5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists), D1 receptor antagonists(Dopamine D1 receptor antagonists), D2 receptor antagonists(Dopamine D2 receptor antagonists)

Therapeutic Areas

Other Diseases

Active Indication-

Inactive Indication

Schizophrenia

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Pfizer Inc.

Drug Highest PhaseWithdrawn

First Approval Date

US (06 Apr 1970),

Schizophrenia

Regulation-

Structure

Molecular FormulaC23H35Cl2N3O4S2

InChIKeyMEUAAEMCZUPORO-LRSHZYOCSA-N

CAS Registry22189-31-7

View All Structures (2)

100 Clinical Results associated with Thiothixene Hydrochloride

100 Translational Medicine associated with Thiothixene Hydrochloride

100 Patents (Medical) associated with Thiothixene Hydrochloride

Literatures (Medical) associated with Thiothixene Hydrochloride

19 Jan 2024·Organic Process Research & Development

Process Development for the Manufacture of the Antimalarial Amodiaquine Dihydrochloride Dihydrate

Article

Author: Zitha, Andile ; Klashorst, Gerrit van der ; Malan, Hannes ; Gohain, Mukut ; Malefo, Modibo S. ; Kunyane, Phaladi ; Baruah, Sangeeta ; Scholtz, Chantal

A robust process for the manufacture of the active pharmaceutical ingredient (API) amodiaquine dihydrochloride dihydrate (ADQ, 3), an important antimalarial, is reported. The process consists of a three-step synthetic route that involves a Mannich reaction, substitution with 4,7-dichloroquinoline (4,7-DCQ, 5), and rehydration. Additionally, a cost-competitive process for the production of 4,7-DCQ (5) is also reported wherein 4,7-DCQ (5) was prepared in four steps from meta-chloroaniline (7). 4-Acetamido-2-(diethylaminomethyl)phenol (14), 4,7-DCQ (5), and ADQ (3) were obtained in yields of 92, 89, and 90%, respectively. Costing and process mass intensities of 4,7-DCQ and ADQ are also reported.

01 Aug 2011·Journal of Pharmaceutical SciencesQ3 · MEDICINE

Determination of quinacrine dihydrochloride dihydrate stability and characterization of its degradants

Q3 · MEDICINE

Article

Author: Espeau, Philippe ; Rotival, Romain ; Corvis, Yohann ; Do, Bernard ; Guyon, François

Although quinacrine dihydrochloride dihydrate is a widely used drug substance, a comprehensive determination of its stability profile is lacking. In this work, an integrative approach is implemented to determine the drug stability both in the solid state and aqueous solutions, identify the impurities that can be found in the active pharmaceutical ingredient, and evaluate the associated toxicity risks. Thermal analyses pointed out a two-step dehydration of the solid state. This phenomenon seems to be consistent with the organization of the water molecules in the crystal structure and results in the destruction of the lattice. Seven related compounds of quinacrine have been identified by liquid chromatography-ion trap mass spectrometry. The main thermal degradant both in the solid state and the solution corresponds to the N-deethyl compound, whereas quinacrine tertiary amine oxyde appears to be a signal impurity of oxidative stress in solution. Moreover, two photolytic impurities can be formed in solution either by aromatic amine cleavage or via O-demethylation. Additionally, using computational approaches, the analysis of the potential toxicity of the impurities compared with the parent compound one shows that ketone and O-demethyl derivatives may exhibit specific toxicity profiles.

01 Oct 2010·Mutation Research/Genetic Toxicology and Environmental Mutagenesis

Evaluation of phenolphthalein, diazepam and quinacrine dihydrochloride in the in vitro mammalian cell micronucleus test in Chinese hamster ovary (CHO) and TK6 cells

Article

Author: Shyam Kumar ; Nkechi Maduka ; Catherine Thiffeault ; Donna Dickinson ; Maria Engel ; Jocelyn Sherman ; Maik Schuler ; Anna Szkudlinska ; Megan Colman ; Jennifer Cheung ; Ramadevi Gudi

The in vitro micronucleus assay has been extensively used as an in vitro screening tool to identify test articles that might have aneugenic or clastogenic potential. Currently, the Organization for Economic Co-operation and Development (OECD) is working towards a final version of the guideline for the conduct of the in vitro mammalian cell micronucleus Test (MNvit). A few questions regarding appropriate cytotoxicity measurements and cytotoxicity limits to use remain to be answered. In order to resolve the remaining questions, we compared the induction of micronuclei at the top dose (50-60% cytotoxicity) determined by either Relative Cell Counts (RCC), Relative Increase in Cell Counts (RICC), Relative Population Doublings (RPD), or Cytokinesis-Blocked Proliferating Index (CBPI) using weak and strong inducers of micronuclei in both the presence and absence of cytochalasin B (CYB) in Chinese hamster ovary (CHO) and human lymphoblastoid TK6 cells. In order to assess extensive dose-response relationships, we selected expected weak (diazepam, phenolphthalein, quinacrine dihydrochloride dihydrate) and strong (cytosine arabinoside, mitomycin C, vinblastine sulphate) inducers of micronuclei with a variety of different mechanisms of action for testing. The results clearly demonstrated that all six compounds produced positive responses using either cytotoxicity measurement. The outcome from these studies further supports the cytotoxicity measurements and cytotoxicity limits proposed in the draft OECD guideline.

100 Deals associated with Thiothixene Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D02612	Thiothixene Hydrochloride	N05AF04	DBSALT001423

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