Delving into the Latest Updates on Loxapine Succinate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Loxapine, Loxapine succinate (USP), 琥珀酸洛沙平

+ [7]

Target

5-HT receptor x DRDs

Action

antagonists

Mechanism

5-HT receptor antagonists(Serotonin (5-HT) receptor antagonists), DRDs antagonists(Dopamine receptors antagonists)

Therapeutic Areas

Other DiseasesNervous System DiseasesImmune System Diseases+ [1]

Active Indication-

Inactive Indication

AsthmaMigraine DisordersSchizophrenia

Originator Organization

Actavis A/S

Active Organization-

Inactive Organization

Alexza Pharmaceuticals, Inc.Teva Branded Pharmaceutical Products R&D, Inc.

Drug Highest PhaseApproved

First Approval Date

United States (25 Feb 1975),

Schizophrenia

Regulation-

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Structure/Sequence

Molecular FormulaC22H24ClN3O5

InChIKeyYQZBAXDVDZTKEQ-UHFFFAOYSA-N

CAS Registry27833-64-3

View All Structures (2)

Optical methods for single-molecule analysis hold the promise of accurate, sensitive, and rapid detection of target molecules. Here, we demonstrate the efficiency of such an approach for the competitive detection of small molecules in water. Our biosensing method is based on a combination of a single-DNA biochip for the parallelization of tethered particle motion real-time measurements with antibodies and modified targets as molecular competitors. The antibodies are coupled to the particles tethered to the surface by a long DNA bearing in its middle the molecular competitor bound to the antibodies. Competitive target binding leads to a detectable conformational change of the DNA tethers from looped to unlooped in proportions related to the target concentration. We thus managed to detect fluorescein, chosen as a model of a target molecule, in freshwater of various qualities, from solutions prepared with ultrapure water to more complex matrices such as river water and wastewater treatment plant effluent samples. Similar dose-response curves were obtained under these various conditions in a wide range of concentrations from nanomolar to micromolar with a limit of detection around 2 nM.

12 Aug 2024·Inorganic Chemistry

Poly(2,2′-Bibenzimidazole)–Supported Iridium Complex: A Recyclable Metal–Polymer Ligand Bifunctional Catalyst for the N-Methylation of Amines with Methanol

Article

Author: Shen, Lu ; Dong, Beixuan ; He, Yiqian ; Zhang, Shouhai ; Chen, Xiaozhong ; Li, Feng ; Wu, Xingliang

The design and development of new types of catalysts is one of the most important topics for modern chemistry. Herein, a polymer-supported iridium complex Cp*Ir@Poly(2,2'-BiBzIm) was designed and synthesized by the coordinative immobilization of [Cp*IrCl₂]₂ on 2,2'-bibenzimidazoles. In the presence of the catalyst (0.5 mol % Ir) and Cs₂CO₃ (0.3 equiv), a variety of N-methylated amines were obtained in high yields with complete selectivity. More importantly, the catalyst could be recycled without an obvious loss of activity for six cycles. Apparently, the designed catalyst combines the advantages of both homogeneous and heterogeneous catalysis.

01 Aug 2024·Drug Safety

Antipsychotic-Related DRESS Syndrome: Analysis of Individual Case Safety Reports of the WHO Pharmacovigilance Database

Article

Author: Kane, John M ; Raschi, Emanuel ; De Fazio, Pasquale ; Barbui, Corrado ; Arzenton, Elena ; Trifirò, Gianluca ; Schoretsanitis, Georgios ; Gastaldon, Chiara ; Moretti, Ugo ; de Filippis, Renato

INTRODUCTIONDrug reaction with eosinophilia and systemic symptoms (DRESS) syndrome is gaining attention in pharmacovigilance, but its association with antipsychotics, other than clozapine, is still unclear.METHODSWe conducted a case/non-case study with disproportionality analysis based on the World Health Organization (WHO) global spontaneous reporting database, VigiBase®. We analyzed individual case safety reports of DRESS syndrome related to antipsychotics compared to (1) all other medications in VigiBase®, (2) carbamazepine (a known positive control), and (3) within classes (typical/atypical) of antipsychotics. We calculated reporting odds ratio (ROR) and Bayesian information component (IC), with 95% confidence intervals (CIs). Disproportionate reporting was prioritized based on clinical importance, according to predefined criteria. Additionally, we compared characteristics of patients reporting with serious/non-serious reactions.RESULTSA total of 1534 reports describing DRESS syndrome for 19 antipsychotics were identified. The ROR for antipsychotics as a class as compared to all other medications was 1.0 (95% CI 0.9-1.1). We found disproportionate reporting for clozapine (ROR 2.3, 95% CI 2.1-2.5; IC 1.2, 95% CI 1.1-1.3), cyamemazine (ROR 2.3, 95% CI 1.5-3.5; IC 1.2, 95% CI 0.5-1.7), and chlorpromazine (ROR 1.5, 95% CI 1.1-2.1; IC 0.6, 95% CI 0.1-1.0). We found 35.7% of cases with co-reported anticonvulsants, and 25% with multiple concurrent antipsychotics in serious compared to 8.6% in non-serious cases (p = 0.03). Fatal cases were 164 (10.7%).CONCLUSIONSApart from the expected association with clozapine, chlorpromazine and cyamemazine (sharing an aromatic heteropolycyclic molecular structure) emerged with a higher-than-expected reporting of DRESS. Better knowledge of the antipsychotic-related DRESS syndrome should increase clinicians' awareness leading to safer prescribing of antipsychotics.

100 Deals associated with Loxapine Succinate

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External Link

KEGG	Wiki	ATC	Drug Bank
D00794	Loxapine Succinate	N05AH01	DB00408

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Preclinical	United States	Alexza Pharmaceuticals, Inc.	01 May 2009
Migraine Disorders	Preclinical	United States	Alexza Pharmaceuticals, Inc.	01 Jun 2007