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Loxapine succinate

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Chemical Structure| 27833-64-3 同义名 : 丁二酸洛沙平 ;CL 71,563;Loxapine (succinate);Succinate, Loxapine;Oxilapine;Maleate, Loxipine;Daxolin;Cloxazepin;Loxapac;Loxapine succinate salt;NSC 759578
CAS号 : 27833-64-3
货号 : A945672
分子式 : C22H24ClN3O5
纯度 : 99%
分子量 : 445.896
MDL号 : MFCD00069298
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(235.48 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2.5 mg/mL(5.61 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • 5-HT2

    5-HT2 (human), Ki:6.8 nM

    5-HT2 (bovine), Ki:6.6 nM

  • D4 receptor

    D4 receptor (human), Ki:7.5 nM

  • D1 receptor

    D1 receptor (human), Ki:26 nM

    D2 receptor (Human), Ki:62 nM

  • D2 receptor

    D2 receptor (human), Ki:24 nM

    D2 receptor (bovine), Ki:26 nM
描述 Loxapine succinate, the succinate form of loxapine, is a kind of typical antipsychotic. In vitro studies, it was found that loxapine succinate showed high affinity for the human recombinant D2 receptor, intermediate affinity for the D1, D4, D5 and 5-HT2C receptors, and low affinity toward D3, 5-HT1A, 5-HT4, 5-HT6 and 5-HT7 receptors in transfected CHO cells and HEK-293 cells, which demonstrated that loxapine should be rightly classified as a DS-RAn agent in the neuroscience based nomenclature classification[3]. Besides this, loxapine could inhibit the sodium-potassium ATPase activity by 25-35% at 0.1mM in rat brain[4]. In vivo studies, loxapine could contribute to the significant depression of the paradoxical sleep (PS) with maximal within 30min and lasting about 24hr in Wistar albino rats, while only slightly influence the synchronized sleep, when given 0.4–1.6mg/kg in one single dose. In addition, loxapine could also affect the frequency and mean duration of PS episodes[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.21mL

2.24mL

1.12mL

22.43mL

4.49mL

2.24mL
参考文献

[1]Labuzek K, Kowalski J, et al. 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]Singh AN, Barlas C, et al. A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes. J Psychiatry Neurosci. 1996 Jan;21(1):29-35.

[3]Ferreri F, Drapier D, Baloche E, Ouzid M, Zimmer L, Llorca PM. The in Vitro Actions of Loxapine on Dopaminergic and Serotonergic Receptors. Time to Consider Atypical Classification of This Antipsychotic Drug? Int J Neuropsychopharmacol. 2018 Apr 1;21(4):355-360. doi: 10.1093/ijnp/pyx102. PMID: 29106549; PMCID: PMC5887516.

[4]Velasco-Martín A, Garcia JL, Dueñas A. Effects of several neuroleptics, antidepressants and monoamine uptake blockers on ATPase activity and related oxygen uptake in rat brain in vitro. Methods Find Exp Clin Pharmacol. 1989 Dec;11(12):737-41. PMID: 2576298.

[5]Schmidek WR, Timo-Iaria C, Schmidek M, Krakowiak M, Delmutti EE, Alves MR. Influence of loxapine on the sleep-wakefulness cycle of the rat. Pharmacol Biochem Behav. 1974 Nov-Dec;2(6):747-51. doi: 10.1016/0091-3057(74)90105-1. PMID: 4377026.