BMY 14802 hydrochloride
(Synonyms: BMY-14802-1; BMS 181100 hydrochloride) 目录号 : GC13796
BMY 14802 hydrochloride (BMY-14802-1) 是一种选择性和口服活性的 sigma 受体拮抗剂，IC50 为 112 nM。
Cas No.:105565-55-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 112 nM for (+)-[3H]-3-PPP
The theoretical role of sigma receptors in psychosis has led to the discovery of selective sigma receptor ligands as potential antipsychotic agents. BMY 14802 is a sigma receptor ligand.
In vitro: BMY 14802 has its most potent binding at the sigma binding site, with some degree of serotonin subtype 1A and negligible dopamine receptor binding [1].
In vivo: BMY 14802 is atypical of standard neuroleptics in that it does not induce catalepsy in rats. In addition, it has been shown to have efficacy in animal models of psychosis [1].
Clinical trial: After 1 week of single-blind placebo treatment, 28 patients were treated with BMY 14802 (up to 3000 mg/day) for up to 4 weeks. However, there was no significant improvement in psychiatric symptoms. There were no changes in involuntary movements, as measured by the Abnormal Involuntary Movement Scale, or in extrapyramidal symptoms as measured by the Simpson-Angus Scale [1].
Reference:
[1] Gewirtz GR, Gorman JM, Volavka J, Macaluso J, Gribkoff G, Taylor DP, Borison R. BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology. 1994 Feb;10(1):37-40.
| Cas No. | 105565-55-7 | SDF | |
| 别名 | BMY-14802-1; BMS 181100 hydrochloride | ||
| 化学名 | (R)-1-(4-fluorophenyl)-4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)butan-1-ol hydrochloride | ||
| Canonical SMILES | FC1=CN=C(N=C1)N2CCN(CCC[C@H](C(C=C3)=CC=C3F)O)CC2.Cl | ||
| 分子式 | C18H22F2N4O.HCl | 分子量 | 384.86 |
| 溶解度 | <9.62mg/ml in Water | 储存条件 | Desiccate at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5983 mL | 12.9917 mL | 25.9835 mL |
| 5 mM | 0.5197 mL | 2.5983 mL | 5.1967 mL |
| 10 mM | 0.2598 mL | 1.2992 mL | 2.5983 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。