Tag: 412.9356

Effects on suicidal risk: Comparison of clozapine to other newer medicines indicated to treat schizophrenia or bipolar disorder was written by Forte, Alberto;Pompili, Maurizio;Imbastaro, Benedetta;De Luca, Gabriele Pasquale;Mastrangelo, Martina;Montalbani, Benedetta;Baldessarini, Ross J.. And the article was included in Journal of Psychopharmacology (London, United Kingdom) in 2021.Reference of 146939-27-7 This article mentions the following:

Background:: Clozapine is the only treatment with regulatory-recognition of lowering suicidal risk, at least in schizophrenia patients. It remains uncertain whether such effects extend to other drugs for psychosis. Methods:: We searched for reports on rates of suicidal behavior during treatment with clozapine and other modern drugs for psychosis (aripiprazole, olanzapine, risperidone, quetiapine, and ziprasidone) vs. comparison or control treatments and analyzed the contrasts by random-effect meta-anal. to obtain pooled odds ratios (ORs) with 95% confidence intervals (CIs). Results:: We identified 35 paired comparisons of modern drugs for psychosis vs. comparison or control treatments in 18 reports. There was moderate overall superiority of all agents tested over alternatives (OR = 0.522, p = 0.004). With clozapine, this effect was large (OR = 0.229, p < 0.0001) and consistent (7/7 trials), but significant antisuicidal effects were not found with other drugs for psychosis in 28 other trials (OR = 0.941, p = 0.497). Apparent efficacy of specific agents ranked: risperidone ≥ olanzapine ≥ aripiprazole ≥ ziprasidone ≥ mixed drugs for psychosis ≥ quetiapine, but none of these differences was significant. Conclusions:: An ability of clozapine to reduce risk of suicides and attempts in schizophrenia patients appears to be a unique effect not shared with other modern medicines indicated for schizophrenia or bipolar disorder. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Reference of 146939-27-7).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. The chemistry of isothiazoles is being intensively developed, which is evidenced by the wide range of selective transformations involving the isothiazole heterocycle and the high biological activity of its derivatives that can be used as effective new drugs and plant protection chemicals. The isothiazoles can be oxidized to the corresponding sulfoxides on treatment with peracids.Reference of 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Development of Nanocrystal Ziprasidone Orally Disintegrating Tablets: Optimization by Using Design of Experiment and In Vitro Evaluation was written by Tashan, Emine;Karakucuk, Alptug;Celebi, Nevin. And the article was included in AAPS PharmSciTech in 2020.Application of 146939-27-7 This article mentions the following:

The objective of the current study was to develop ziprasidone hydrochloride monohydrate (ZHM) nanocrystal-based orally dispersible tablet (ODT) formulations. Design of experiment approach was used to develop ODTs. The tablets were compressed using direct compression method and characterized with quality control tests. In vitro dissolution studies and Caco-2 cell permeability tests were executed. The hardness and friability values of nanocrystal-based ODTs were found 31.2 N and 1.05%, resp. The disintegration time was below 10 s. Dissolution profile in pH 7.4 phosphate buffer showed that nanocrystal-based ODTs and com. product were dissolved in 120 min 58.98% and 16%, resp. In pH 7.4 phosphate buffer with SLS, sample groups dissolved above 85% at the end of the study. Permeability value and cumulative ZHM amount on the cells were improved with nanocrystals. In conclusion, the novel formulation of ZHM nanocrystal-based ODTs was successfully developed for alternative dosage form. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Application of 146939-27-7).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Isothiazoles and isothiazolium cations are attacked by carbanions at sulfur and on recyclization can give thiophenes. Isothiazoles are readily prepared from isoxazoles. Thus, reductive ring opening of isoxazoles gives enaminones , which on treatment with phosphorus pentasulfide and chloranil give the corresponding isothiazoles.Application of 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Antipsychotic patterns in outpatients with schizophrenia in China: A cross sectional study was written by Guo, Xiaobing;Yu, Hongye;Wang, Hu. And the article was included in Medicine (Philadelphia, PA, United States) in 2021.HPLC of Formula: 146939-27-7 This article mentions the following:

It is essential to monitor pharmacol. treatment for schizophrenic outpatients regularly in clin. practice. Especially in China, the situation of common prescribing patterns remains unclear. The objective of this study is to reveal real-world treatment prescription patterns of antipsychotics for schizophrenia patients in a representative large tertiary hospital in China.This study is a cross-sectional observational anal. of outpatients with schizophrenia in a large tertiary psychiatric hospital in Beijing, China, from May 11th to 24th, 2019. Data on subjects’ socio-demog. and clin. characteristics, prescriptions of psychotropic drugs were collected from the electronic medical record (EMR) system with a standardized protocol. A multivariate anal. was performed to explore the potential association between antipsychotics treatments and subjects’ characteristics.Of the 1940 patients included in this study, only 1470 (75.77%) patients were prescribed antipsychotic medications. 1228 (83.53%) patients were prescribed second-generation antipsychotics (SGAs), 202 (13.74%) patients were treated only with first-generation antipsychotics (FGAs), 40 (2.72%) were prescribed both SGAs and FGAs. The proportion of single SGAs prescriptions was significantly higher than that of single FGAs antipsychotics in each course of monotherapy group, especially among patients with the course less than 2 years (96.08%). Risperidone was most frequently prescribed antipsychotic medication during the study (29.86%, 439 out of 1470). Intermediate-acting sedative benzodiazepines were the most commonly co-prescribed psychotropic class at 23.66%. Long-acting injectable antipsychotics (LAIs) could be the prescribing trend in clinics. Disease course, self-paying cost and LAI antipsychotic use were independently associated with antipsychotics treatments.Second-generation antipsychotics showed domination in prescriptions. More concerns should be paid with concomitant psychiatric medications in clinics. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7HPLC of Formula: 146939-27-7).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Isothiazoles and their saturated and/or oxygenated analogs play an important role in pharmaceutical research. Many compounds with an isothiazole scaffold demonstrated a wide range of biological profiles, including antiinflammatory, antithrombotic, and anticonvulsive agents.HPLC of Formula: 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

N-Skatyltryptamines-Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential was written by Hogendorf, Agata;Hogendorf, Adam S.;Kurczab, Rafal;Satala, Grzegorz;Szewczyk, Bernadeta;Cieslik, Paulina;Latacz, Gniewomir;Handzlik, Jadwiga;Lenda, Tomasz;Kaczorowska, Katarzyna;Staron, Jakub;Bugno, Ryszard;Duszynska, Beata;Bojarski, Andrzej J.. And the article was included in Molecules in 2021.Product Details of 146939-27-7 This article mentions the following:

A series of N-skatyltryptamines was synthesized and their affinities for serotonin and dopamine receptors were determined Compounds exhibited activity toward 5-HT1A, 5-HT2A, 5-HT6, and D2 receptors. Substitution patterns resulting in affinity/activity switches were identified and studied using homol. modeling. Chosen hits were screened to determine their metabolism, permeability, hepatotoxicity, and CYP inhibition. Several D2 receptor antagonists with addnl. 5-HT6R antagonist and agonist properties were identified. The former combination resembled known antipsychotic agents, while the latter was particularly interesting due to the fact that it has not been studied before. Selective 5-HT6R antagonists have been shown previously to produce procognitive and promnesic effects in several rodent models. Administration of 5-HT6R agonists was more ambiguous-in naive animals, it did not alter memory or produce slight amnesic effects, while in rodent models of memory impairment, they ameliorated the condition just like antagonists. Using the identified hit compounds 15 and 18, we tried to sort out the difference between ligands exhibiting the D2R antagonist function combined with 5-HT6R agonism, and mixed D2/5-HT6R antagonists in murine models of psychosis. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Product Details of 146939-27-7).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Some representatives of isothiazoles have proven to be synergists of bioactive substances, which opens the way to lower the doses of drugs used and is especially important in cancer chemotherapy. It has been found that isothiazole-based compounds show synergistic effects when used with other biocidal compounds.Product Details of 146939-27-7

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Genome-wide association study of antipsychotic-induced sinus bradycardia in Chinese schizophrenia patients was written by Weng, Saizheng;Wang, Bo;Li, Mo;Chao, Shan;Lin, Ruiqian;Zheng, Rongyan;Yu, Yinliang;Guo, Shaonan;Lin, Xianhao. And the article was included in PLoS One in 2021.Recommanded Product: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one This article mentions the following:

Second-generation antipsychotics (SGAs) play a critical role in current treatment of schizophrenia (SCZ). It has been observed that sinus bradycardia, rare but in certain situations life threatening adverse drug reaction, can be induced by SGAs across different schizophrenia populations. However, the roles of genetic factors in this phenomenon have not been studied yet. In the present study, a genome-wide association study of single nucleotide polymorphisms (SNPs) was performed on Chinese Han SCZ patients to identify susceptibility loci that were associated with sinus bradycardia induced by SGAs. This study applied microarray to obtain genotype profiles of 88 Han Chinese SCZ patients. Our results found that there were no SNPs had genome-wide significant association with sinus bradycardia induced by SGAs. The top GWAS hit located in gene KIAA0247, which mainly regulated by the tumor suppressor P53 and thus plays a role in carcinogenesis based on resent research and it should not be a susceptibility locus to sinus bradycardia induced by SGAs. Using gene-set functional anal., we tested that if top 500 SNPs mapped genes were relevant to sinus bradycardia. The result of gene prioritization anal. showed CTNNA3 was strongly correlated with sinus bradycardia, hinting it was a susceptibility gene of this ADR. Our study provides a preliminary study of genetic variants associated with sinus bradycardia induced by SGAs in Han Chinese SCZ patients. The discovery of a possible susceptibility gene shed light on further study of this adverse drug reaction in Han Chinese SCZ patients. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Recommanded Product: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Isothiazole is more toxic than pyridine. But the more substituted isothiazoles are usually far less toxic. It has been found that isothiazole-based compounds show synergistic effects when used with other biocidal compounds.Recommanded Product: 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

Can pediatric bipolar disorder be successfully treated when comorbid with conduct disorder? A secondary analysis of clinical trials of risperidone, olanzapine, quetiapine, ziprasidone, and aripiprazole was written by Wozniak, Janet;DiSalvo, Maura;Farrell, Abigail;Yule, Amy;Joshi, Gagan;Cook, Emmaline;Faraone, Stephen V.;Biederman, Joseph. And the article was included in Journal of Psychopharmacology (London, United Kingdom) in 2022.Electric Literature of C21H21ClN4OS This article mentions the following:

Pediatric bipolar disorder (BP) is frequently comorbid with conduct disorder (CD) and its presence adds to the morbidity of BP. While there are no known pharmacol. treatments for CD, pediatric BP is responsive to treatment with medications initially indicated for the treatment of psychosis, several of which have Food and Drug Administration (FDA) approval for the treatment of pediatric mania. The main aim of this secondary anal. was to examine whether pediatric BP comorbid with CD responds similarly to treatment with such selected medications. Considering the well-documented morbidity of CD, this finding could have important clin. and public health significance. We conducted a secondary anal. of six prospective 8-wk open-label trials of selected medications (risperidone, olanzapine, quetiapine, ziprasidone, and aripiprazole) using identical methodol. in youth with BP with and without comorbid CD. Of 165 youths with BP, 54% (N = 89) met criteria for comorbid CD. The antimanic effects observed did not significantly differ between BP youths with and without comorbid CD, as measured either by a reduction in Young Mania Rating Scale (YMRS) ≥ 30% or Clin. Global Impression (CGI)-Improvement ≤ 2 (p = 0.23), or by the more stringent definition of a reduction in YMRS ≥ 50% (p = 0.61). Pediatric BP can be effectively treated with the abovementioned medications in the context of comorbid CD. Based on previous research showing that remission of BP is associated with remission of CD, if confirmed, these findings raise the possibility that antimanic treatment of youth with BP comorbid with CD could have secondary benefits in mitigating the morbidity associated with CD. This is a pilot scale finding, the results of which are promising and should be confirmed by larger and long-term follow-up studies. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Electric Literature of C21H21ClN4OS).

5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Isothiazole is a good solvent for many organic substances but should be used with caution because it is more toxic than pyridine. In general, isothiazole undergoes nitration in the presence of HNO3, sulfuric acid, and sulfonation by using sulfuric acid under thermal conditions to generate corresponding 4-nitro- and 4-sulfonic acid derivatives, respectively.Electric Literature of C21H21ClN4OS

Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com