生物活性
Olanzapine (Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. It has a higher affinity for 5-HT2 serotonin receptors than D2 dopamine receptors. Like most atypical antipsychotics, compared to the older typical ones, olanzapine has a lower affinity for histamine, cholinergic muscarinic and alpha adrenergic receptors. Olanzapine also exhibits weak affinity for GABAA, BZD receptor site which may contribute slightly to its sedating properties. Antagonizing H1 histamine receptors causes sedation and may cause weight gain, although antagonistic actions at 5-HT2C receptors have also been implicated in weight gain.
化学数据
分子量 | 312.44 |
分子式 | C17H20N4S |
CAS号 | 132539-06-1 |
纯度 | 99.93% |
溶解性(25°C) | DMSO 60 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 |
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 | 3.2006 mL | 16.0031 mL | 32.0061 mL |
5 mM | 0.6401 mL | 3.2006 mL | 6.4012 mL |
10 mM | 0.3201 mL | 1.6003 mL | 3.2006 mL |