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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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

176

Literatures (Medical) associated with Thioproperazine

12 Apr 2011·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

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

Q3 · MEDICINE

Article

Author: 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.

12 Apr 2011·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

Biotransformations in vitro undergone by phenothiazine derivatives in a liver preparation

Q3 · MEDICINE

Article

Author: 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.

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.

100 Deals associated with Thioproperazine

External Link

KEGG	Wiki	ATC	Drug Bank
-	Thioproperazine	N05AB08	DB01622

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