Loxapine Succinate

Catalog No.S4086

For research use only.

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

Loxapine Succinate Chemical Structure

CAS No. 27833-64-3

Selleck's Loxapine Succinate has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Targets
5-HT2 (human) [1] 5-HT2 (bovine) [1] 5-HT2 (bovine) [1] D4 receptor (human) [1] D2 receptor (Human) [1] Click to View More Targets
6.2 nM(Ki) 6.6 nM(Ki) 6.8 nM(Ki) 7.5 nM(Ki) 24 nM(Ki)
In vitro

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. [1] 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. [2]

In vivo Loxapine (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. [3] 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. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 89 mg/mL
(199.59 mM)
Ethanol 2 mg/mL
(4.48 mM)
Water Insoluble

Chemical Information

Molecular Weight 445.9
Formula

C18H18ClN3O.C4H6O4

CAS No. 27833-64-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl.C(CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02820519 Terminated Drug: Loxapine Neuropathic Pain University of Witten/Herdecke June 2016 Phase 2
NCT00789360 Completed Drug: Inhaled Placebo|Drug: Inhaled Loxapine Healthy Alexza Pharmaceuticals Inc. November 2008 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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