Wang, Guangbao et al. published their research in Bioorganic Chemistry in 2021 | CAS: 27913-99-1

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Safety of 4-(4-Methylpiperazin-1-yl)benzaldehyde

The discovery of novel sanjuanolide derivatives as chemotherapeutic agents targeting castration-resistant prostate cancer was written by Wang, Guangbao;Chen, Xiaojing;Wang, Nan;Xiao, Yunbei;Shu, Sheng;Alsayed, Ali Mohammed Mohammed;Liu, Lu;Ma, Yue;Liu, Peng;Zhang, Qianwen;Chen, Xiangjuan;Liu, Zhiguo;Zheng, Xiaohui. And the article was included in Bioorganic Chemistry in 2021.Safety of 4-(4-Methylpiperazin-1-yl)benzaldehyde This article mentions the following:

There remains a critical need for more effective therapies for the treatment of castration-resistant prostate cancer (CRPC), which is the leading cause of death in patients with prostate cancer. In this study, a series of sanjuanolide derivatives were designed, synthesized and evaluated as potential anti-CRPC agents. Most of the compounds had excellent selectivity for CRPC cells with IC50 values < 20渭M. Moreover, minimal side effects on human normal hepatic MIHA cells and normal prostatic stromal myofibroblast WPMY-1 cells were observed, with IC50 > 100渭M. The representative compound S07 slowed down the proliferative rate of CRPC cells, promoted cell apoptosis and caused G2/M phase accumulation, as well as G1/G0 phase reduction Further mechanistic studies showed that S07 treatment triggered intense DNA damage and provoked strong DNA damage response in a dose-dependent manner. These findings suggested that sanjuanolide derivatives, especially S07, selectively induced CRPC cell death by triggering intense DNA damage and DNA damage response. In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1Safety of 4-(4-Methylpiperazin-1-yl)benzaldehyde).

4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Safety of 4-(4-Methylpiperazin-1-yl)benzaldehyde

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Kim, Youjin et al. published their research in Precision and Future Medicine in 2018 | CAS: 1035270-39-3

rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Category: piperazines

Identification of FGFR3-TACC3 gene fusion in metastatic gastric cancer was written by Kim, Youjin;Kim, Seung Tae;Lee, Jeeyun;Kang, Won Ki;Kim, Kyoung-Mee;Park, Se Hoon. And the article was included in Precision and Future Medicine in 2018.Category: piperazines This article mentions the following:

In preclin. cancer models, fibroblast growth factor receptor (FGFR) gene aberration has been known to be associated with increased tumor cell proliferation and survival in several cancer types. Oncogenic fusions consisting of FGFR3 and transforming acid coiled coil 3 (TACC3) had been identified as potential therapeutic target. We report on a gastric cancer patient with liver metastases who harbored FGFR3-TACC3 fusion which is extremely rare in gastrointestinal cancer. Herein, we report a case presentation with literature review of FGFR3-TACC3 fusion. In the experiment, the researchers used many compounds, for example, rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3Category: piperazines).

rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide (cas: 1035270-39-3) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Basavaiah, K. et al. published their research in Eastern Pharmacist in 1998 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Determination of some phenothiazine neuroleptics by means of absorption spectrophotometry was written by Basavaiah, K.;Krishnamurthy, G.;Swamy, J. Manjunatha. And the article was included in Eastern Pharmacist in 1998.Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide This article mentions the following:

A simple, rapid and sensitive spectrophotometric method was described for the quant. determination of 6 phenothiazine-based antipsychotic and anticholinergic drugs in bulk and in formulations. The method is based on the formation of stable phenothiazinium free radical cation by the use of sodium nitroprusside as the chromogenic agent. The drugs in a 1.5-2.5M H2SO4 medium reacted with the reagent to give intense orange or purple products which had characteristic absorption maxima at 500-530 nm. Beer’s law was obeyed over the concentration range 4-32 渭g/mL with apparent molar absorptivities ranging from 9.8 脳 103 16.59 脳 103 l.mol.-1 cm-1. The average percent recovery was 99.5-101.6. The accuracy and precision of the assay method were comparable to those of the British Pharmacopeia method. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Yamamoto, Shohei et al. published their research in PLoS One in 2015 | CAS: 692737-80-7

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Recommanded Product: 692737-80-7

Screening of drugs to treat 8p11 myeloproliferative syndrome using patient- derived induced pluripotent stem cells with fusion gene CEP110-FGFR1 was written by Yamamoto, Shohei;Otsu, Makoto;Matsuzaka, Emiko;Konishi, Chieko;Takagi, Haruna;Hanada, Sachiyo;Mochizuki, Shinji;Nakauchi, Hiromitsu;Imai, Kohzoh;Tsuji, Kohichiro;Ebihara, Yasuhiro. And the article was included in PLoS One in 2015.Recommanded Product: 692737-80-7 This article mentions the following:

Induced pluripotent stem (iPS) cells provide powerful tools for studying disease mechanisms and developing therapies for diseases. The 8p11 myeloproliferative syndrome (EMS) is an aggressive chronic myeloproliferative disorder (MPD) that is caused by constitutive activation of fibroblast growth factor receptor 1. EMS is rare and, consequently, effective treatment for this disease has not been established. Here, iPS cells were generated from an EMS patient (EMS-iPS cells) to assist the development of effective therapies for EMS. When iPS cells were co-cultured with murine embryonic stromal cells, EMS-iPS cells produced more hematopoietic progenitor and hematopoietic cells, and CD34+ cells derived from EMS-iPS cells exhibited 3.2-7.2-fold more macrophage and erythroid colony forming units (CFUs) than those derived from control iPS cells. These data indicate that EMS-iPS cells have an increased hematopoietic differentiation capacity, which is characteristic of MPDs. To determine whether a tyrosine kinase inhibitor (TKI) could suppress the increased number of CFUs formed by EMS-iPS-induced CD34+ cells, cells were treated with one of four TKIs (CHIR258, PKC 412, ponatinib, and imatinib). CHIR258, PKC 412, and ponatinib reduced the number of CFUs formed by EMS-iPS-induced CD34+ cells in a dose-dependent manner, whereas imatinib did not. Similar effects were observed on primary peripheral blood cells (more than 90% of which were blasts) isolated from the patient. This study provides evidence that the EMS-iPS cell line is a useful tool for the screening of drugs to treat EMS and to investigate the mechanism underlying this disease. In the experiment, the researchers used many compounds, for example, 4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7Recommanded Product: 692737-80-7).

4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate (cas: 692737-80-7) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Recommanded Product: 692737-80-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ozkul, Bahattin et al. published their research in International Journal of Neuroscience in 2022 | CAS: 224785-90-4

2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

Demonstration of ameliorating effect of vardenafil through its anti-inflammatory and neuroprotective properties in autism spectrum disorder induced by propionic acid on rat model was written by Ozkul, Bahattin;Urfali, Furkan Erturk;Sever, Ibrahim Halil;Bozkurt, Mehmet Fatih;Sogut, Ibrahim;Elgormus, Cagri Serdar;Erdogan, Mumin Alper;Erbas, Oytun. And the article was included in International Journal of Neuroscience in 2022.Category: piperazines This article mentions the following:

Autism spectrum disorder (ASD) is a neurodevelopmental disorder with complex etiol. In this study, we aimed to determine the ameliorating effects of vardenafil in the ASD rat model induced by propionic acid (PPA) in terms of neurobehavioral changes and also support these effects with histopathol. changes, brain biochem. anal. and magnetic resonance spectroscopy (MRS) findings. Twenty-one male rats were randomly assigned into three groups. Group 1 (control, 7 rats) did not receive treatment. Rats in groups 2 and 3 were given PPA at the dose of 250 mg/kg/day i.p. for 5 days. After PPA administration, animals in group 2 (PPAS, 7 rats) were given saline and animals in group 3 (PPAV, 7 rats) were given vardenafil. Behavioral tests were performed between the 20th and 24th days of the study. The rats were taken for MRS on the 25th day. At the end of the study, brain levels of interleukin-2 (IL-2), IL-17, tumor necrosis factor-伪, nerve growth factor, cGMP and lactate levels were measured. In the cerebellum and the CA1 and CA3 regions of the hippocampus, counts of neurons and Purkinje cells and glial fibrillary acidic protein (associated with gliosis) were evaluated histol. Three chamber sociability and passive avoiding test, histopathol. results, lactate levels derived from MRS, and biochem. biomarkers revealed significant differences among the PPAV and PPAS groups. We concluded that vardenafil improves memory and social behaviors and prevent loss of neuronal and Purkinje cell through its anti-inflammatory and neuroprotective effect. In the experiment, the researchers used many compounds, for example, 2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4Category: piperazines).

2-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one (cas: 224785-90-4) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Barbato, Francesco et al. published their research in European Journal of Medicinal Chemistry in 1982 | CAS: 316-81-4

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Category: piperazines

Hydrophobic constants and quantitative structure activity relationships (QSAR) in sets of phenothiazine drugs was written by Barbato, Francesco;Recanatini, Maurizio;Silippo, Carlo;Vittoria, Antonio. And the article was included in European Journal of Medicinal Chemistry in 1982.Category: piperazines This article mentions the following:

Octanol/water partition coefficients of a large set of phenothiazine drugs I [R = Me2N(CH2)3, CH2CHMeNMe2, CH2CHMeCH2NMe2, etc.; R1 = H, Cl, CN, Me, CF3, etc.] were determined and related to the corresponding high-performance liquid chromatog. capacity factors. The bovine serum albumin binding affinity and antihemolytic activity of sets of congeners are discussed from the quant. structure-activity point of view. Results show that both activities are largely affected by the degree of hydrophobicity of the mols. as measured by the log P apparent values, while other factors play only a minor role. Moreover, in vivo data are considered to uncover quant. correlations between structural features and neuroleptic biol. activities. Correlation equations show that the major factor influencing the considered activities is a particular electronic demand of the phenothiazine side chain, while 2-R1-substituents may enhance the activity either affecting the side chain conformation or directly interacting at receptor site. In the experiment, the researchers used many compounds, for example, N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4Category: piperazines).

N,N-Dimethyl-10-(3-(4-methylpiperazin-1-yl)propyl)-10H-phenothiazine-2-sulfonamide (cas: 316-81-4) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ranjani, S. et al. published their research in Applied Biochemistry and Biotechnology in 2022 | CAS: 62893-19-0

(6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application In Synthesis of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

Novel Polyherbal Nanocolloids to Control Bovine Mastitis was written by Ranjani, S.;Priya, P. Shruthy;Veerasami, Maroudam;Hemalatha, S.. And the article was included in Applied Biochemistry and Biotechnology in 2022.Application In Synthesis of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid This article mentions the following:

Mastitis is a widespread disease in dairy cattle occurring throughout the world. The increased use of antibiotics brings about the development of antibiotic-resistant microbes. The application of antibiotics in dairy farming led to increased antibiotic resistance and represents a major obstacle for the treatment of mastitis. Recent advancements in nanotechnol. led to the development of nanocolloids to overcome disadvantages posed by conventional antimicrobial agents. Hence, a novel, environmentally friendly, cost-effective, biocompatible, and long-term antibacterial represents a promising solution for medicine and farming. Hence, polyherbal nanocolloids (PHNc) was formulated by using the extracts of Syzygium aromaticum, Cinnamomum verum, Emblica officinalis, Terminalia belerica, Terminalia chebula, and Cymbopogon citratus and physicochem. characterized. From mastitis milk samples, microorganisms were isolated including Acinetobacter junii, Klebsiella pneumoniae, Pseudomonas stutzeri, and Acinetobacter baumannii and screened for antibiotic susceptibility. All the isolated strains were tested with PHNc and compared with antibiotics. Min. inhibitory concentration (MIC), min. bactericidal concentration (MBC), and biofilm assays were performed at different concentrations, and antibacterial effects were quantified. In our results, PHNc showed potent bacteriostatic, bactericidal, and antibiofilm activity against all the strains. Our results indicated that PHNc can reduce the virulence factors responsible for infection by different bacterial strains. This study confirmed that PHNc had the potential to inhibit the growth of pathogenic Gram-neg. and Gram-pos. strains and could be utilized as an alternative to antibiotics to inhibit multidrug-resistant microbial pathogens in cattle. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0Application In Synthesis of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid).

(6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (cas: 62893-19-0) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application In Synthesis of (6R,7R)-7-((R)-2-(4-Ethyl-2,3-dioxopiperazine-1-carboxamido)-2-(4-hydroxyphenyl)acetamido)-3-(((1-methyl-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Anderson, Lyndsey L. et al. published their research in Neuropharmacology in 2022 | CAS: 1446817-84-0

1,1,1,3,3,3-Hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (cas: 1446817-84-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Computed Properties of C20H22F9N3O2

The endocannabinoid system impacts seizures in a mouse model of Dravet syndrome was written by Anderson, Lyndsey L.;Doohan, Peter T.;Hawkins, Nicole A.;Bahceci, Dilara;Garai, Sumanta;Thakur, Ganesh A.;Kearney, Jennifer A.;Arnold, Jonathon C.. And the article was included in Neuropharmacology in 2022.Computed Properties of C20H22F9N3O2 This article mentions the following:

Dravet syndrome is a catastrophic childhood epilepsy with multiple seizure types that are refractory to treatment. The endocannabinoid system regulates neuronal excitability so a deficit in endocannabinoid signaling could lead to hyperexcitability and seizures. Thus, we sought to determine whether a deficiency in the endocannabinoid system might contribute to seizure phenotypes in a mouse model of Dravet syndrome and whether enhancing endocannabinoid tone is anticonvulsant. Scn1a+/- mice model the clin. features of Dravet syndrome: hyperthermia-induced seizures, spontaneous seizures and reduced survival. We examined whether Scn1a+/- mice exhibit deficits in the endocannabinoid system by measuring brain cannabinoid receptor expression and endocannabinoid concentrations Next, we determined whether pharmacol. enhanced endocannabinoid tone was anticonvulsant in Scn1a+/- mice. We used GAT229, a pos. allosteric modulator of the cannabinoid (CB1) receptor, and ABX-1431, a compound that inhibits the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). The Scn1a+/- phenotype is strain-dependent with mice on a 129S6/SvEvTac (129) genetic background having no overt phenotype and those on an F1 (129S6/SvEvTac x C57BL/6J) background exhibiting a severe epilepsy phenotype. We observed lower brain cannabinoid CB1 receptor expression in the seizure-susceptible F1 compared to seizure-resistant 129 strain, suggesting an endocannabinoid deficiency might contribute to seizure susceptibility. GAT229 and ABX-1431 were anticonvulsant against hyperthermia-induced seizures. However, subchronic ABX1431 treatment increased spontaneous seizure frequency despite reducing seizure severity. Cnr1 is a putative genetic modifier of epilepsy in the Scn1a+/- mouse model of Dravet syndrome. Compounds that increase endocannabinoid tone could be developed as novel treatments for Dravet syndrome. In the experiment, the researchers used many compounds, for example, 1,1,1,3,3,3-Hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (cas: 1446817-84-0Computed Properties of C20H22F9N3O2).

1,1,1,3,3,3-Hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate (cas: 1446817-84-0) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Computed Properties of C20H22F9N3O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Stanicki, Dimitri et al. published their research in Pharmaceuticals in 2013 | CAS: 7479-12-1

4,4′-(Piperazine-1,4-diyl)dianiline (cas: 7479-12-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

Diamidines versus monoamidines as anti-Pneumocystis agents: an in vivo study was written by Stanicki, Dimitri;Pottier, Muriel;Gantois, Nausicaa;Pincon, Claire;Forge, Delphine;Mahieu, Isabelle;Boutry, Sebastien;Vanden Eynde, Jean Jacques;Martinez, Ann;Dei-Cas, Eduardo;Aliouat, El-Moukhtar. And the article was included in Pharmaceuticals in 2013.Category: piperazines This article mentions the following:

Some compounds articulated around a piperazine or an ethylenediamine linker have been evaluated in vitro to determine their activity in the presence of a 3T6 fibroblast cell line and an axenic culture of Pneumocystis carinii, resp. The most efficient antifungal derivatives, namely N,N’-bis(benzamidine-4-yl)ethane-1,2-diamine (compound 6, a diamidine) and N-(benzamidine-4-yl)-N’-phenylethane-1,2-diamine (compound 7, a monoamidine), exhibited no cytotoxicity and were evaluated in vivo in a rat model. Only the diamidine 6 emerged as a promising hit for further studies. In the experiment, the researchers used many compounds, for example, 4,4′-(Piperazine-1,4-diyl)dianiline (cas: 7479-12-1Category: piperazines).

4,4′-(Piperazine-1,4-diyl)dianiline (cas: 7479-12-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Suzuki, Mikio et al. published their research in Nippon Yakurigaku Zasshi in 2019 | CAS: 913611-97-9

7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 913611-97-9) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Recommanded Product: 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one

Preclinical pharmacological profiles and clinical efficacy of the novel antipsychotic drug brexpiprazole (REXULTI Tablets 1 mg, 2 mg) was written by Suzuki, Mikio;Niidome, Kazunari;Maeda, Kenji;Kikuchi, Tetsuro;Usami, Tomohiro;Futamura, Takashi. And the article was included in Nippon Yakurigaku Zasshi in 2019.Recommanded Product: 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one This article mentions the following:

Brexpiprazole (Rexulti) is the second antipsychotic agent in the world with dopamine D2 receptor partial agonist which was developed by Otsuka Pharmaceutical Co. Ltd. It is categorized as “Serotonin- dopamine Activity Modulator (SDAM)” that regulates both serotoninergic and dopaminergic systems by acting as a partial agonist for serotonin 5-HT1A receptors and D2 receptors and as an antagonist for 5-HT2A receptors. In preclin. pharmacol. studies, brexpiprazole showed the equivalent antipsychotic-like effects to those of other atypical antipsychotics. And it was suggested that brexpiprazole has the low potentials to induce extrapyramidal symptoms, hyperprolactinemia and tardive dyskinesia, with improvement effects on cognitive dysfunction. Furthermore, brexpiprazole has the weak effects on histamine H1 receptors which are associated with sedation and weight gain in clin. In the clin. trials in patients with schizophrenia in both acute and maintenance phase, brexpiprazole showed improvement of antipsychotic effects against placebo, and low incidence of adverse events, e.g., extrapyramidal symptoms, hyperprolactinemia, and weight gain, as suggested in preclin. studies. Furthermore, brexpiprazole showed low incidence of metabolic abnormalities. In particular, brexpiprazole showed relatively low incidences of akathisia, insomnia and agitation which has been commonly reported with aripiprazole. This would be based on the pharmacol. features of brexpiprazole that is more potent antagonism at 5-HT2A receptors and D2 receptors partial agonism with lower intrinsic activity compared to those of aripiprazole. In conclusion, brexpiprazole could be one of the antipsychotics with the most rational mechanism of action, and the better efficacy and safety/tolerability profiles would contribute to the treatment of patients with schizophrenia. In the experiment, the researchers used many compounds, for example, 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 913611-97-9Recommanded Product: 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one).

7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one (cas: 913611-97-9) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Recommanded Product: 7-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butoxy)quinolin-2(1H)-one

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics