但此结果并不显著。 |
| 体内活性 | 经静脉注射LY334370后，以3 mg/kg (n=3) 或10 mg/kg (n=6) 剂量进行电刺激，可以观察到硬脑膜血管直径分别增加至135±6%和106±11%，这与各自的对照值无显著差异。LY334370本身对硬脑膜血管直径无影响，因为在药物注射前后15分钟，硬脑膜血管的实际直径分别为43±4任意单位和43±4任意单位（10 mg/kg）。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 50 mg/mL (142.28 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.69 mM), Sonication is recommended.
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| 关键字 | Serotonin Receptor | LY-334370 | LY334370 | Inhibitor | inhibit | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT1F | 5-HT Receptor | 5HT Receptor |
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