D1 receptor antagonists(Dopamine D1 receptor antagonists), D2 receptor antagonists(Dopamine D2 receptor antagonists), α1A-AR antagonists(Alpha-1a adrenergic receptor antagonists)

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Drug Highest PhaseApproved

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Regulation-

Structure

Molecular FormulaC22H30N4O2S2

InChIKeyVZYCZNZBPPHOFY-UHFFFAOYSA-N

CAS Registry316-81-4

Clinical Trials associated with Thioproperazine

NCT02582736 / CompletedNot ApplicableIIT

Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data

The purpose of this study is to determine whether the use of atypical antipsychotic medication increases the risk of hospitalization for a hyperglycemic emergency.
The investigators will carry out separate population-based cohort studies using administrative health databases in eight jurisdictions in Canada and the UK. Cohort entry will be defined by the initiation of a new antipsychotic medication. Follow-up will continue until hospitalization for a hyperglycemic emergency or the end of 365 days. The results from the separate sites will be combined to provide an overall assessment of the risk of hyperglycemic emergencies among new users of various antipsychotic drugs.

Start Date01 Apr 2012

Sponsor / Collaborator

Canadian Institutes of Health Research

100 Clinical Results associated with Thioproperazine

100 Translational Medicine associated with Thioproperazine

100 Patents (Medical) associated with Thioproperazine

174

Literatures (Medical) associated with Thioproperazine

01 Jul 2007·Journal of Chromatography BQ3 · MEDICINE

Simple and simultaneous determination for 12 phenothiazines in human serum by reversed-phase high-performance liquid chromatography

Q3 · MEDICINE

Article

Author: Katsuya Honda ; Masaru Terada ; Einosuke Tanaka ; Takako Nakamura ; Katsuyoshi Kurihara ; Tatsuo Shinozuka ; Chikako Hashimoto

A high-performance liquid chromatographic method has been developed for the simultaneous analysis of the 12 phenothiazines (chlorpromazine, fluphenazine, levomepromazine, perazine, perphenazine, prochlorperazine, profenamine, promethazine, propericiazine, thioproperazine, thioridazine and trifluoperazine) in human serum using HPLC/UV. The separation was achieved using a C(18) reversed-phase column (250 mm x 4.6 mm I.D., particle size 5 microm, Inersil ODS-SP). The mobile phase, consisting of acetonitrile-methanol-30 mM NaH(2)PO(4) (pH 5.6) (300:200:500, v/v/v), was delivered at a flow rate of 0.9 mL/min and UV detection was carried out at 250 nm. The recoveries of the 12 phenothiazines spiked into serum samples were 87.6-99.8%. Regression equations for the 12 phenothiazines showed excellent linearity, with detection limits of 3.2-5.5 ng/mL for serum. The inter-day and intra-day coefficients of variation for serum samples were commonly below 8.8%. The selectivity, accuracy and precision of this method are satisfactory for clinical and forensic purposes. This sensitive and selective method offers the opportunity for simultaneous screening and quantification of almost all phenothiazines available in Japan for the purposes of clinical and forensic applications.

01 Sep 2005·Journal of AOAC INTERNATIONALQ4 · AGRICULTURAL & FORESTRY SCIENCE

Analysis of Phenothiazines in Human Body Fluids Using Disk Solid-Phase Extraction and Liquid Chromatography

Q4 · AGRICULTURAL & FORESTRY SCIENCE

Article

Author: Hasegawa, Chika ; Sato, Keizo ; Kumazawa, Takeshi ; Kuriki, Ayako ; Fujimaki, Koichiro ; Seno, Hiroshi ; Lee, Xiao-Pen ; Marumo, Akemi ; Suzuki, Osamu

AbstractSeven phenothiazine derivatives, perazine, perphenazine, prochlorperazine, propericiazine, thioproperazine, trifluoperazine, and flupentixol, have been found to be extractable from human plasma and urine samples using disk solid-phase extraction (SPE) with an Empore C18 cartridge. Human plasma and urine (1 mL each) containing the 7 phenothiazine derivatives were mixed with 2 mL of 0.1M NaOH and 7 mL distilled water and then poured into the disk SPE cartridges. The drugs were eluted with 1 mL chloroform– acetonitrile (8 + 2) and determined by liquid chromatography with ammonium formate/formic acid–acetonitrile gradient elution. The detection was performed by ultraviolet absorption at 250 nm. The separation of the 7 phenothiazine derivatives from each other and from impurities was generally satisfactory using a SymmetryShield RP8 column (150 × 2.1 mm id, 3.5 μm particle size). The recoveries of the 7 phenothiazine derivatives spiked into plasma and urine samples were 64.0–89.9% and 65.1–92.1%, respectively. Regression equations for the 7 phenothiazine derivatives showed excellent linearity, with detection limits of 0.021–0.30 mg/mL for plasma and 0.017–0.30 μg/mL for urine. The within-day and day-to-day coefficients of variation for both samples were commonly below 9.0 and 14.9%, respectively.

01 May 2000·Biochemistry. Biokhimiia

Effect of strophanthin G on peroxidase oxidation kinetics of slowly oxidizable peroxidase substrates.

Article

Author: Rogozhin, V V ; Rogozhina, T V

Steady-state kinetics of thioproperazine, triftazine, aminazine, and o-dianisidine oxidation with hydrogen peroxide catalyzed by horseradish peroxidase were studied in the presence of strophanthin G. Values of the inhibition and activation constants (Ki, Ka) were determined in the pH range 5.0-7.5. At acidic pH, strophanthin G activated peroxidase during the oxidation of thioproperazine by the uncompetitive mechanism, and when triftazine was oxidized, the inhibition was noncompetitive. At pH > 6.0, the patterns of activation and inhibition changed to mixed-type during the peroxidase oxidation of thioproperazine and triftazine and to competitive inhibition of peroxidase with strophanthin G during the oxidation of aminazine. These effects are suggested to be due to an ionizable enzyme group of pK approximately 6.0. Strophanthin G inhibited free-radical oxidation of o-dianisidine via binding to the enzyme-substrate complex, preventing the generation of a stable semi-oxidized product of o-dianisidine, and thus inhibiting the enzyme by the anticompetitive mechanism. Mechanisms of oxidation of slowly and rapidly oxidizable substrates of peroxidase in the presence of strophanthin G are suggested.

100 Deals associated with Thioproperazine

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KEGG	Wiki	ATC	Drug Bank
-	Thioproperazine	N05AB08	DB01622

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