Home Neuronal Signaling 5-HT Receptor antagonist - Dopamine Receptor antagonist Loxapine Succinate For research use only.

Loxapine Succinate

Synonyms: NSC 759578

Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

Loxapine Succinate Chemical Structure

Loxapine Succinate Chemical Structure

CAS: 27833-64-3

Selleck's Loxapine Succinate has been cited by 1 publication

Purity & Quality Control

Batch: S408601 DMSO] 89 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 99.71%
99.71

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Biological Activity

Description Loxapine Succinate(NSC 759578) 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 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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05324852 Recruiting Emergence Delirium Assistance Publique - Hôpitaux de Paris|Lariboisière-Saint Louis clinical research unit April 14 2023 Phase 3
NCT02820519 Terminated Neuropathic Pain University of Witten/Herdecke June 7 2016 Phase 2
NCT00789360 Completed Healthy Alexza Pharmaceuticals Inc. November 2008 Phase 1

Chemical lnformation & Solubility

Molecular Weight 445.9 Formula

C18H18ClN3O.C4H6O4
CAS No. 27833-64-3 SDF Download Loxapine Succinate SDF
Smiles CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl.C(CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (199.59 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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