生物活性
BRL-15572 is a hydrochloride salt form of BRL-15572 which is a selective serotonin receptor subtype 5-HT1D antagonist with an IC50 of 260 μM. BRL-15572 indicates 60-fold selectivity over h5-HT1B, and displays little or no affinity for a range of other receptor types. In the presence of the 5-HT1D antagonist BRL15572 at a dose of 10 μM triggered a significant reduction in evoked IPSC (inhibitory postsynaptic currents) amplitude. Additionally, the antianti-migraine agent sumatriptan (1 μM) produced a striking reduction in evoked IPSC amplitude in the presence of BRL15572 (10 μM) which was not significantly different to that produced in its absence. For a comparison, sumatriptan (1 μM) did not produce a marked reduction in evoked IPSC amplitude in the presence of both NAS181 (10 μM) and BRL15572 (10 μM). In addition, it was observed that the prevention of GABAergic synaptic transmission produced by 5-HT was abolished by the 5-HT1B antagonist NAS181, but not by the 5-HT1A and 5-HT1D antagonists WAY100135 and BRL15572, while that produced by sumatriptan was only abolished in the combined presence of NAS181 and BRL15572.
化学数据
| 分子量 | 479.87 |
| 分子式 | C25H27ClN2O.2HCl |
| CAS号 | 193611-72-2 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 90 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | CHO cells expressing the h5-HT1B or h5-HT1D receptors |
| 方法 | [35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 μ M), with or without BRL-15572. Starting the reaction by the addition of 10 μL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Determing Non-specific binding by addition of unlabelled GTPγS (10 μM), prior to the addition of cells. Stoping the reaction by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Determining radioactivity by liquid scintillation spectrometry |
| 浓度 | 0 μM -10 μM |
| 处理时间 | 30 minutes |
| 动物实验 |
|---|
| 动物模型 | Male Wistar rats with diabetes |
| 配制 | 20% propylene glycol |
| 剂量 | 1 mg/kg, 2 mg/kg |
| 给药处理 | Administered via i.v. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0839 mL | 10.4195 mL | 20.839 mL |
| 5 mM | 0.4168 mL | 2.0839 mL | 4.1678 mL |
| 10 mM | 0.2084 mL | 1.0419 mL | 2.0839 mL |
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