1428327-31-4 | Heterocyclic Building Blocks-piperazine

Huang, Hui et al. published their research in Journal of Chemical Neuroanatomy in 2021 |CAS: 1428327-31-4

The Article related to schizophrenia p2x7 receptor phencyclidine jnj47965567, cognitive disorder, p2x7 receptor, pcp, schizophrenia, Placeholder for records without volume info and other aspects.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

On October 31, 2021, Huang, Hui; Zheng, Suyue; Chen, Min; Xie, Liyuan; Li, Ziyi; Guo, Min; Wang, Jianhong; Lu, Mingwei; Zhu, Xingen published an article.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide The title of the article was The potential of the P2X7 receptor as a therapeutic target in a sub-chronic PCP-induced rodent model of schizophrenia. And the article contained the following:

We studied the role of the P2X7 receptor on cognitive dysfunction in a mouse model of schizophrenia. An adult mouse model was established by treatment with phencyclidine (PCP), an N-methyl-D-aspartate (NMDA) receptor antagonist. Young mice were divided into three groups: (1) the control (saline-injected) group; (2) exptl. 5 mg/kg PCP-injected group; and (3) exptl. 10 mg/kg PCP-injected group. The mice were subjected to the open-field and Morris water maze tests at 7 wk. After i.p. injection of the P2X7 receptor antagonist JNJ-47965567, the behavior tests were performed again. Samples were taken after testing. The P2X7 receptor protein and mRNA expression levels were detected by immunohistochem., Western blotting and PCR. This study revealed that the infant sub-chronic PCP mice model showed severe spatial learning and memory impairment in the Morris water maze and schizophrenia-like symptoms (hypermotor behavior) in the open-field test. The P2X7 receptor protein was highly expressed in the sub-chronic PCP mouse model and more highly expressed in the hippocampus than the prefrontal lobe. After the P2X7 receptor was blocked with JNJ-47965567, P2X7 receptor protein and mRNA expression in the frontal lobe were significantly increased, and the spatial memory impairment and hypermotor behavior induced by PCP were reversed. PCP-induced cognitive impairment can be significantly improved by antagonizing the P2X7 receptor. Therefore, we believe that the P2X7 receptor plays an important role in the cognition of schizophrenic-like mice. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

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Dias, Liliana et al. published their research in Cellular and Molecular Life Sciences in 2022 |CAS: 1428327-31-4

The Article related to amyloid beta adenosine a2a receptor p2y1 p2x7 calcium astrocyte, adenosine a2a receptors, alzheimer’s disease, astrocyte, ca2+ dynamics, p2 receptors, Mammalian Hormones: Neurotransmitters and other aspects.Related Products of 1428327-31-4

On August 31, 2022, Dias, Liliana; Madeira, Daniela; Dias, Rafael; Tome, Angelo R.; Cunha, Rodrigo A.; Agostinho, Paula published an article.Related Products of 1428327-31-4 The title of the article was Aβ1-42 peptides blunt the adenosine A2A receptor-mediated control of the interplay between P2X7 and P2Y1 receptors mediated calcium responses in astrocytes. And the article contained the following:

The contribution of astrocytes to Alzheimer disease (AD) is still ill defined. AD involves an abnormal accumulation of amyloid-β peptides (Aβ) and increased production of danger signals such as ATP. ATP can direct or indirectly, through its metabolism into adenosine, trigger adaptive astrocytic responses resulting from intracellular Ca2+ oscillations. AD also triggers an upregulation of astrocytic adenosine A2A receptors (A2AR), which blockade prevents memory dysfunction in AD. We now investigated how Aβ peptides affect ATP-mediated Ca2+ responses in astrocytes measured by fluorescence live-cell imaging and whether A2AR control astrocytic Ca2+ responses mediated by ATP receptors, mainly P2X7R and P2Y1R. In primary cultures of rat astrocytes exposed to Aβ1-42, ATP-evoked Ca2+ responses had a lower amplitude but a longer duration than in control astrocytes and involved P2X7R and P2Y1R, the former potentiating the later. Moreover, Aβ1-42 exposure increased protein levels of P2Y1R in astrocytes. A2AR antagonism with SCH58261 controlled in a protein kinase A-dependent manner both P2X7R- and P2Y1R-mediated Ca2+ responses in astrocytes. The interplay between these purinoceptors in astrocytes was blunted upon exposure to Aβ1-42. These findings uncover the ability of A2AR to regulate the inter-twinned P2X7R- and P2Y1R-mediated Ca2+ dynamics in astrocytes, which is disrupted in conditions of early AD. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Related Products of 1428327-31-4

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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Huang, Hui et al. published their research in Journal of Chemical Neuroanatomy in 2021 |CAS: 1428327-31-4

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

Han, Yue et al. published their research in Purinergic Signalling |CAS: 1428327-31-4

The Article related to atractylenolide anticancer agent p2x7 receptor cervical cancer, atractylenolide i, hela cells, human cervical cancer cells, p2x7rs, siha cells, Placeholder for records without volume info and other aspects.HPLC of Formula: 1428327-31-4

Han, Yue; Bai, Can; He, Xi-Meng; Ren, Qing-Ling published an article in , the title of the article was P2X7 receptor involved in antitumor activity of atractylenolide I in human cervical cancer cells.HPLC of Formula: 1428327-31-4 And the article contains the following content:

Atractylenolide I (Atr-I) was found to sensitize a variety of human cancer cells in previous studies. Purinergic P2X7R plays important role in different cancers. However, whether Atr-I could generate antitumor activity in human cervical cancer cells and P2X7R get involved in this effect remain unclear. In this study, Hela (HPV 18 +) and SiHa (HPV 16 +) cells were treated with different doses of Atr-I. The results indicated that agonist and antagonist of P2X7 receptors, BzATP and JNJ-47965567 (JNJ), could suppress the proliferation of Hela and SiHa cells. Atr-I demonstrated a considerable antitumor effect in both human cervical cancer cells in vitro. Atr-I combined with P2X7R agonist, BzATP, restored Atr-I-induced growth inhibition in Hela cells but not in SiHa cells. However, the combinatorial treatment of P2X7R antagonist JNJ and Atr-I has an additive effect on cell growth inhibition in SiHa cells rather than in Hela cells. It implied that P2X7R would get involved in the anti-human cervical cancer cells effect of Atr-I. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).HPLC of Formula: 1428327-31-4

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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Han, Yue et al. published their research in Purinergic Signalling |CAS: 1428327-31-4

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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Perfettini, Jean-Luc et al. published their patent in 2021 |CAS: 1428327-31-4

The Article related to purinergic receptors modulators sars cov2 covid19 respiratory system disease, Pharmacology: Effects Of Gastrointestinal and Respiratory Drugs and other aspects.Quality Control of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

On December 9, 2021, Perfettini, Jean-Luc; Lecuyer, Deborah; Tannous, Desiree; Allouch, Awatef; Delelis, Olivier; Subra, Frederic published a patent.Quality Control of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide The title of the patent was Modulators of purinergic receptors and related immune checkpoint for treating acute respiratory distress syndrome. And the patent contained the following:

The inventors herein show that purinergic receptors regulate the conversion of macrophage pro-inflammatory reprogramming into anti-inflammatory phenotype in patients suffering from COVID-19 disease. Moreover, they show that P2Y receptor agonists repress NLRP3 inflammasome-dependent IL-1b secretion, but also impair the replication and the cytopathogenic effects of SARS-CoV-2. These results therefore suggest that some purinergic receptors agonists can treat acute lung injury and respiratory disease that are associated with SARS-CoV-2 infection. In addition, their results show that antagonists of the purinergic receptors P2X impair the replication of said virus. The present invention therefore proposes to use purinergic receptors modulators and NLR3-P2Y2R immune checkpoint modulators to treat patients suffering from a virus-induced acute respiratory distress syndrome. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Quality Control of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

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Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Perfettini, Jean-Luc et al. published their patent in 2021 |CAS: 1428327-31-4

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

Platania, Chiara Bianca Maria et al. published their research in Biochemical Pharmacology (Amsterdam, Netherlands) in 2017 |CAS: 1428327-31-4

The Article related to p2x7 receptor antagonism diabetic retinopathy, diabetic retinopathy, il-1尾, inflammation, molecular modeling, p2x7 receptor, pericytes, Pharmacology: Effects Of Agents For Treating Metabolic and Endocrine Disorders and other aspects.COA of Formula: C28H32N4O2S

On August 15, 2017, Platania, Chiara Bianca Maria; Giurdanella, Giovanni; Di Paola, Luisa; Leggio, Gian Marco; Drago, Filippo; Salomone, Salvatore; Bucolo, Claudio published an article.COA of Formula: C28H32N4O2S The title of the article was P2X7 receptor antagonism: Implications in diabetic retinopathy. And the article contained the following:

Diabetic retinopathy (DR) is the most frequent complication of diabetes and one of leading causes of blindness worldwide. Early phases of DR are characterized by retinal pericyte loss mainly related to concurrent inflammatory process. Recently, an important link between P2X7 receptor (P2X7R) and inflammation has been demonstrated indicating this receptor as potential pharmacol. target in DR. Here the authors first carried out an in silico mol. modeling study in order to characterize the allosteric pocket in P2X7R, and identify a suitable P2X7R antagonist through mol. docking. JNJ47965567 was identified as the hit compound in docking calculations, as well as for its absorption, distribution, metabolism and excretion (ADME) profile. As an in vitro model of early diabetic retinopathy, human retinal pericytes were exposed to high glucose (25 mM, 48 h) that caused a significant (p < 0.05) release of IL-1尾 and LDH. The block of P2X7R by JNJ47965567 significantly (p < 0.05) reverted the damage elicited by high glucose, detected as IL-1尾 and LDH release. Overall, the findings suggest that the P2X7R represents an attractive pharmacol. target to manage the early phase of diabetic retinopathy, and the compound JNJ47965567 is a good template to discover other P2X7R selective antagonists. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).COA of Formula: C28H32N4O2S

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Zhao, Ya-Fei et al. published their research in International Journal of Molecular Sciences in 2022 |CAS: 1428327-31-4

The Article related to acute stress depression astrocyte microglia receptor rodent hippocampus, p2x7 receptor, extracellular atp, hippocampus, major depression, mouse, rat, Mammalian Pathological Biochemistry: Nervous System and Psychiatric Diseases and other aspects.Electric Literature of 1428327-31-4

Zhao, Ya-Fei; Ren, Wen-Jing; Zhang, Ying; He, Jin-Rong; Yin, Hai-Yan; Liao, Yang; Rubini, Patrizia; Deussing, Jan M.; Verkhratsky, Alexei; Yuan, Zeng-Qiang; Illes, Peter; Tang, Yong published an article in 2022, the title of the article was High, in Contrast to Low Levels of Acute Stress Induce Depressive-like Behavior by Involving Astrocytic, in Addition to Microglial P2X7 Receptors in the Rodent Hippocampus.Electric Literature of 1428327-31-4 And the article contains the following content:

Extracellular ATP (ATP) in the brain is suggested to be an etiol. factor of major depressive disorder (MDD). It has been assumed that stress-released ATP stimulates P2X7 receptors (Rs) at the microglia, thereby causing neuroinflammation; however, other central nervous system (CNS) cell types such as astrocytes also possess P2X7Rs. In order to elucidate the possible involvement of the MDD-relevant hippocampal astrocytes in the development of a depressive-like state, we used various behavioral tests (tail suspension test [TST], forced swim test [FST], restraint stress, inescapable foot shock, unpredictable chronic mild stress [UCMS]), as well as fluorescence immunohistochem., and patch-clamp electrophysiol. in wild-type (WT) and genetically manipulated rodents. The TST and FST resulted in learned helplessness manifested as a prolongation of the immobility time, while inescapable foot shock caused lower sucrose consumption as a sign of anhedonia. We confirmed the participation of P2X7Rs in the development of the depressive-like behaviors in all forms of acute (TST, FST, foot shock) and chronic stress (UCMS) in the rodent models used. Further, pharmacol. agonists and antagonists acted in a different manner in rats and mice due to their diverse potencies at the resp. receptor orthologs. In hippocampal slices of mice and rats, only foot shock increased the current responses to locally applied dibenzoyl-ATP (Bz-ATP) in CA1 astrocytes; in contrast, TST and restraint depressed these responses. Following stressful stimuli, immunohistochem. demonstrated an increased co-localization of P2X7Rs with a microglial marker, but no change in co-localization with an astroglial marker. Pharmacol. damage to the microglia and astroglia has proven the significance of the microglia for mediating all types of depression-like behavioral reactions, while the astroglia participated only in reactions induced by strong stressors, such as foot shock. Because, in addition to acute stressors, their chronic counterparts induce a depressive-like state in rodents via P2X7R activation, we suggest that our data may have relevance for the etiol. of MDD in humans. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Electric Literature of 1428327-31-4

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Garrosa-Jimenez, Javier et al. published their research in Neuroscience Letters in 2021 |CAS: 1428327-31-4

The Article related to human mdd calcium inflammatory marker purinergic stimulation monocyte, calcium homeostasis, inflammation, major depression disorder, p2x7 receptors, Mammalian Pathological Biochemistry: Nervous System and Psychiatric Diseases and other aspects.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

On November 20, 2021, Garrosa-Jimenez, Javier; Sanchez Carro, Yolanda; Ovejero-Benito, Maria C.; del Sastre, Eric; Garcia, Antonio G.; Lopez, Manuela G.; Lopez-Garcia, Pilar; Cano-Abad, Maria F. published an article.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide The title of the article was Intracellular calcium and inflammatory markers, mediated by purinergic stimulation, are differentially regulated in monocytes of patients with major depressive disorder. And the article contained the following:

The P2X7 receptor (P2X7R) is a ligand-gated ion channel that is being recognized as a major player in neuropsychiatric disorders such as Major Depressive Disorder (MDD). P2X7R activation is triggered by high extracellular ATP concentrations, leading to channel opening and inducing an increase in cytosolic calcium concentration ([Ca2+]c), that activates the inflammatory pathway. Those receptors are expressed not only in CNS cells but also in peripheral blood cells, where they are activated in response to inflammatory mols. such as bacterial lipopolysaccharide (LPS). LPS induced-tissue damage promotes an elevation of extracellular ATP, triggering the NRLP3-inflammasome assembly and activation that, sequentially, induces caspase-1 cleavage and IL-1尾 processing and secretion. In this context, we attempt to understand the role of P2X7R in [Ca2+]c homeostasis regulation, inflammasome expression and its pharmacol. modulation in MDD. For this purpose, monocytes were isolated from peripheral blood of MDD patients and [Ca2+]c was monitored with the intracellular probe Fura-2. Our results point out to P2X7R as the responsible of the Ca2+ imbalance, as well as TNF-伪-dependent activation of caspase-1 in MDD patients. In addition, P2X7R blockade with its specific antagonist, JNJ-47965567, reduces the Ca2+ entry upon Bz-ATP exposure. Altogether, our results point that MDD patients have both, Ca2+ homeostasis alteration and an inflammatory status, which promote an independent-inflammasome activation of caspase-1. Therefore, we propose the pharmacol. modulation of P2X7R as a therapeutic approach against MDD symptoms. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

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