Loxapine Succinate

Catalog No.S4086

Loxapine Succinate Chemical Structure

Molecular Weight(MW): 445.9

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

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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]
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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 445.9
Formula

C18H18ClN3O.C4H6O4

CAS No. 27833-64-3
Storage powder
in solvent
Synonyms N/A

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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

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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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID