Disease relevance of Serentil

• Mesoridazine use and priapism [1].
• Complete heart block associated with mesoridazine and lithium combination [2].
• In the early 1990s, it became clear that mesoridazine could cause torsades de pointes [3].
• Despite the paucity of data on the potential cardiotoxicity associated with mesoridazine overdose, this case demonstrates that malignant arrhythmias and cardiac arrest occur; consequently, these patients probably require constant ECG monitoring [4].
• We present a case of malignant arrhythmias associated with hypocalcemia and subsequent cardiac arrest in a 20-year-old woman due to ingestion of 3.1 g mesoridazine in a suicide attempt [4].

Psychiatry related information on Serentil

• Steady-state plasma and RBC levels of thioridazine, mesoridazine, and sum of thioridazine and mesoridazine, determined by gas-liquid chromatography, were not significantly correlated with clinical response as measured by improvement on the Brief Psychiatric Rating Scale [5].
• A double-blind study vs. placebo was carried out over a 6-week period in thirty adolescent patients to determine the efficacy and safety of mesoridazine, in the form of 10 mg tablets, in the treatment of symptoms associated with various personality disorders [6].
• Mesoridazine in Huntington's disease (chorea): effect on weight, dyskinesia, and mental function [7].

High impact information on Serentil

• Our prediction that drugs allosterically regulating [3H]nitrendipine binding should be calcium antagonists is confirmed by calcium antagonism in guinea pig ileum observed with the antihistamine dimethindene, the neuroleptics thioridazine and mesoridazine, and the anticholinergic biperiden [8].
• The factors accounting for the increased intrapatient variability of plasma levels of thioridazine, mesoridazine, and haloperidol in schizophrenic outpatients remain unclear [9].
• Tonic block of HERG current by mesoridazine (1.8 microM) was minimal (< 2-4%) [10].
• The inactivation kinetics and voltage dependence of steady-state inactivation of the HERG channel were not significantly altered by mesoridazine [10].
• Additionally, several typical antipsychotic drugs had high affinities for the cloned rat D4 receptor, with Kis less than 20 nM (loxapine, chlorpromazine, fluphenazine, mesoridazine, thioridazine and trifluoroperazine) [11].

Biological context of Serentil

• Mesoridazine blocked HERG currents in a concentration-dependent manner (IC50 550 nM at 0 mV); block increased significantly over the voltage range where HERG activates and saturated at voltages eliciting maximal HERG channel activation [10].
• A significant decrease in the mean AUC infinity 0 or AUCt0 was observed for mesoridazine after the administration of the divided dose.(ABSTRACT TRUNCATED AT 250 WORDS)[12]
• Studies on thioridazine and mesoridazine metabolism. I. Protein binding [13].

Anatomical context of Serentil

• Thioridazine and mesoridazine levels and levels of thioridazine plus metabolites were determined in plasma and red blood cells (RBC) by gas-liquid chromatography (GLC) and spectrofluorometry (SP), respectively, in schizophrenic patients treated with fixed doses of thioridazine [14].
• In light of the fact that the thioridazine and mesoridazine concentrations used in these experiments are in the range of those used clinically in patients, our results suggest that inhibition of gap junction intercellular communication may be one factor contributing to the cardiac side-effects observed in some patients taking these medications [15].
• Micromolar concentrations of thioridazine and mesoridazine inhibited gap junction-mediated intercellular communication between WB-F344 epithelial cells in a dose-dependent manner, as measured by fluorescent dye transfer [15].

Associations of Serentil with other chemical compounds

• Estimates of neuroleptic activity by RRA and the weighted sum of thioridazine, mesoridazine and sulforidazine by HPLC were very similar [16].
• 1 Mesoridazine, a phenothiazine of short half-life, and potentially useful as an hypnotic, has here been investigated using volunteers of late middle age [17].
• This RIA procedure was compared with a high-performance liquid chromatographic (HPLC) method by determining concentrations of mesoridazine in plasma samples from human volunteers over 72 h after administration of single 50-mg oral doses of thioridazine hydrochloride [18].
• Dysphoric response to neuroleptics as a predictor of treatment outcome with schizophrenics. A comparative study of haloperidol versus mesoridazine [19].

Gene context of Serentil

• The four stereoisomers of mesoridazine were synthesized and evaluated in D2, 5-HT1A, 5-HT2A, 5-HT2C, D1, and D3 receptor binding and functional assays [20].
• Thioridazine is metabolized in humans by CYP2D6 to mesoridazine, which is an active metabolite [21].
• A radioimmunoassay (RIA) procedure for mesoridazine was developed using an antiserum raised in rabbits immunized with N-(2-carboxyethyl) desmethylmesoridazine-porcine thyroglobulin conjugate [18].
• Mesoridazine increased REM sleep above baseline levels and a rebound fall below baseline occurred on withdrawal [17].
• Thioridazine hapten was coupled to bovine serum albumin, whereas the haptens for mesoridazine and sulforidazine were coupled to porcine thyroglobulin [22].

Analytical, diagnostic and therapeutic context of Serentil

• Thioridazine and its active metabolites, mesoridazine and sulforidazine, were estimated in plasma by high performance liquid chromatography (HPLC) and radioreceptor assay (RRA) [16].
• Development of a radioimmunoassay procedure for mesoridazine and its comparison with a high-performance liquid chromatographic method [18].
• After oral administration THD is extensively biotransformed to thioridazine 2-sulfone (THD 2-SO(2)), thioridazine 5-sulfoxide (THD 5-SO) and thioridazine 2-sulfoxide (THD 2-SO) [23].

References