Disease relevance of Thioxanthene

• The toxicity of thioxanthene neuroleptics to isolated rat liver cells [1].
• Reversal of multidrug resistance in murine fibrosarcoma cells by thioxanthene flupentixol [2].
• Schizophrenic patients at risk for developing hyponatremia drank water excessively(P less than .01) and were most likely to be taking thioxanthene (P = .05(4)) antipsychotic and anticholinergic medications (P Less than .01) [3].
• Flupenthixol, a new thioxanthene derivative, was studied for its effects on gastric secretion and gastric ulcers in rats [4].

High impact information on Thioxanthene

• Thioxanthine is toxic for mammalian cells transformed by the dominant selectable marker gpt [5].
• In this study, we demonstrate that inhibition of Pgp-mediated drug transport by cis-(Z)-flupentixol, a thioxanthene derivative, occurs through an allosteric mechanism [6].
• Among 1,152 psychiatric inpatients who received a phenothiazine, a butyrophenone, or a thioxanthene, 116 developed dystonia attributed to one or more of these drugs [7].
• The X-ray structure of the charge-transfer complex (CTC) of 10 with 2,4,5,7-tetranitrofluorene-9-dicyanomethylenefluorene (DTeF) [stoichiometry: 10(.+)(DTeF)(2) (.-)2 PhCl] reveals a twisted conformation of 10(.+) (driven by the bulky thioxanthene moiety) and provides a very rare example of segregated stacking of a fluorene acceptor in a CTC [8].
• In summary, we demonstrate that allosteric modulation by cis-(Z)-flupentixol is mediated through its interaction with Pgp at a site specific for tricyclic ring-containing Pgp modulators of thioxanthene and phenothiazine backbone, independent of other cellular components and the phosphorylation status of the protein [9].

Biological context of Thioxanthene

• This study investigates how neuroleptics of phenothiazine or thioxanthene structure influence the pharmacokinetics of carbamazepine [10].
• We investigated the effect of the stereo-isomers of clopenthizol, a thioxanthene, and of CPZ on human neutrophil chemotaxis [11].

Anatomical context of Thioxanthene

• Schizophrenic patients treated with high dose phenothiazine or thioxanthene become deficient in polyunsaturated fatty acids in their thrombocytes [12].

Associations of Thioxanthene with other chemical compounds

• The thioxanthene neuroleptic, cis-chlorprothixene, was approximately 200 times more potent than its transisomer as an inhibitor of the aggregation of human blood platelets induced by 5-hydroxytryptamine (5HT) [13].
• Antimicrobial potentiality of the thioxanthene flupenthixol through extensive in vitro and in vivo experiments [14].
• The present open-label study assessed the efficacy of zuclopenthixol, an thioxanthene neuroleptic with combined dopamine receptors (D1/D2) antagonist activity, in the treatment of severe behavioral disturbances in mentally retarded children and adolescents [15].
• Zuclopenthixol is a thioxanthene derivative which acts as a mixed dopamine D1/D2 receptor antagonist [16].
• A high-performance liquid chromatography (HPLC) method was developed for quantification of both isomers of the thioxanthene neuroleptic flupentixol and of the butyrophenone derivative haloperidol in human serum [17].

Gene context of Thioxanthene

• Thioxanthine, which is known to be a strong inhibitor of TPMT when added to the assay system to give a 2% contamination, reduced TPMT activity from 100% to 72% [18].
• The compounds, possessing thioxanthene and dihydroanthracene moieties as the terminal substituents, show a fast rotation around the butatriene bonds at ambient temperatures (DeltaG() = 13.7 and 14.9 kcal/mol, respectively) [19].
• When the thioxanthene neuroleptics 3H-cis (Z)-flupenthixol or 3H-piflutixol are used as ligands D-1 receptors coupled to adenylate cyclase can be detected [20].

Analytical, diagnostic and therapeutic context of Thioxanthene

• Separation of (Z)- and (E)-isomers of thioxanthene and dibenz[b,e]oxepin derivatives with calixarenes and resorcinarenes as additives in nonaqueous capillary electrophoresis [21].
• Separation of cis- and trans-isomers of thioxanthene and dibenz[b,e]oxepin derivatives on calixarene- and resorcinarene-bonded high-performance liquid chromatography stationary phases [22].
• The thioxanthene neuroleptic flupenthixol, which can be given intramuscularly (i.m.) for improving compliance, has been studied as a possible anti-craving drug both in animal models of alcoholism and some clinical studies [23].

References