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      Loxapine Succinate
      Loxapine Succinate

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1031
      CAS #: 27833-64-3Purity ≥98%

      Description: Loxapine Succinate (Loxapac; Adasuve; Cloxazepin; Daxolin; Oxilapine), the succinate salt of Loxapine which is a dibenzoxazepine anti-psychotic drug, is a potent D2DR/D4DR inhibitor as well as serotonergic receptor antagonist. It is a typical antipsychotic agent primarily used for the treatment of schizophrenia. 

      References: Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30; Psychiatry Res. 1984 Aug;12(4):277-85.

      Related CAS#: 1977-10-2

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      Molecular Weight (MW)445.9 
      FormulaC18H18ClN3O.C4H6O4 
      CAS No.27833-64-3  
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 89 mg/mL (199.6 mM)
      Water: <1 mg/mL
      Ethanol: 2 mg/mL (4.5 mM) 
      Other info

      Chemical Name: butanedioic acid;8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4] benzoxazepine

      InChi Key: YQZBAXDVDZTKEQ-UHFFFAOYSA-N

      InChi Code: InChI=1S/C18H18ClN3O.C4H6O4/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18;5-3(6)1-2-4(7)8/h2-7,12H,8-11H2,1H3;1-2H2,(H,5,6)(H,7,8)

      SMILES: CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl.C(CC(=O)O)C(=O)O

      SynonymsLoxapac; Cloxazepin; Daxolin; Maleate, Loxipine; Oxilapine


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      In Vitro

      In vitro activity: In the presence of Loxapine, [3H]ketanserin binds to 5-HT2 receptor in Frontal cortex of brain in human and bovine with ki value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows:5-HT2≥D4>>>D1>D2 in comparing competition experiments involving the human membranes. Loxapine 0.2 μM, 2 μM and 20 μM reduces IL-1beta secretion by LPS-activated mixed glia cultures after 1 and 3 days of exposure. Loxapine in concentrations of 0.2 μM, 2 μM and 20 μM reduces IL-2 secretion in mixed glia cultures after 1 and 3 days of exposure, and additionally Loxapine decreases IL-1beta and IL-2 secretion in LPS-induced microglia cultures in concentrations of 2 μM, 10 μM and 20 μM.

      In VivoLoxapine (5 mg/kg) induces a very significant reduction (more than 50%) of serotonin (S2) receptor density after 4 weeks or 10 weeks of daily injection in the rat. Loxapine (5 mg/kg) does not change dopamine receptor density but greatly reduces serotonin receptor density by 47% in the brain of rats. Loxapine (0.3 mg/kg s.c.) induces marked catalepsy, the scores reaching the cut-off level of 45 s two to 5 hours after injection in rats. Loxapine-induced catalepsy is fully established then treated by clozapine (10 mg/kg s.c.), the high catalepsy score is reduced to a value not significantly different from vehicle-treated controls in rats. 
      Animal modelRats
      Formulation & Dosage0.3, 5 mg/kg; s.c.
      References

      Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30; Psychiatry Res. 1984 Aug;12(4):277-85. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

       
      Loxapine Succinate
      Least-squares mean ΔΔQTcI (predose subtracted individually corrected QT duration compared with placebo) and two-sided 90% CIs, primary analysis model (QT population). Int J Clin Pharmacol Ther. 2015 Nov; 53(11): 963–971.
      		 
      Loxapine Succinate
      Predose subtracted individually corrected QT duration compared with placebo (ΔΔQTcI, msec) vs. loxapine concentrations (ng/mL) and fitted linear regression (ΔΔQTcI = –1.1 + 1.64 (log (loxapine)); p = 0.013). Int J Clin Pharmacol Ther. 2015 Nov; 53(11): 963–971.
      		 
      Loxapine Succinate
      Predose subtracted individually corrected QT duration compared with placebo (ΔΔQTcI, msec) vs. 8-OH-loxapine concentrations (ng/mL) and fitted linear regression (ΔΔQTcI = 1.7 – 0.561 (log (loxapine)); p = not significant). Int J Clin Pharmacol Ther. 2015 Nov; 53(11): 963–971.

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