Loxapine
(Synonyms: 洛沙平) 目录号 : GC13081
洛沙平是一种口服活性多巴胺抑制剂、5-HT 受体拮抗剂，也是一种二苯并沙西平抗精神病药物。
Cas No.:1977-10-2
Sample solution is provided at 25 µL, 10mM.
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Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent [1].
In vitro: Loxapine was a typical neuroleptic that showed great structural and functional homology to the atypical antipsychotic clozapine. Chronic loxapine treatment was usually associated with extrapyramidal symptoms (EPS). Loxapineexihibited an extremely strong binding affinity fordopamineD4 andserotonin5-HT2receptors, suggesting that both serotonergic and dopaminergic mechanisms contributed to the antipsychotic drug action and EPS associated with loxapine in the treatment of schizophrenia [1]. In frontal cortex of brain in human and bovine, in the presence of Loxapine, [3H]ketanserin bound to 5-HT2 receptor with ki value of 6.2 nM and 6.6 nM, respectively. In comparing competition experiments involving the human membranes, loxapine exihibited the rank order of potency for the various receptors as follows: 5-HT2≥D4>>>D1>D2 [1]. Loxapine administration at 0.2, 2 and 20 μMafter 1 and 3 days of exposure reduced IL-1βand IL-2 secretion by LPS-activated mixed glia cultures. Loxapine also decreased IL-1βand IL-2 secretion in LPS-induced microglia cultures [2].
In vivo: Chronic administration of loxapine(5 mg/kg) in rats for 4 weeks or 10 weeks significantly reduced more than 50% of serotonin (S2) receptor density. Loxapine (5 mg/kg) didn’t change dopamine receptor density but greatly reduced serotonin receptor density by 47% in the brain of rats [3].
References:
[1]. Singh AN1,Barlas C,Singh S,Franks P,Mishra RK. A neurochemical basis for the antipsychotic activity of loxapine: interactions withdopamineD1,D2, D4 andserotonin5-HT2receptorsubtypes.J Psychiatry Neurosci.1996 Jan;21(1):29-35.
[2]. Labuzek K1,Kowalski J,Gabryel B,Herman ZS. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures.Eur Neuropsychopharmacol.2005 Jan;15(1):23-30.
[3]. Lee T,Tang SW. Loxapine and clozapine decreaseserotonin(S2) but do not elevatedopamine(D2)receptornumbers in the rat brain.Psychiatry Res.1984 Aug;12(4):277-85.
| Cell experiment [1]: | |
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Cell lines |
Rat glial and microglial cells |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.2, 2 and 20 μM; 1 and 3 days |
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Applications |
In LPS-activated rat mixed glial and microglial cell cultures, Loxapine at all indicated concentrations reduced IL-1β secretion. Besides, Loxapine also reduced IL-2 secretion in mixed glia cultures. In addition, in LPS-induced microglia cultures, Loxapine decreased both IL-1β and IL-2 secretion at the concentrations of 0.2, 2 and 20 μM after the exposure of 1 and 3 days. |
| Animal experiment [2]: | |
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Animal models |
Wistar rats |
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Dosage form |
5 mg/kg; i.p. |
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Applications |
In Wistar rats, chronic administration of Loxapine for 4 weeks or 10 weeks did not increase striatal dopamine receptor density. However, Loxapine significantly reduced cortical serotonin receptor density by 50 ~ 60%. In addition, a single dose of Loxapine exhibited the same potent effect. The results suggested that Loxapine exerted its effect via the serotonin system. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Labuzek K1,Kowalski J,Gabryel B,Herman ZS. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures.Eur Neuropsychopharmacol.2005 Jan;15(1):23-30. [2]. Lee T,Tang SW. Loxapine and clozapine decreaseserotonin(S2) but do not elevatedopamine(D2)receptornumbers in the rat brain.Psychiatry Res.1984 Aug;12(4):277-85. | |
| Cas No. | 1977-10-2 | SDF | |
| 别名 | 洛沙平 | ||
| 化学名 | 8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine | ||
| Canonical SMILES | CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl | ||
| 分子式 | C18H18ClN3O | 分子量 | 327.81 |
| 溶解度 | DMSO : 66mg/mL | 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 | 3.0505 mL | 15.2527 mL | 30.5055 mL |
| 5 mM | 0.6101 mL | 3.0505 mL | 6.1011 mL |
| 10 mM | 0.3051 mL | 1.5253 mL | 3.0505 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet