An atypical antipsychotic
Cas No.:106516-24-9
Sample solution is provided at 25 µL, 10mM.
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Sertindole is an atypical antipsychotic that binds to dopamine D2 receptors and the serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 2.7, 20, 0.14, and 6 nM, respectively).1 It also binds to histamine H1 and α1- and α2-adrenergic receptors (Kds = 320, 3.9, and 190 nM, respectively). In vivo, sertindole (10 mg/kg) increases extracellular dopamine, acetylcholine (ACh), and glutamate levels in the medial prefrontal cortex in conscious rats.2 Sertindole (2.5 mg/kg) reverses ketamine-induced impairments in the extradimensional shift stage of the attentional set-shifting task (ASST) in rats.3 It reverses phencyclidine (PCP)-induced selective reversal learning deficits in rats and subchronic PCP-induced deficits in the novel object recognition task in mice.4 Sertindole (0.02-0.32 mg/kg) also prevents accuracy deficits and anticipatory over-responding in the 5-choice serial reaction time task (5CSRTT) induced by the NMDA receptor antagonist (R)-CPP in rats.5 Formulations containing sertindole have been used in the treatment of schizophrenia.
1.Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1)29-39(2000) 2.M?rk, A., Witten, L.M., and Arnt, J.Effect of sertindole on extracellular dopamine, acetylcholine, and glutamate in the medial prefrontal cortex of conscious rats: A comparison with risperidone and exploration of mechanisms involvedPsychopharmacol. (Berl)206(1)39-49(2009) 3.Nikiforuk, A., and Popik, P.Effects of quetiapine and sertindole on subchronic ketamine-induced deficits in attentional set-shifting in ratsPsychopharmacol. (Berl)220(1)65-74(2012) 4.Idris, N., Neill, J., Grayson, B., et al.Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: Involvement of 5-HT6 and 5-HT 2A receptor mechanismsPsychopharmacol. (Berl)208(1)23-36(2010) 5.Carli, M., Calcagno, E., Mainini, E., et al.Sertindole restores attentional performance and suppresses glutamate release induced by the NMDA receptor antagonist CPPPsychopharmacol. (Berl)214(3)625-637(2011)
| Cas No. | 106516-24-9 | SDF | |
| 别名 | 舍吲哚; Lu 23-174 | ||
| Canonical SMILES | FC1=CC=C(N2C3=CC=C(Cl)C=C3C(C4CCN(CCN5CCNC5=O)CC4)=C2)C=C1 | ||
| 分子式 | C24H26ClFN4O | 分子量 | 440.94 |
| 溶解度 | DMSO : 50 mg/mL (113.39 mM) | 储存条件 | Store at -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2679 mL | 11.3394 mL | 22.6788 mL |
| 5 mM | 453.6 μL | 2.2679 mL | 4.5358 mL |
| 10 mM | 226.8 μL | 1.1339 mL | 2.2679 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet