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Loxapine Succinate

CAS# 27833-64-3

Loxapine Succinate

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Chemical structure

Loxapine Succinate

3D structure

Chemical Properties of Loxapine Succinate

Cas No. 27833-64-3 SDF Download SDF
PubChem ID 71399 Appearance Powder
Formula C22H24ClN3O5 M.Wt 445.9
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 100 mg/mL (224.27 mM; Need ultrasonic)
Chemical Name butanedioic acid;8-chloro-6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepine
SMILES CN1CCN(CC1)C2=Nc3ccccc3Oc4ccc(Cl)cc24.OC(=O)CCC(O)=O
Standard InChIKey YQZBAXDVDZTKEQ-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Loxapine Succinate Dilution Calculator

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Loxapine Succinate Molarity Calculator

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Preparing Stock Solutions of Loxapine Succinate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2427 mL 11.2133 mL 22.4266 mL 44.8531 mL 56.0664 mL
5 mM 0.4485 mL 2.2427 mL 4.4853 mL 8.9706 mL 11.2133 mL
10 mM 0.2243 mL 1.1213 mL 2.2427 mL 4.4853 mL 5.6066 mL
50 mM 0.0449 mL 0.2243 mL 0.4485 mL 0.8971 mL 1.1213 mL
100 mM 0.0224 mL 0.1121 mL 0.2243 mL 0.4485 mL 0.5607 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Loxapine Succinate

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

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References on Loxapine Succinate

Loxapine succinate as initial treatment of hostile and aggressive schizophrenic criminal offenders.[Pubmed:7130427]

J Clin Pharmacol. 1982 Aug-Sep;22(8-9):366-70.

The efficacy and safety of loxapine were evaluated in 18 acutely ill schizophrenic criminal offenders in the Essex County Jail. The offender patients were treated for three days with intramuscular loxapine (25 mg three or four times a day), followed by seven days of oral concentrate (up to 150 mg/day in three or four divided doses). Psychiatric status was determined with the Brief Psychiatric Rating and the Clinical Global impression scales at the time of admission, after 8, 24, 48, and 72 hours, amd on days 7 and 10 of medication. Three patients did not complete treatment: one was released on bail after 24 hours of therapy, and the other two had adverse reactions (tongue swelling and muscle spasms, each in one patient) which required cessation of treatment. Statistically significant improvement in both rating scale results was evident as early as 8 hours after treatment began. By day 10, all Brief Psychiatric Rating Scale items and factors and the Clinical Global impression results were statistically improved over baseline measurements. At the end of the study, 87 per cent (13/15) of the patients were well enough to cooperate with their attorneys and understand the procedures of the court. Adverse effects (generally extrapyramidal) appeared in four of 18 patients during parenteral administration and in two of 15 patients during oral therapy.

A complementary experimental and computational study of loxapine succinate and its monohydrate.[Pubmed:24192171]

Acta Crystallogr C. 2013 Nov;69(Pt 11):1273-8.

The crystal structures of Loxapine Succinate [systematic name: 4-(2-chlorodibenzo[b,f][1,4]oxazepin-11-yl)-1-methylpiperazin-1-ium 3-carboxypropanoate], C18H19ClN3O(+).C4H5O4(-), and Loxapine Succinate monohydrate {systematic name: bis[4-(2-chlorodibenzo[b,f][1,4]oxazepin-11-yl)-1-methylpiperazin-1-ium] succinate succinic acid dihydrate}, 2C18H19ClN3O(+).C4H4O4(2-).C4H6O4.2H2O, have been determined using X-ray powder diffraction and single-crystal X-ray diffraction, respectively. Fixed cell geometry optimization calculations using density functional theory confirmed that the global optimum powder diffraction derived structure also matches an energy minimum structure. The energy calculations proved to be an effective tool in locating the positions of the H atoms reliably and verifying the salt configuration of the structure determined from powder data. Crystal packing analysis of these structures revealed that the Loxapine Succinate structure is based on chains of protonated loxapine molecules while the monohydrate contains dispersion stabilized centrosymmetric dimers. Incorporation of water molecules within the crystal lattice significantly alters the molecular packing and protonation state of the succinic acid.

[Clinical trial of loxapine succinate in the treatment of 30 cases of psychotic states].[Pubmed:6357022]

Ann Med Psychol (Paris). 1983 Mar;141(3):309-22.

An open clinical study of Loxapine Succinate was developed on 30 hospitalized psychiatric patients in order to confirm its antipsychotic properties and its originality opposite the other major neuroleptics. Dosages ranged from 100 to 200 mg per day in 12 cases (40%), and more than 200 mg in serious psychosis or unamenable to therapeutic for which inferior dosages were inefficacious (11 cases). 56,7% of favourable results have been obtained, with a fair improvement of whole symptoms, paranoid schizophrenic attack and acute delusions. Tolerance was remarkable: no neuro-vegetative manifestation was reported. The considerable sedative effect of loxapine had involved moderate and no invalidating drowsiness in 23% of cases. The extra-pyramidal occurring symptoms disappeared within 2 or 3 days. So Loxapine Succinate in proving to be a major first intention neuroleptic, suiting a considerable antipsychotic efficacy to a good tolerance, allowing new perspectives in the therapeutic and the approach of psychotic patients.

Description

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

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