更新于：2024-11-01

Thioproperazine

更新于：2024-11-01

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-

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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

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100 项与 Thioproperazine 相关的转化医学

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100 项与 Thioproperazine 相关的专利（医药）

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176

项与 Thioproperazine 相关的文献（医药）

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Antagonistic effects of neuroleptics and apomorphine on synaptosomal tyrosine hydroxylase in vitro

3区 · 医学

Article

作者: Christiansen, Jan ; Squires, Richard F

Spiramide (I) [510-74-7], thioproperazine [316-81-4], perphenazine [58-39-9], fluphenazine [69-23-8], α-flupenthixol [53772-82-0], chlorpromazine [50-53-3], thioridazine [50-52-2], clozapine [5786-21-0], but not β-flupenthixol [53772-85-3] antagonized the inhibition of rat brain synaptosomal tyrosine hydroxylase [9036-22-0] by apomorphine [58-00-4].The antagonizing activity was correlated with in vivo potency, suggesting that the postulated presynaptic dopamine receptors on synaptosomes are similar to postsynaptic receptors.

2011-04-12·Journal of Pharmacy and Pharmacology3区 · 医学

Biotransformations in vitro undergone by phenothiazine derivatives in a liver preparation

3区 · 医学

Article

作者: ROBINSON, ANN E

AbstractCharacterisation of the products of biotransformations resulting when a wide range of medicinally used phenothiazine derivatives were incubated with a “microsomal and soluble” fraction of livers from albino Wistar rats, is described. The compounds were chlorpromazine, demethylchlorpromazine, dedimethylchlorpromazine, triflupromazine, promazine, acepromazine, propiomazine, diethazine, promethazine, isopromethazine, ethopropazine, trimeprazine, methotrimeprazine, ethylmemazine, proquamezine, cyamemazine, trifluoperazine, prochlorperazine, thioproperazine, fluphenazine, pecazine, and also the sulphoxides of the first three compounds and of promazine. The predominant reactions were those of dealkylation and of hydroxylation of the aromatic ring. Sulphoxidation did not occur to a significant extent with any of the compounds examined.

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.

100 项与 Thioproperazine 相关的药物交易

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