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Loxapine

现货
Catalog No.
B1001
5-HT受体拮抗剂
组合的产品项目
规格价格库存 数量
100mg
¥ 840.00
Ship with 10-15 days
500mg
¥ 2,880.00
Ship with 10-15 days

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Background

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.

文献引用

1. Perez-Gomez A, Carretero M, et al. "A phenotypic Caenorhabditis elegans screen identifies a selective suppressor of antipsychotic-induced hyperphagia." Nat Commun. 2018 Dec 10;9(1):5272. PMID:30532051

Chemical Properties

StorageStore at -20°C
M.Wt327.81
Cas No.1977-10-2
FormulaC18H18ClN3O
SolubilitySoluble in DMSO
Chemical Name8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine
SDFDownload SDF
Canonical SMILESCN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

大鼠胶质细胞和小胶质细胞

制备方法

上述化合物可溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.2、2和20 μM;1和3天

实验结果

在LPS激活的大鼠神经胶质细胞和小胶质细胞混合培养物中,Loxapine在指定浓度下减少IL-1β分泌。Loxapine还减少了胶质细胞混合培养物中的IL-2分泌。此外,在LPS诱导的小胶质细胞培养物中,给予0.2、2和20 μM Loxapine,于第1天和第3天,IL-1β和IL-2分泌均减少。

动物实验 [2]:

动物模型

Wistar大鼠

给药剂量

5 mg/kg;腹腔注射

实验结果

在Wistar大鼠中,慢性给予Loxapine 4周或10周,不能增加纹状体多巴胺受体密度。然而,Loxapine显著降低皮层血清素受体密度 (50 ~ 60%)。此外,单次给予Loxapine也显示出类似的强效作用。上述结果表明,Loxapine通过血清素系统发挥作用

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

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.

质量控制

质量控制和MSDS

批次:

化学结构

Loxapine

相关生物数据

Loxapine