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[PMID]:29279438
[Au] Autor:Ebitani M; Ebitani T
[Ad] Endereço:Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University.
[Ti] Título:[Rotational Isomers of Diphenhydramine].
[So] Source:Yakugaku Zasshi;138(3):417-424, 2018 Mar 01.
[Is] ISSN:1347-5231
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo: Diphenhydramine (DP), an antihistaminic agent, may become colored and daker or more fluorescent during storage. Herein, we spectroscopically examined the causes of this phenomenon under various DP storage conditions and durations. The infrared vibration-rotation spectrum shows multiple Gauche (G)-type conformers with different intramolecular n→π interaction strengths. The splitting pattern of the dimethylamino group protons in the H-NMR spectrum indicates that DP is mainly in the G-type with a small portion in the Trans (T)-type. The correlation between the red-shifted peak intensity in the UV•VIS absorbance spectrum and the coloring progression indicates a decreased intramolecular n→π interaction of the G-type under elevated temperature during storage. Enhanced fluorescence detected in the Excitation•Fluorescence spectrum demonstrates G-type (quenching) to T-type (fluorescent) conformation conversion, which is due to activated internal rotation of the dimethylamino group under elevated storage temperature and electronic excitation in the phenyl groups under light irradiation during storage. A signal detected in the ESR spectrum corresponds to the G-type charge transfer (CT) structure wherein part of the nonbonding electron pair on the N atom is intramolecularly redistributed to the phenyl groups. The CT structure presents the G-type quenching characteristics, whereas weak CT bonding corresponds to coloring. The results indicate that the quenching G-type is converted to T-type by heat or light to become color faded and bright with enhanced fluorescence and that T-type is reverted to G-type after storage under cool and dark conditions or by vacuum distillation to lose fluorescence.
[Mh] Termos MeSH primário: Difenidramina/química
Estabilidade de Medicamentos
Armazenamento de Medicamentos
Antagonistas dos Receptores Histamínicos/química
[Mh] Termos MeSH secundário: Cor
Espectroscopia de Ressonância de Spin Eletrônica
Fluorescência
Isomerismo
Luz
Espectroscopia de Ressonância Magnética
Conformação Molecular
Rotação
Espectrometria de Fluorescência
Espectrofotometria Infravermelho
Análise Espectral
Temperatura Ambiente
Vibração
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine Antagonists); 8GTS82S83M (Diphenhydramine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171228
[St] Status:MEDLINE
[do] DOI:10.1248/yakushi.17-00175


  2 / 3037 MEDLINE  
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[PMID]:28866099
[Au] Autor:Takano M; Kamei H; Nagahiro M; Kawami M; Yumoto R
[Ad] Endereço:Department of Pharmaceutics and Therapeutics, Graduate School of Biomedical & Health Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima 734-8553, Japan. Electronic address: takanom@hiroshima-u.ac.jp.
[Ti] Título:Nicotine transport in lung and non-lung epithelial cells.
[So] Source:Life Sci;188:76-82, 2017 Nov 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: Nicotine is rapidly absorbed from the lung alveoli into systemic circulation during cigarette smoking. However, mechanism underlying nicotine transport in alveolar epithelial cells is not well understood to date. In the present study, we characterized nicotine uptake in lung epithelial cell lines A549 and NCI-H441 and in non-lung epithelial cell lines HepG2 and MCF-7. MATERIALS AND METHODS: Characteristics of [ H]nicotine uptake was studied using these cell lines. KEY FINDINGS: Nicotine uptake in A549 cells occurred in a time- and temperature-dependent manner and showed saturation kinetics, with a Km value of 0.31mM. Treatment with some organic cations such as diphenhydramine and pyrilamine inhibited nicotine uptake, whereas treatment with organic cations such as carnitine and tetraethylammonium did not affect nicotine uptake. Extracellular pH markedly affected nicotine uptake, with high nicotine uptake being observed at high pH up to 11.0. Modulation of intracellular pH with ammonium chloride also affected nicotine uptake. Treatment with valinomycin, a potassium ionophore, did not significantly affect nicotine uptake, indicating that nicotine uptake is an electroneutral process. For comparison, we assessed the characteristics of nicotine uptake in another lung epithelial cell line NCI-H441 and in non-lung epithelial cell lines HepG2 and MCF-7. Interestingly, these cell lines showed similar characteristics of nicotine uptake with respect to pH dependency and inhibition by various organic cations. SIGNIFICANCE: The present findings suggest that a similar or the same pH-dependent transport system is involved in nicotine uptake in these cell lines. A novel molecular mechanism of nicotine transport is proposed.
[Mh] Termos MeSH primário: Transporte Biológico/efeitos dos fármacos
Células Epiteliais/metabolismo
Pulmão/metabolismo
Nicotina/farmacocinética
[Mh] Termos MeSH secundário: Carnitina/farmacologia
Células Cultivadas
Difenidramina/farmacologia
Interações Medicamentosas
Seres Humanos
Concentração de Íons de Hidrogênio
Pirilamina/farmacologia
Temperatura Ambiente
Tetraetilamônio/farmacologia
Fatores de Tempo
Trítio/metabolismo
Valinomicina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
10028-17-8 (Tritium); 2001-95-8 (Valinomycin); 66-40-0 (Tetraethylammonium); 6M3C89ZY6R (Nicotine); 8GTS82S83M (Diphenhydramine); HPE317O9TL (Pyrilamine); S7UI8SM58A (Carnitine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170904
[St] Status:MEDLINE


  3 / 3037 MEDLINE  
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[PMID]:28697105
[Au] Autor:Abernathy A; Alsina L; Greer J; Egerman R
[Ad] Endereço:University of Florida College of Medicine, Gainesville, Florida.
[Ti] Título:Transient Fetal Tachycardia After Intravenous Diphenhydramine Administration.
[So] Source:Obstet Gynecol;130(2):374-376, 2017 Aug.
[Is] ISSN:1873-233X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Fetal tachycardia is attributable to a variety of etiologies, including an untreated maternal medical condition or an indicator of potential fetal compromise. Maternal medication administration may also affect the fetal heart rate. CASE: A 28-year-old nulliparous patient at 41 weeks of gestation was treated for pruritus with intravenous diphenhydramine after epidural administration of fentanyl. Within 14 minutes, the fetal heart rate increased from a baseline of 155 beats per minute (bpm) to more than 200 bpm while maintaining moderate variability. This was accompanied by an increase in uterine contractions occurring every 1.5 minutes. The fetal tachycardia lasted 51 minutes; several hours later, a healthy neonate was delivered. CONCLUSION: Diphenhydramine may produce transient fetal tachycardia as well as increased maternal uterine activity.
[Mh] Termos MeSH primário: Difenidramina/efeitos adversos
Doenças Fetais/induzido quimicamente
Frequência Cardíaca Fetal/efeitos dos fármacos
Antagonistas dos Receptores Histamínicos H1/efeitos adversos
Taquicardia/induzido quimicamente
Taquicardia/embriologia
[Mh] Termos MeSH secundário: Administração Intravenosa
Adulto
Analgésicos Opioides
Cesárea
Feminino
Fentanila/efeitos adversos
Idade Gestacional
Seres Humanos
Recém-Nascido
Trabalho de Parto Induzido
Gravidez
Prurido/induzido quimicamente
Prurido/tratamento farmacológico
Contração Uterina/efeitos dos fármacos
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Opioid); 0 (Histamine H1 Antagonists); 8GTS82S83M (Diphenhydramine); UF599785JZ (Fentanyl)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170821
[Lr] Data última revisão:
170821
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170712
[St] Status:MEDLINE
[do] DOI:10.1097/AOG.0000000000002147


  4 / 3037 MEDLINE  
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[PMID]:28421841
[Au] Autor:Johnson J; Williams K; Banner W
[Ad] Endereço:a Oklahoma Center for Poison and Drug Information, University of Oklahoma College of Pharmacy , Oklahoma City , OK , USA.
[Ti] Título:Adolescent with prolonged toxidrome.
[So] Source:Clin Toxicol (Phila);55(5):364-365, 2017 Jun.
[Is] ISSN:1556-9519
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A 13-year-old female was presented to the emergency department following an intentional ingestion. The patient developed significant toxicity including multiple, discreet tonic-clonic seizures. Despite appropriate resuscitation and antidotal management, the patient's symptoms persisted for more than 36 hours post-ingestion. An upright abdominal radiograph was performed revealing a radiopacity suggesting a pharmacobezoar. An esophagogastroduodenoscopy was performed with successful removal of a tennis ball-sized pharmacobezoar. The patient's symptoms subsequently subsided and she recovered fully with no neurologic deficits. Diphenhydramine has not been previously identified as a medication likely to form a pharmacobezoar and has not been shown to be radiopaque. Though bezoar formation is a rare clinical scenario, it is one that toxicologists must consider in patients with clinical courses that persist far beyond expected based on known toxicokinetic principles.
[Mh] Termos MeSH primário: Bezoares/diagnóstico por imagem
Bezoares/terapia
Antagonistas Colinérgicos/envenenamento
Difenidramina/envenenamento
[Mh] Termos MeSH secundário: Adolescente
Overdose de Drogas/terapia
Serviço Hospitalar de Emergência
Endoscopia do Sistema Digestório
Feminino
Seres Humanos
Convulsões/diagnóstico por imagem
Convulsões/terapia
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinergic Antagonists); 8GTS82S83M (Diphenhydramine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170425
[Lr] Data última revisão:
170425
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170420
[St] Status:MEDLINE
[do] DOI:10.1080/15563650.2017.1287912


  5 / 3037 MEDLINE  
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[PMID]:28365158
[Au] Autor:Haddad SP; Du B; Scott WC; Saari GN; Breed C; Kelly M; Broach L; Chambliss CK; Brooks BW
[Ad] Endereço:Department of Environmental Science, Center for Reservoir and Aquatic Systems Research, Baylor University, Waco, TX, USA.
[Ti] Título:Ontogenetic dietary shifts and bioaccumulation of diphenhydramine in Mugil cephalus from an urban estuary.
[So] Source:Mar Environ Res;127:155-162, 2017 Jun.
[Is] ISSN:1879-0291
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Though bioaccumulation of pharmaceuticals has received attention in inland waters, studies of pharmaceutical bioaccumulation in estuarine and marine systems are limited. Further, an understanding of pharmaceutical bioaccumulation across size classes of organisms displaying ontogenetic feeding shifts is lacking. We selected the striped mullet, Mugil cephalus, a euryhaline and eurythermal species that experiences dietary shifts with age, to identify whether a model base, diphenhydramine, accumulated in a tidally influenced urban bayou. We further determined whether diphenhydramine accumulation differed among size classes of striped mullet over a two year study period. Stable isotope analysis identified that ontogenetic feeding shifts of M. cephalus occurred from juveniles to adults. However, bioaccumulation of diphenhydramine did not significantly increase across age classes of M. cephalus but corresponded to surface water levels of the pharmaceutical, which suggests inhalational uptake to diphenhydramine was more important for bioaccumulation than dietary exposure in this urban estuary.
[Mh] Termos MeSH primário: Difenidramina/metabolismo
Monitoramento Ambiental
Estuários
Smegmamorpha/metabolismo
Poluentes Químicos da Água/metabolismo
[Mh] Termos MeSH secundário: Animais
Dieta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Water Pollutants, Chemical); 8GTS82S83M (Diphenhydramine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170623
[Lr] Data última revisão:
170623
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170403
[St] Status:MEDLINE


  6 / 3037 MEDLINE  
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[PMID]:28215473
[Au] Autor:Gao M; Igata H; Takeuchi A; Sato K; Ikegaya Y
[Ad] Endereço:Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo 113-0033, Japan; iPS-non Clinical Experiments for Nervous System (iNCENS) Project, Japan.
[Ti] Título:Machine learning-based prediction of adverse drug effects: An example of seizure-inducing compounds.
[So] Source:J Pharmacol Sci;133(2):70-78, 2017 Feb.
[Is] ISSN:1347-8648
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Various biological factors have been implicated in convulsive seizures, involving side effects of drugs. For the preclinical safety assessment of drug development, it is difficult to predict seizure-inducing side effects. Here, we introduced a machine learning-based in vitro system designed to detect seizure-inducing side effects. We recorded local field potentials from the CA1 alveus in acute mouse neocortico-hippocampal slices, while 14 drugs were bath-perfused at 5 different concentrations each. For each experimental condition, we collected seizure-like neuronal activity and merged their waveforms as one graphic image, which was further converted into a feature vector using Caffe, an open framework for deep learning. In the space of the first two principal components, the support vector machine completely separated the vectors (i.e., doses of individual drugs) that induced seizure-like events and identified diphenhydramine, enoxacin, strychnine and theophylline as "seizure-inducing" drugs, which indeed were reported to induce seizures in clinical situations. Thus, this artificial intelligence-based classification may provide a new platform to detect the seizure-inducing side effects of preclinical drugs.
[Mh] Termos MeSH primário: Convulsões/induzido quimicamente
Máquina de Vetores de Suporte
[Mh] Termos MeSH secundário: Animais
Região CA1 Hipocampal/efeitos dos fármacos
Difenidramina/efeitos adversos
Enoxacino/efeitos adversos
Técnicas In Vitro
Masculino
Camundongos
Camundongos Endogâmicos ICR
Estricnina/efeitos adversos
Teofilina/efeitos adversos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
325OGW249P (Enoxacin); 8GTS82S83M (Diphenhydramine); C137DTR5RG (Theophylline); H9Y79VD43J (Strychnine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170504
[Lr] Data última revisão:
170504
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170221
[St] Status:MEDLINE


  7 / 3037 MEDLINE  
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[PMID]:28190755
[Au] Autor:Kanamitsu K; Nozaki Y; Nagaya Y; Sugiyama Y; Kusuhara H
[Ad] Endereço:Laboratory of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-0033, Japan; Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., 463-10 Kagasuno, Kawauchi-cho, Tokushima-shi, Tokushima, 771-0192, Japan.
[Ti] Título:Quantitative prediction of histamine H1 receptor occupancy by the sedative and non-sedative antagonists in the human central nervous system based on systemic exposure and preclinical data.
[So] Source:Drug Metab Pharmacokinet;32(2):135-144, 2017 Apr.
[Is] ISSN:1880-0920
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Significant histamine H1 receptor occupation in the central nervous system (CNS) is associated with sedation. Here we examined the time profiles of the H1 receptor occupancy (RO) in the CNS using sedative (diphenhydramine and ketotifen) and non-sedative (bepotastine and olopatadine) antagonists at their therapeutic doses by integrating in vitro and animal data. A pharmacokinetic model was constructed to associate plasma concentrations and receptor binding in the brain. Dissociation and association rate constants with the H1 receptor and plasma and brain unbound fractions were determined in vitro. Passive and active clearances across the blood-brain barrier (BBB) were estimated based on physicochemical properties and microdialysis studies in mice and monkeys. The estimated RO values were comparable with the reported values determined at time to maximum concentration (T ) of plasma by positron-emission tomography in humans. The simulation suggested that the predicted maximum ROs by bepotastine and olopatadine were greater than the reported values. Sensitivity analysis showed that active transport across BBB had a significant impact on the RO duration of the H1 antagonists examined. The present study demonstrated that modeling and simulation permits a reasonable RO estimation in the human CNS. Our findings will facilitate the development of CNS-acting drugs.
[Mh] Termos MeSH primário: Sistema Nervoso Central/efeitos dos fármacos
Antagonistas dos Receptores Histamínicos H1/farmacologia
Receptores Histamínicos H1/metabolismo
[Mh] Termos MeSH secundário: Animais
Encéfalo/metabolismo
Sistema Nervoso Central/metabolismo
Difenidramina/sangue
Difenidramina/farmacologia
Antagonistas dos Receptores Histamínicos H1/sangue
Seres Humanos
Cetotifeno/sangue
Cetotifeno/farmacologia
Macaca fascicularis
Masculino
Camundongos
Camundongos Endogâmicos
Cloridrato de Olopatadina/sangue
Cloridrato de Olopatadina/farmacologia
Piperidinas/sangue
Piperidinas/farmacologia
Tomografia por Emissão de Pósitrons
Piridinas/sangue
Piridinas/farmacologia
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine H1 Antagonists); 0 (Piperidines); 0 (Pyridines); 0 (Receptors, Histamine H1); 2XG66W44KF (Olopatadine Hydrochloride); 8GTS82S83M (Diphenhydramine); HYD2U48IAS (bepotastine); X49220T18G (Ketotifen)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170505
[Lr] Data última revisão:
170505
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170214
[St] Status:MEDLINE


  8 / 3037 MEDLINE  
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[PMID]:28154308
[Au] Autor:Shiraishi S; Haraguchi T; Nakamura S; Kojima H; Kawasaki I; Yoshida M; Uchida T
[Ad] Endereço:School of Pharmaceutical Sciences, Mukogawa Women's University.
[Ti] Título:Suppression in Bitterness Intensity of Bitter Basic Drug by Chlorogenic Acid.
[So] Source:Chem Pharm Bull (Tokyo);65(2):151-156, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The purpose of the study was to evaluate suppression of the bitterness intensity of bitter basic drugs by chlorogenic acid (CGA) using the artificial taste sensor and human gustatory sensation testing and to investigate the mechanism underlying bitterness suppression using H-NMR. Diphenhydramine hydrocholoride (DPH) was the bitter basic drug used in the study. Quinic acid (QNA) and caffeic acid (CFA) together form CGA. Although all three acids suppressed the bitterness intensity of DPH in a dose-dependent manner as determined by the taste sensor and in gustatory sensation tests, CFA was less effective than either CGA or QNA. Data from H-NMR spectroscopic analysis of mixtures of the three acids with DPH suggest that the carboxyl group, which is present in both QNA and CGA but not CFA, interact with the amine group of DPH. This study showed that the bitterness intensity of DPH was suppressed by QNA and CGA through a direct electrostatic interaction with DPH as confirmed in H-NMR spectroscopic analysis. CGA and QNA may therefore be useful bitterness-masking agents for the basic drug DPH.
[Mh] Termos MeSH primário: Ácido Clorogênico/farmacologia
Percepção Gustatória/efeitos dos fármacos
Paladar/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Ácidos Cafeicos/farmacologia
Ácido Clorogênico/química
Difenidramina/química
Difenidramina/farmacologia
Relação Dose-Resposta a Droga
Interações Medicamentosas
Feminino
Seres Humanos
Espectroscopia de Prótons por Ressonância Magnética
Ácido Quínico/farmacologia
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Caffeic Acids); 058C04BGYI (Quinic Acid); 318ADP12RI (Chlorogenic Acid); 8GTS82S83M (Diphenhydramine); U2S3A33KVM (caffeic acid)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170314
[Lr] Data última revisão:
170314
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170204
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c16-00670


  9 / 3037 MEDLINE  
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[PMID]:28154306
[Au] Autor:Shiraishi S; Haraguchi T; Nakamura S; Li D; Kojima H; Yoshida M; Uchida T
[Ad] Endereço:Faculty of Pharmaceutical Science, Mukogawa Women's University.
[Ti] Título:Taste-Masking Effect of Chlorogenic Acid (CGA) on Bitter Drugs Evaluated by Taste Sensor and Surface Plasmon Resonance on the Basis of CGA-Drug Interactions.
[So] Source:Chem Pharm Bull (Tokyo);65(2):127-133, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RBM≈ETD. The association rate constant (k ) for the interaction between drugs and CGA as evaluated by SPR measurement also decreased in the following order DPH>DNP>AMD>DCF≈ETD≈RBM. It was suggested that basic drugs (AMD, DNP, DPH) associate more easily with CGA than acidic drugs (DCF, RBM, ETD). The inhibition ratios (%) of the taste sensor output of bitter drugs caused by CGA and the association rate constants (k ) between the drugs and CGA were significantly correlated (r =0.886, p<0.05, Spearman's correlation test). Our findings suggest that the taste-masking effects of CGA are due to its direct association with the drugs. CGA may therefore be a useful taste-masking agent for basic drugs.
[Mh] Termos MeSH primário: Ácido Clorogênico/farmacologia
Interações Medicamentosas
Ressonância de Plasmônio de Superfície
Paladar/efeitos dos fármacos
[Mh] Termos MeSH secundário: Alanina/análogos & derivados
Anlodipino/farmacologia
Diclofenaco/farmacologia
Difenidramina/farmacologia
Etodolac/farmacologia
Indanos/farmacologia
Piperidinas/farmacologia
Quinolonas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Indans); 0 (Piperidines); 0 (Quinolones); 144O8QL0L1 (Diclofenac); 1J444QC288 (Amlodipine); 2M36281008 (Etodolac); 318ADP12RI (Chlorogenic Acid); 8GTS82S83M (Diphenhydramine); 8SSC91326P (donepezil); LR583V32ZR (rebamipide); OF5P57N2ZX (Alanine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170314
[Lr] Data última revisão:
170314
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170204
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c16-00621


  10 / 3037 MEDLINE  
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[PMID]:28131782
[Au] Autor:Kim J; Song JH
[Ad] Endereço:Department of Pharmacology, College of Medicine, Chung-Ang University, 84 Heukseok-Ro, Dongjak-Gu, Seoul 06974, Republic of Korea.
[Ti] Título:Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells.
[So] Source:Eur J Pharmacol;798:122-128, 2017 Mar 05.
[Is] ISSN:1879-0712
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Microglial NADPH oxidase is a major source of toxic reactive oxygen species produced during chronic neuroinflammation. Voltage-gated proton channel (H 1) functions to maintain the intense activity of NADPH oxidase, and channel inhibition alleviates the pathology of neurodegenerative diseases such as ischemic stroke and multiple sclerosis associated with oxidative neuroinflammation. Antagonists of histamine H receptors have beneficial effects against microglia-mediated oxidative stress and neurotoxicity. We examined the effects of the H antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells recorded using the whole-cell patch clamp technique. Diphenhydramine and chlorpheniramine reduced the proton currents with almost the same potency, yielding IC values of 42 and 43µM, respectively. Histamine did not affect proton currents, excluding the involvement of histamine receptors in their action. Neither drug shifted the voltage-dependence of activation or the reversal potential of the proton currents, even though diphenhydramine slowed the activation and deactivation kinetics. The inhibitory effects of the two antihistamines on proton currents could be utilized to develop therapeutic agents for neurodegenerative diseases and other diseases associated with H 1 proton channel abnormalities.
[Mh] Termos MeSH primário: Clorfeniramina/farmacologia
Difenidramina/farmacologia
Antagonistas dos Receptores Histamínicos/farmacologia
Microglia/efeitos dos fármacos
Microglia/metabolismo
Prótons
[Mh] Termos MeSH secundário: Animais
Linhagem Celular
Canais Iônicos/antagonistas & inibidores
Canais Iônicos/metabolismo
Cinética
Camundongos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Histamine Antagonists); 0 (Hv1 proton channel, mouse); 0 (Ion Channels); 0 (Protons); 3U6IO1965U (Chlorpheniramine); 8GTS82S83M (Diphenhydramine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170515
[Lr] Data última revisão:
170515
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170130
[St] Status:MEDLINE



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