Home Neuronal Signaling 5-HT Receptor antagonist Loxapine Succinate

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Loxapine Succinate 5-HT Receptor antagonist

Cat.No.S4086

Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Loxapine Succinate 5-HT Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 445.9

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (199.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 445.9 Formula

C18H18ClN3O.C4H6O4

 Storage (From the date of receipt)
CAS No. 27833-64-3 Download SDF Storage of Stock Solutions

Synonyms NSC 759578 Smiles CN1CCN(CC1)C2=NC3=CC=CC=C3OC4=C2C=C(C=C4)Cl.C(CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC50/Ki
5-HT2 (human)
6.2 nM(Ki)
5-HT2 (bovine)
6.6 nM(Ki)
5-HT2 (bovine)
6.8 nM(Ki)
D4 receptor (human)
7.5 nM(Ki)
D2 receptor (Human)
24 nM(Ki)
D2 receptor (human)
24 nM(Ki)
D1 receptor (human)
26 nM(Ki)
D2 receptor (bovine)
26 nM(Ki)
D1 receptor (bovine)
62 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. 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 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. 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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9089667/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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