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[PMID]:26690045
[Au] Autor:Ruokolainen M; Gul T; Permentier H; Sikanen T; Kostiainen R; Kotiaho T
[Ad] Endereço:Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56 (Viikinkaari 5E), FI-00014, Finland. Electronic address: miina.ruokolainen@helsinki.fi.
[Ti] Título:Comparison of TiO2 photocatalysis, electrochemically assisted Fenton reaction and direct electrochemistry for simulation of phase I metabolism reactions of drugs.
[So] Source:Eur J Pharm Sci;83:36-44, 2016 Feb 15.
[Is] ISSN:1879-0720
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The feasibility of titanium dioxide (TiO2) photocatalysis, electrochemically assisted Fenton reaction (EC-Fenton) and direct electrochemical oxidation (EC) for simulation of phase I metabolism of drugs was studied by comparing the reaction products of buspirone, promazine, testosterone and 7-ethoxycoumarin with phase I metabolites of the same compounds produced in vitro by human liver microsomes (HLM). Reaction products were analysed by UHPLC-MS. TiO2 photocatalysis simulated the in vitro phase I metabolism in HLM more comprehensively than did EC-Fenton or EC. Even though TiO2 photocatalysis, EC-Fenton and EC do not allow comprehensive prediction of phase I metabolism, all three methods produce several important metabolites without the need for demanding purification steps to remove the biological matrix. Importantly, TiO2 photocatalysis produces aliphatic and aromatic hydroxylation products where direct EC fails. Furthermore, TiO2 photocatalysis is an extremely rapid, simple and inexpensive way to generate oxidation products in a clean matrix and the reaction can be simply initiated and quenched by switching the UV lamp on/off.
[Mh] Termos MeSH primário: Buspirona/química
Cumarínicos/química
Promazina/química
Testosterona/química
Titânio/química
[Mh] Termos MeSH secundário: Buspirona/metabolismo
Catálise
Cumarínicos/metabolismo
Remoção de Radical Alquila
Eletroquímica
Seres Humanos
Hidrogenação
Hidroxilação
Ferro/química
Microssomos Hepáticos/metabolismo
Oxirredução
Promazina/metabolismo
Testosterona/metabolismo
Titânio/efeitos da radiação
Raios Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Coumarins); 15FIX9V2JP (titanium dioxide); 31005-02-4 (7-ethoxycoumarin); 3XMK78S47O (Testosterone); D1JT611TNE (Titanium); E1UOL152H7 (Iron); O9M39HTM5W (Promazine); TK65WKS8HL (Buspirone)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151223
[St] Status:MEDLINE


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[PMID]:25615803
[Au] Autor:Wang Q; Liu L; Yang X; Wang K; Chen N; Zhou C; Luo B; Du S
[Ad] Endereço:State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Key Laboratory for Bio-Nanotechnology and Molecular Engineering of Hunan Province, Hunan University , Changsha, Hunan 410082, P. R. China.
[Ti] Título:Evaluation of medicine effects on the interaction of myoglobin and its aptamer or antibody using atomic force microscopy.
[So] Source:Anal Chem;87(4):2242-8, 2015 Feb 17.
[Is] ISSN:1520-6882
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The effects of medicine on the biomolecular interaction have been given increasing attention in biochemistry and affinity-based analytics since the environment in vivo is complex especially for the patients. Herein, myoglobin, a biomarker of acute myocardial infarction, was used as a model, and the medicine effects on the interactions of myoglobin/aptamer and myoglobin/antibody were systematically investigated using atomic force microscopy (AFM) for the first time. The results showed that the average binding force and the binding probability of myoglobin/aptamer almost remained unchanged after myoglobin-modified gold substrate was incubated with promazine, amoxicillin, aspirin, and sodium penicillin, respectively. These parameters were changed for myoglobin/antibody after the myoglobin-modified gold substrate was treated with these medicines. For promazine and amoxicillin, they resulted in the change of binding force distribution of myoglobin/antibody (i.e., from unimodal distribution to bimodal distribution) and the increase of binding probability; for aspirin, it only resulted in the change of the binding force distribution, and for sodium penicillin, it resulted in the increase of the average binding force and the binding probability. These results may be attributed to the different interaction modes and binding sites between myoglobin/aptamer and myoglobin/antibody, the different structures between aptamer and antibody, and the effects of medicines on the conformations of myoglobin. These findings could enrich our understanding of medicine effects on the interactions of aptamer and antibody to their target proteins. Moreover, this work will lay a good foundation for better research and extensive applications of biomolecular interaction, especially in the design of biosensors in complex systems.
[Mh] Termos MeSH primário: Anticorpos/química
Aptâmeros de Nucleotídeos/química
Microscopia de Força Atômica
Mioglobina/química
[Mh] Termos MeSH secundário: Amoxicilina/química
Amoxicilina/farmacologia
Anticorpos/metabolismo
Aptâmeros de Nucleotídeos/metabolismo
Aspirina/química
Aspirina/farmacologia
Sítios de Ligação/efeitos dos fármacos
Biomarcadores/química
Biomarcadores/metabolismo
Ouro/química
Mioglobina/metabolismo
Penicilina G/química
Penicilina G/farmacologia
Promazina/química
Promazina/farmacologia
Ligação Proteica/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antibodies); 0 (Aptamers, Nucleotide); 0 (Biomarkers); 0 (Myoglobin); 7440-57-5 (Gold); 804826J2HU (Amoxicillin); O9M39HTM5W (Promazine); Q42T66VG0C (Penicillin G); R16CO5Y76E (Aspirin)
[Em] Mês de entrada:1511
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150124
[St] Status:MEDLINE
[do] DOI:10.1021/ac503885e


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[PMID]:25499340
[Au] Autor:La Rocca R; Ferrari-Toninelli G; Patanè S
[Ad] Endereço:Resp. U.O. Medicina Generale, Istituto Clinico Città di Brescia, Brescia, Italy.
[Ti] Título:Widened QRS interval and left ventricular systolic depression after propafenone and promazine exposure.
[So] Source:Int J Cardiol;177(1):57-60, 2014 Nov 15.
[Is] ISSN:1874-1754
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Mh] Termos MeSH primário: Fibrilação Atrial/tratamento farmacológico
Demência/tratamento farmacológico
Eletrocardiografia/efeitos dos fármacos
Promazina/efeitos adversos
Propafenona/efeitos adversos
Torsades de Pointes/induzido quimicamente
Função Ventricular Esquerda/efeitos dos fármacos
[Mh] Termos MeSH secundário: Idoso de 80 Anos ou mais
Antiarrítmicos/efeitos adversos
Fibrilação Atrial/complicações
Fibrilação Atrial/fisiopatologia
Demência/complicações
Antagonistas de Dopamina/efeitos adversos
Relação Dose-Resposta a Droga
Interações Medicamentosas
Quimioterapia Combinada
Feminino
Ventrículos do Coração/efeitos dos fármacos
Ventrículos do Coração/fisiopatologia
Seres Humanos
Promazina/administração & dosagem
Propafenona/administração & dosagem
Torsades de Pointes/fisiopatologia
[Pt] Tipo de publicação:CASE REPORTS; LETTER
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 0 (Dopamine Antagonists); 68IQX3T69U (Propafenone); O9M39HTM5W (Promazine)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:141217
[Lr] Data última revisão:
141217
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141216
[St] Status:MEDLINE


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[PMID]:25148730
[Au] Autor:Simon A; Alexandru T; Boni M; Damian V; Stoicu A; Dutschk V; Pascu ML
[Ad] Endereço:Laser Department, National Institute for Laser, Plasma and Radiation Physics, 409 Atomistilor, 077125, Magurele, Ilfov, Romania; Faculty of Physics, University of Bucharest, 405 Atomistilor, 077125, Magurele, Ilfov, Romania. Electronic address: agota.simon@inflpr.ro.
[Ti] Título:Interaction of solutions containing phenothiazines exposed to laser radiation with materials surfaces, in view of biomedical applications.
[So] Source:Int J Pharm;475(1-2):270-81, 2014 Nov 20.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Phenothiazine drugs - chlorpromazine (CPZ), promazine (PZ) and promethazine (PMZ) - were exposed to 266 nm (fourth harmonic of the Nd:YAG pulsed laser radiation) in order to be modified at molecular level and to produce an enhancement of their antibacterial activity. The irradiated samples were analysed by several methods: pH and surface tension measurements, UV-vis-NIR absorption spectroscopy, laser induced fluorescence and thin layer chromatography. The purpose of these investigations was to study and describe the modified properties of the medicines to further investigate their specific interactions with materials such as cotton, polyester and Parafilm M as a model smooth surface. The textile materials may be impregnated with phenothiazines drug solutions exposed to laser radiation in order to be used in treatments applied on the surface of the organism. Some of the phenothiazines solutions exposed prolonged time intervals to laser radiation have much better activity against several bacteria. Therefore, in the paper, it is reported the wetting behaviour of CPZ, PZ and PMZ solutions, irradiated for time intervals between 1 and 240 min, on the surfaces of the three textures in order to draw a conclusion about their wettability as a function of time.
[Mh] Termos MeSH primário: Fenotiazinas/química
Soluções/química
[Mh] Termos MeSH secundário: Antibacterianos/química
Clorpromazina/química
Cromatografia em Camada Delgada/métodos
Fibra de Algodão
Concentração de Íons de Hidrogênio
Lasers
Parafina/química
Poliésteres/química
Promazina/química
Prometazina/química
Tensão Superficial
Molhabilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Phenothiazines); 0 (Polyesters); 0 (Solutions); 8002-74-2 (Paraffin); FF28EJQ494 (Promethazine); GS9EX7QNU6 (phenothiazine); O9M39HTM5W (Promazine); U42B7VYA4P (Chlorpromazine)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:141202
[Lr] Data última revisão:
141202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140824
[St] Status:MEDLINE


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[PMID]:24840407
[Au] Autor:Dziomba S; Biernacki M; Oledzka I; Skrzydlewska E; Baczek T; Kowalski P
[Ad] Endereço:Department of Pharmaceutical Chemistry, Medical University of Gdansk, Hallera 107, 80-416 Gdansk, Poland.
[Ti] Título:Repetitive injection field-amplified sample stacking for cationic compounds determination.
[So] Source:Talanta;125:1-6, 2014 Jul.
[Is] ISSN:1873-3573
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The development of a field-amplified sample stacking technique is presented. Sensitivity enhancement in this technique was obtained by repetitive injections of a sample followed by steps of sample matrix removal through the application of counter-pressure. Under optimized conditions the background electrolyte (BGE) was composed of 80 mM H3PO4 while the sample matrix contained 0.5mM H3PO4 and 30% (v/v) methanol. The elaborated method enabled a 4-fold effective injection of the sample (53 s, 0.5 psi). Each injection was followed by a focusing step during which the application of a voltage (2 kV) and counter-pressure (-1 psi) was performed for 0.65 min. The method was developed for the determination of six psychiatric drugs (opipramol, hydroxyzine, promazine, amitriptyline, fluoxetine, and thioridazine). The elaborated method was applied for analysis of human urine samples after a simple liquid-liquid extraction procedure. The detection limits obtained were in the range of 2.23-6.21 ng/mL.
[Mh] Termos MeSH primário: Urinálise/métodos
[Mh] Termos MeSH secundário: Amitriptilina/urina
Antidepressivos Tricíclicos/urina
Calibragem
Cátions
Eletrólitos
Eletroforese
Eletroforese Capilar
Fluoxetina/urina
Seres Humanos
Concentração de Íons de Hidrogênio
Hidroxizina/urina
Limite de Detecção
Opipramol/urina
Ácidos Fosfóricos/química
Pressão
Promazina/urina
Solventes/química
Temperatura Ambiente
Tioridazina/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Antidepressive Agents, Tricyclic); 0 (Cations); 0 (Electrolytes); 0 (Phosphoric Acids); 0 (Solvents); 01K63SUP8D (Fluoxetine); 1806D8D52K (Amitriptyline); 30S50YM8OG (Hydroxyzine); D23ZXO613C (Opipramol); E4GA8884NN (phosphoric acid); N3D6TG58NI (Thioridazine); O9M39HTM5W (Promazine)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:140520
[Lr] Data última revisão:
140520
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140521
[St] Status:MEDLINE


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[PMID]:24373770
[Au] Autor:Baral PK; Swayampakula M; Rout MK; Kav NN; Spyracopoulos L; Aguzzi A; James MN
[Ad] Endereço:Department of Biochemistry, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB T6G 2H7, Canada.
[Ti] Título:Structural basis of prion inhibition by phenothiazine compounds.
[So] Source:Structure;22(2):291-303, 2014 Feb 04.
[Is] ISSN:1878-4186
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Conformational transitions of the cellular form of the prion protein, PrP(C), into an infectious isoform, PrP(Sc), are considered to be central events in the progression of fatal neurodegenerative diseases known as transmissible spongiform encephalopathies. Tricyclic phenothiazine compounds exhibit antiprion activity; however, the underlying molecular mechanism of PrP(Sc) inhibition remains elusive. We report the molecular structures of two phenothiazine compounds, promazine and chlorpromazine bound to a binding pocket formed at the intersection of the structured and the unstructured domains of the mouse prion protein. Promazine binding induces structural rearrangement of the unstructured region proximal to ß1, through the formation of a "hydrophobic anchor." We demonstrate that these molecules, promazine in particular, allosterically stabilize the misfolding initiator-motifs such as the C terminus of α2, the α2-α3 loop, as well as the polymorphic ß2-α2 loop. Hence, the stabilization effects of the phenothiazine derivatives on initiator-motifs induce a PrP(C) isoform that potentially resists oligomerization.
[Mh] Termos MeSH primário: Fenotiazinas/química
Príons/química
[Mh] Termos MeSH secundário: Sítio Alostérico
Motivos de Aminoácidos
Animais
Sítios de Ligação
Clorpromazina/química
Camundongos
Simulação de Dinâmica Molecular
Promazina/química
Ligação Proteica
Desnaturação Proteica
Dobramento de Proteína
Isoformas de Proteínas/química
Estrutura Secundária de Proteína
Estrutura Terciária de Proteína
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Phenothiazines); 0 (Prions); 0 (Protein Isoforms); GS9EX7QNU6 (phenothiazine); O9M39HTM5W (Promazine); U42B7VYA4P (Chlorpromazine)
[Em] Mês de entrada:1410
[Cu] Atualização por classe:140210
[Lr] Data última revisão:
140210
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131231
[St] Status:MEDLINE


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[PMID]:23856051
[Au] Autor:Sun H; Xia M; Shahane SA; Jadhav A; Austin CP; Huang R
[Ad] Endereço:National Center for Advancing Translational Sciences, National Institutes of Health (NIH), 9800 Medical Center Drive, Bethesda, Rockville, MD 20892, USA. sunh7@mail.nih.gov
[Ti] Título:Are hERG channel blockers also phospholipidosis inducers?
[So] Source:Bioorg Med Chem Lett;23(16):4587-90, 2013 Aug 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Both pharmacophore models of the human ether-à-go-go-related gene (hERG) channel blockers and phospholipidosis (PLD) inducers contain a hydrophobic moiety and a hydrophilic motif/positively charged center, so it is interesting to investigate the overlap between the ligand chemical spaces of both targets. We have assayed over 4000 non-redundant drug-like compounds for both their hERG inhibitory activity and PLD inducing potential in a quantitative high throughput screening (qHTS) format. Seventy-seven percent of PLD inducing compounds identified from the screening were also found to be hERG channel blockers, and 96.9% of the dually active compounds were positively charged. Among the 48 compounds that induced PLD without inhibiting hERG channel, 24 compounds (50.0%) carried steroidal structures. According to our results, hERG channel blockers and PLD inducers share a large chemical space. In addition, a positively charged hERG channel blocker will most likely induce PLD, while a steroid PLD inducer is less likely a hERG channel blocker.
[Mh] Termos MeSH primário: Lipidoses/induzido quimicamente
Fosfolipídeos/metabolismo
[Mh] Termos MeSH secundário: Antipsicóticos/química
Antipsicóticos/farmacologia
Canais de Potássio Éter-A-Go-Go/antagonistas & inibidores
Seres Humanos
Interações Hidrofóbicas e Hidrofílicas
Estrutura Molecular
Fosfolipídeos/química
Promazina/química
Promazina/metabolismo
Promazina/farmacologia
Relação Quantitativa Estrutura-Atividade
Esteroides/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Ether-A-Go-Go Potassium Channels); 0 (Phospholipids); 0 (Steroids); O9M39HTM5W (Promazine)
[Em] Mês de entrada:1401
[Cu] Atualização por classe:161203
[Lr] Data última revisão:
161203
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130717
[St] Status:MEDLINE


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[PMID]:23261572
[Au] Autor:Khan IA; Anjum K; Koya PA; Kabir-Ud-Din
[Ad] Endereço:Department of Chemistry, Aligarh Muslim University, Aligarh 202 002, India. driqrarakhan@gmail.com
[Ti] Título:Effect of inorganic salts on the clouding behavior of hydroxypropyl methyl cellulose in presence of amphiphilic drugs.
[So] Source:Colloids Surf B Biointerfaces;103:496-501, 2013 Mar 01.
[Is] ISSN:1873-4367
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this paper we report the effect of two cationic (imipramine hydrochloride (IMP) and promazine hydrochloride (PMZ)) and one anionic (sodium salt of ibuprofen (IBF)) drugs on the clouding behavior of a nonionic polymer hydroxypropyl methyl cellulose (HPMC). Though all the three drugs increase the cloud point (CP) of HPMC, the effect was found to be minimum in the case of IBF. Further, the effect of adding salts (NaF, NaCl, NaBr, NaNO(3), Na(2)SO(4), Na(3)PO(4), KCl, KBr, KNO(3)) in the presence of amphiphilic drugs (IMP and PMZ) on the CP of HPMC was seen. Almost linear decrease in the CP was observed with the [salt] at fixed concentrations of these drugs whereas in the absence of drugs the decrement in the CP was slight. The energetic parameters (ΔG(c)(0), ΔH(c)(0) and TΔS(c)(0)) were evaluated and it implies that the disruption of water structure becomes significantly prominent at lower concentrations of the drugs at fixed salt concentrations.
[Mh] Termos MeSH primário: Metilcelulose/análogos & derivados
Preparações Farmacêuticas/química
Sais/química
Tensoativos/química
[Mh] Termos MeSH secundário: Ânions
Derivados da Hipromelose
Ibuprofeno/química
Imipramina/química
Metilcelulose/química
Micelas
Modelos Moleculares
Promazina/química
Soluções
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anions); 0 (Micelles); 0 (Pharmaceutical Preparations); 0 (Salts); 0 (Solutions); 0 (Surface-Active Agents); 3NXW29V3WO (Hypromellose Derivatives); 9004-67-5 (Methylcellulose); O9M39HTM5W (Promazine); OGG85SX4E4 (Imipramine); WK2XYI10QM (Ibuprofen)
[Em] Mês de entrada:1308
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:121225
[St] Status:MEDLINE


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[PMID]:23406770
[Au] Autor:Wójcikowski J; Maurel P; Daniel WA
[Ad] Endereço:Department of Pharmacokinetics and Drug Metabolism, Institute of Pharmacology, Polish Academy of Science, Smetna 12, PL 31-343 Kraków, Poland. wojcikow@if-pan.krakow.pl
[Ti] Título:Autoinduction of the metabolism of phenothiazine neuroleptics in a primary culture of human hepatocytes.
[So] Source:Pharmacol Rep;64(6):1578-83, 2012.
[Is] ISSN:1734-1140
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The metabolism of phenothiazine neuroleptics (promazine, perazine) in a primary culture of human hepatocytes after pretreatment of cells with those neuroleptics was studied. METHODS: The hepatocytes were pretreated with 25 µM promazine or perazine for 96 h. Then, the cells were incubated for 2, 4, 6, 8 and 24 h in the presence of neuroleptics. At the indicated time points, concentrations of phenothiazines and their metabolites (5-sulfoxides and N-desmethyl derivatives) were measured in the culture medium using HPLC with UV detection. RESULTS: Pretreatment of the primary culture of human hepatocytes with promazine or perazine resulted in accumulation of their metabolites in the culture medium. Such an effect was not observed in the case of control cultures (not pretreated with neuroleptics). CONCLUSION: The obtained results suggest that the tested phenothiazines may stimulate their own metabolism by inducing CYP1A2, CYP3A4 and CYP2C19 isoforms.
[Mh] Termos MeSH primário: Antipsicóticos/metabolismo
Sistema Enzimático do Citocromo P-450/biossíntese
Hepatócitos/enzimologia
Perazina/metabolismo
Promazina/metabolismo
[Mh] Termos MeSH secundário: Idoso
Antipsicóticos/farmacologia
Biotransformação
Células Cultivadas
Cromatografia Líquida de Alta Pressão
Remoção de Radical Alquila
Indução Enzimática
Feminino
Hepatócitos/efeitos dos fármacos
Seres Humanos
Isoenzimas
Perazina/farmacologia
Cultura Primária de Células
Promazina/farmacologia
Espectrofotometria Ultravioleta
Sulfóxidos/metabolismo
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Isoenzymes); 0 (Sulfoxides); 8915147A2B (Perazine); 9035-51-2 (Cytochrome P-450 Enzyme System); O9M39HTM5W (Promazine)
[Em] Mês de entrada:1307
[Cu] Atualização por classe:140731
[Lr] Data última revisão:
140731
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130215
[St] Status:MEDLINE


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[PMID]:22939256
[Au] Autor:Mahajan S; Mahajan RK
[Ad] Endereço:Department of Chemistry, UGC-Centre for Advanced Studies, Guru Nanak Dev University, Amritsar 143 005, India.
[Ti] Título:Interactions of phenothiazine drugs with bile salts: micellization and binding studies.
[So] Source:J Colloid Interface Sci;387(1):194-204, 2012 Dec 01.
[Is] ISSN:1095-7103
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:An evaluation of the interactions of phenothiazine tranquilizer drugs (promazine hydrochloride; PMZ and promethazine hydrochloride; PMT) with bile salts viz., sodium cholate (NaC) and sodium deoxycholate (NaDC) in aqueous medium, investigated through different physicochemical measurements is presented in this work. The mixed micellization behavior and surface properties of the phenothiazine-bile salt systems have been analyzed by conductivity and surface tension measurements. Application of different theoretical approaches to all the phenothiazine-bile salt mixtures shows a non-ideal behavior. Further, the spectroscopic techniques such as UV-visible and steady state fluorescence have been employed to study the binding of phenothiazines with bile salts. The stoichiometric ratios, binding constants (K), and free energy change (ΔG) for the phenothiazine-bile salt complexes were estimated from the Benesi-Hildebrand (B-H) double reciprocal plots obtained by using the changes in spectral intensities of phenothiazines on addition of bile salts. The results are discussed in the light of use of bile salts as promising drug delivery agents for phenothiazines and hence improve their bioavailabilty.
[Mh] Termos MeSH primário: Ácido Desoxicólico/metabolismo
Promazina/metabolismo
Prometazina/metabolismo
Colato de Sódio/metabolismo
Tranquilizantes/metabolismo
[Mh] Termos MeSH secundário: Micelas
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Micelles); 0 (Tranquilizing Agents); 005990WHZZ (Deoxycholic Acid); FF28EJQ494 (Promethazine); NU3Y4CCH8Z (Sodium Cholate); O9M39HTM5W (Promazine)
[Em] Mês de entrada:1303
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120904
[St] Status:MEDLINE



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