- 関
- perazine、perazine dimalonate、perazine fendizoate
WordNet
- a salt or ester of maleic acid; used as a nontricyclic antidepressant drug for psychomotor activation
UpToDate Contents
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English Journal
- Perazine for schizophrenia.
- Leucht S1, Helfer B, Hartung B.Author information 1Klinik und Poliklinik für Psychiatrie und Psychotherapie, Technische Universität München Klinikum rechts der Isar, Ismaningerstrasse 22, München, Germany, 81675.AbstractBACKGROUND: Perazine is an old phenothiazine derivative used for the treatment of people with schizophrenia and is reputed to have a low level of extrapyramidal adverse effects. As far as we are aware, its use is limited to Germany, Poland, the former Yugoslavia and the Netherlands.
- The Cochrane database of systematic reviews.Cochrane Database Syst Rev.2014 Jan 15;1:CD002832. doi: 10.1002/14651858.CD002832.pub3.
- BACKGROUND: Perazine is an old phenothiazine derivative used for the treatment of people with schizophrenia and is reputed to have a low level of extrapyramidal adverse effects. As far as we are aware, its use is limited to Germany, Poland, the former Yugoslavia and the Netherlands.OBJECTIVES: To ex
- PMID 24425538
- The phenothiazine-class antipsychotic drugs prochlorperazine and trifluoperazine are potent allosteric modulators of the human P2X7 receptor.
- Hempel C1, Nörenberg W1, Sobottka H1, Urban N1, Nicke A2, Fischer W1, Schaefer M3.Author information 1Rudolf-Boehm-Institute of Pharmacology and Toxicology, Medical Faculty, University of Leipzig, Härtelstrasse 16-18, 04107 Leipzig, Germany.2Max-Planck-Institute for Experimental Medicine, Hermann Rein-Str. 3, 37075 Göttingen, Germany.3Rudolf-Boehm-Institute of Pharmacology and Toxicology, Medical Faculty, University of Leipzig, Härtelstrasse 16-18, 04107 Leipzig, Germany. Electronic address: michael.schaefer@medizin.uni-leipzig.de.AbstractP2X7, an ATP-gated cation channel, is involved in immune cell activation, hyperalgesia and neuropathic pain. By regulating cytokine release in the brain, P2X7 has been linked to the pathophysiology of mood disorders and schizophrenia. We here assess the impact of 123 drugs that act in the central nervous system on human P2X7. Most prominently, the tricyclic antipsychotics prochlorperazine (PCP) and trifluoperazine (TFP) potently inhibited P2X7-mediated Ca2+ entry, dye permeation and ionic currents. In divalent cation-containing bath solutions or after prolonged incubation, ATP-evoked P2X7 currents were inhibited by 10 μM PCP. This effect was not related to dopamine receptor antagonism. Surprisingly, PCP co-applied with ATP enhanced inward currents in bath solutions with low divalent cation concentrations. Intracellular perfusion with PCP did not substitute for the extracellularly applied drug, indicating that its binding sites are accessible from the extracellular space. Since P2X7 current potentiation by PCP was voltage-dependent, at least one site may be located within the electrical field of the membrane. While the channel opening and closure kinetic was altered by PCP, the apparent affinity of ATP remained unchanged (potentiation) or changed slightly (inhibition). Measurements in human monocyte-derived macrophages confirmed the PCP-induced inhibition of ATP-evoked Ca2+ influx, Yo-Pro-1 permeability, and whole cell currents. Interestingly, neither heterologously expressed rat or mouse P2X7 nor native P2X7 in rat astrocyte cultures or in mouse bone marrow-derived macrophages were inhibited by perazines with a similar potency. We conclude that perazine-type neuroleptics are potent, but species-selective allosteric modulators of human but not murine P2X7 receptors.
- Neuropharmacology.Neuropharmacology.2013 Dec;75:365-79. doi: 10.1016/j.neuropharm.2013.07.027. Epub 2013 Aug 14.
- P2X7, an ATP-gated cation channel, is involved in immune cell activation, hyperalgesia and neuropathic pain. By regulating cytokine release in the brain, P2X7 has been linked to the pathophysiology of mood disorders and schizophrenia. We here assess the impact of 123 drugs that act in the central ne
- PMID 23954492
- Spectrofluorimetric determination of certain biologically active phenothiazines in commercial dosage forms and human plasma.
- Mohamed AM1, Abdelmageed OH, Salem H, Nagy DM, Omar MA.Author information 1Pharmaceutical Analytical Chemistry Department, faculty of Pharmacy, Assiut University, Assiut, Egypt.AbstractA validated simple and sensitive spectrofluorimetric method was developed for the determination of chlorpromazine hydrochloride, promethazine hydrochloride, trifluperazine hydrochloride, thioridazine hydrochloride, perazine maleate and oxomemazine. The method was based on condensation of malonic acid/acetic anhydride (MAA) under the catalytic effect of the tertiary amine moiety of the studied phenothiazines to provide a deep yellow to brown colour with green fluorescence. Relative fluorescence intensity of the products was measured at λ exc 398 nm and λ em 432 nm. Different variables affecting the reaction were studied and optimized. The method was successfully applied for the determination of the studied drugs in commercial dosage forms. The lower detection limits allowed the application of this method for the determination of the compounds in plasma as an example of a biological fluid. In addition, the method was considered specific for the determination of tertiary amines in the presence of primary and secondary amines; as a result, it was deemed suitable for the determination of the cited drugs in the presence of their degradation products resulting from N-dealkylation or oxidation of the corresponding sulphoxides or sulphones.
- Luminescence : the journal of biological and chemical luminescence.Luminescence.2013 May-Jun;28(3):345-54. doi: 10.1002/bio.2388. Epub 2012 Jul 12.
- A validated simple and sensitive spectrofluorimetric method was developed for the determination of chlorpromazine hydrochloride, promethazine hydrochloride, trifluperazine hydrochloride, thioridazine hydrochloride, perazine maleate and oxomemazine. The method was based on condensation of malonic aci
- PMID 22786713
Japanese Journal
- バルビツール酸系及びベンゾジアゼピン系催眠薬のp-メチルベンジル誘導体化によるHPLC分析
- 三井 利幸,藤村 義和
- 衛生化学 33(2), 113-117, 1987-04-30
- … For the extraction of barbital or nitrazepam from blood sample no interference could be observed with the compounds, such as chloropromazine hydrochloride, perazine maleate, prochloroperazine maleate, glycine, phenyl alanine, glucose, and urea. …
- NAID 110003643371
- Interaction of Phenothiazines with Pectin in Aqueous Solution
- 高橋 靖侑,南部 直樹,永井 恒司
- Chemical & pharmaceutical bulletin 29(3), 828-833, 1981-03-25
- … On the other hand, it was impossible to obtain the γ value (mol of drugs bound per mol of pectin) on Scatchard plots for such slightly soluble drugs as levomepromazine maleate, perazine dimaleate and prochlorperazine dimaleate at higher concentrations. …
- NAID 110003633738
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★リンクテーブル★
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- 英
- perazine、perazine maleate、perazine dimalonate、perazine fendizoate
- 関
- マレイン酸ペラジン、マロン酸ペラジン、フェンジゾ酸ペラジン。プロクロルペラジン
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- 関
- perazine、perazine dimalonate、perazine maleate
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- 関
- perazine、perazine fendizoate、perazine maleate
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- 英
- perazine maleate
- 関
- ペラジン
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- 関
- TFP、trifluoperazine、trifluoperazine hydrochloride
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- 関
- prochlorperazine、prochlorperazine mesilate
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- 関
- thiethylperazine、thiethylperazine malate
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- 関
- butaperazine
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マレイン酸、マレイン酸塩、マレイン酸エステル
- 関
- maleic acid
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ペラジン
- 関
- perazine dimalonate、perazine fendizoate、perazine maleate