更新于：2024-11-21

Thioproperazine

更新于：2024-11-21

概要

研发状态

概要

基本信息

药物类型

小分子化药

别名

Majeptil

靶点

D1 receptor x D2 receptor x α1A-AR x α1B-AR

作用机制

D1 receptor拮抗剂(多巴胺D1受体拮抗剂)、D2 receptor拮抗剂(多巴胺D2受体拮抗剂)、α1A-AR拮抗剂(肾上腺素能受体α-1a拮抗剂)

+ [1]

治疗领域-

在研适应症-

非在研适应症-

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构

分子式C22H30N4O2S2

InChIKeyVZYCZNZBPPHOFY-UHFFFAOYSA-N

CAS号316-81-4

关联

项与 Thioproperazine 相关的临床试验

NCT02582736 / CompletedN/AIIT

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.

开始日期2012-04-01

申办/合作机构

Canadian Institutes of Health Research

100 项与 Thioproperazine 相关的临床结果

登录后查看更多信息

100 项与 Thioproperazine 相关的转化医学

登录后查看更多信息

100 项与 Thioproperazine 相关的专利（医药）

登录后查看更多信息

174

项与 Thioproperazine 相关的文献（医药）

2007-07-01·Journal of Chromatography B3区 · 医学

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

3区 · 医学

Article

作者: 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.

2005-09-01·Journal of AOAC INTERNATIONAL4区 · 农林科学

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

4区 · 农林科学

Article

作者: 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.

2000-05-01·Biochemistry. Biokhimiia

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

Article

作者: 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 项与 Thioproperazine 相关的药物交易

登录后查看更多信息