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1.
Brain Nerve ; 75(12): 1297-1300, 2023 Dec.
Artigo em Japonês | MEDLINE | ID: mdl-38097216

RESUMO

Veronal, introduced during the early 20th century was widely used as a sleeping pill at the time, and this drug is mentioned in Agatha Christie's novels. Research has proved that in addition to their sedative effects, Veronal and other sleeping pills with similar mechanisms of action are associated with undesirable effects that can lead to addiction and overdose. Barbiturate-induced deaths include the high-profile suicides of the famous American actress Marilyn Monroe and Ryunosuke Akutagawa, a prolific Japanese writer and poet. Soseki Natsume attempted an overdose of sleeping pills; however, he was surrounded by many disciples, and a disciple who observed the adverse effects of the drug prevented Natsume from overdosing. This example highlights that addiction depends on the social relationships surrounding an individual.


Assuntos
Medicamentos Indutores do Sono , Suicídio , Masculino , Humanos , Barbital
2.
Forensic Toxicol ; 41(1): 126-134, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36652071

RESUMO

PURPOSE: This study aims to develop and validate a rapid, simple, and efficient bioanalytical method for the simultaneous quantification of phenobarbital and barbital in human whole blood using liquid-liquid extraction combined with direct analysis in real time (DART) and high-resolution mass spectrometry (HRMS). METHOD: Phenobarbital-d5 and aprobarbital were selected as internal standards (ISs) of phenobarbital and barbital, respectively. A mixed solvent of o-xylene and ethyl acetate at a ratio of 1:6 was used to extract analytes of interest and ISs from 100 µL of human whole blood samples. Phenobarbital and barbital were detected by DART-HRMS. The proposed method has been validated in accordance with United States Food and Drug Administration Guidelines for Bioanalytical Method Validation in terms of selectivity, linearity, accuracy, precision, matrix effect, recovery, stability, and dilution integrity. RESULTS: The lower limits of quantification (LLOQs) of phenobarbital and barbital were both 10 ng/mL. The linearities were in the range of 10-1000 ng/mL (R2 ≥ 0.99). The mean recovery values of phenobarbital and barbital were 99.7% and 88.1%, respectively. The interday and intraday precision values were less than 10.4%, and the interday and intraday accuracy values ranged from 87.6 to 106.7%. Furthermore, the validated method was applied to four cases of phenobarbital poisoning at the Shanghai Institute of Forensic Science. CONCLUSION: The developed and fully validated method enabled the simultaneous quantification of phenobarbital and barbital in human whole blood and was successfully applied to authentic cases.


Assuntos
Barbital , Fenobarbital , Estados Unidos , Humanos , China , Espectrometria de Massas/métodos , Extração Líquido-Líquido
3.
J Am Chem Soc ; 144(34): 15595-15602, 2022 08 31.
Artigo em Inglês | MEDLINE | ID: mdl-35976640

RESUMO

The interest in the photochromism and functional applications of donor-acceptor Stenhouse adducts (DASAs) soared in recent years owing to their outstanding advantages and flexible design. However, their low solubility and irreversible conversion in aqueous solutions hampered exploring DASAs for biology and medicine. It is notably unknown whether the barbiturate electron acceptor group retains the pharmacological activity of drugs such as phenobarbital, which targets γ-aminobutyric acid (GABA)-type A receptors (GABAARs) in the brain. Here, we have developed the model compound DASA-barbital based on a scaffold of red-switching second-generation DASAs, and we demonstrate that it is active in GABAARs and alters the neuronal firing rate in a physiological medium at neutral pH. DASA-barbital can also be reversibly photoswitched in acidic aqueous solutions using cyclodextrin, an approved ingredient of drug formulations. These findings clarify the path toward the biological applications of DASAs and to exploit the versatility displayed in polymers and materials science.


Assuntos
Barbital , Água , Barbital/farmacologia , Neurônios , Polímeros , Ácido gama-Aminobutírico
4.
Molecules ; 26(14)2021 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-34299653

RESUMO

The formation of most multicomponent crystals relies on the interaction of hydrogen bonds between the components, so rational crystal design based on the expected hydrogen-bonded supramolecular synthons was employed to establish supramolecular compounds with desirable properties. This theory was put into practice for metformin to participate in more therapeutic fields to search for a fast and simple approach for the screening of candidate crystal co-formers. The prediction of intermolecular synthons facilitated the successful synthesis of a new multicomponent crystal of metformin (Met) and barbital (Bar) through an anion exchange reaction and cooling crystallization method. The single crystal X-ray diffraction analysis demonstrated the hydrogen bond-based ureide/ureide and guanidine/ureide synthons were responsible for the self-assembly of the primary structural motif and extended into infinite supramolecular heterocatemeric structures.


Assuntos
Barbital/química , Metformina/química , Modelos Moleculares , Cristalografia por Raios X , Ligação de Hidrogênio , Estrutura Molecular
5.
J Am Coll Nutr ; 38(5): 415-423, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-30696389

RESUMO

Objective: Tea (Camellia sinensis Linn.; family: Theaceae) is popular as a stimulant beverage across the globe and is also utilized as a functional antioxidant in alternative medicine. This study has evaluated the impact of seasonal variation on phyto-constituents of tea. Method: The antiproliferative potential of methanolic extracts of tea leaves collected in the rainy season (MECR) was compared with the extract of tea leaves collected in the autumn season (MECA) of the same mother plant. Evaluation of in vivo antitumor activity was carried out in adult female Swiss albino mice groups inoculated with Ehrlich ascites carcinoma (EAC) cells. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to compare efficacy of MECR with that of MECA in the EAC cell line. Both qualitative and quantitative tests for phytochemical constituents present in MECA and MECR were performed. Antitumor efficacy of both the extracts was determined by evaluating different tumor markers showing dose-dependent cytotoxicity. Results: Statistically significant reduction in EAC-induced tumor was observed in MECR treated mice compared to MECA treated ones. Cell decimation was significantly higher with MECR treatment, where restoration of different parameters including tissue structures returned to normal. Moreover, gas chromatography-mass spectrometry (GC-MS) study revealed the presence of cyclobarbital and benzazulene derivative in MECR, which is thought to be a novel source of these chemicals. Conclusions: To our knowledge, there is no report that has attempted to reveal nutritional changes in terms of efficacy and variation in anticancer constituents in tea leaves, plucked in two seasons. This study revealed a novel source of barbital and benzazulene derivative. The unique presence of cyclobarbital and benzazulene, as revealed from GC-MS data, in methanolic extract of tea leaves collected during the rainy season (MECR) may have contributed to its enhanced in vitro (adopting MTT assay) and in vivo (on EAC-infected Swiss albino mice) cytotoxicity vis-à-vis antiproliferative properties compared to methanolic extract of tea leaves collected during the autumn season (MECA). The nature of plucking leaves in the two selected seasons is different.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Metanol/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Chá/química , Animais , Antineoplásicos Fitogênicos/química , Barbital/farmacologia , Camellia sinensis , Carcinoma de Ehrlich , Linhagem Celular Tumoral , Feminino , Metanol/química , Camundongos , Extratos Vegetais/química , Estações do Ano
6.
J Phys Chem A ; 122(11): 3031-3044, 2018 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-29481082

RESUMO

Experimental charge density distribution studies, complemented by quantum mechanical theoretical calculations, of a host-guest system composed of a macrocycle (1) and barbital (2) in a 1:1 ratio (3) have been carried out via high-resolution single-crystal X-ray diffraction. The data were modeled using the conventional multipole model of electron density according to the Hansen-Coppens formalism. The asymmetric unit of macrocycle 1 contained an intraannular ethanol molecule and an extraannular acetonitrile molecule, and the asymmetric unit of 3 also contained an intraannular ethanol molecule. Visual comparison of the conformations of the macrocyclic ring shows the rotation by 180° of an amide bond attributed to competitive hydrogen bonding. It was found that the intraannular and extraannular molecules inside were orientated to maximize the number of hydrogen bonds present, with the presence of barbital in 3 resulting in the greatest stabilization. Hydrogen bonds ranging in strength from 4 to 70 kJ mol-1 were the main stabilizing force. Further analysis of the electrostatic potential among 1, 2, and 3 showed significant charge redistribution when cocrystallization occurred, which was further confirmed by a comparison of atomic charges. The findings presented herein introduce the possibility of high-resolution X-ray crystallography playing a more prominent role in the drug design process.


Assuntos
Barbital/química , Compostos Macrocíclicos/química , Teoria Quântica , Sítios de Ligação , Ligação de Hidrogênio , Modelos Moleculares , Estrutura Molecular
7.
Int J Pharm ; 493(1-2): 434-8, 2015 Sep 30.
Artigo em Inglês | MEDLINE | ID: mdl-26253375

RESUMO

The effect of salt formulation on the electrostatic property of active pharmaceutical ingredients was investigated. The electrostatic property of weak acids (carboxylic acids and amide-enole type acid) and their sodium salts was evaluated by a suction-type Faraday cage meter. Free carboxylic acids showed negative chargeability, whereas their sodium salts showed more positive chargeability than the free acids. However, no such trend was observed for amide-enole type acids.


Assuntos
Ácidos Carboxílicos/química , Barbital/química , Química Farmacêutica , Dantroleno/química , Omeprazol/química , Sais/química , Eletricidade Estática
8.
Chem Asian J ; 9(10): 2831-41, 2014 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25080369

RESUMO

In our previous paper, we reported that a dimeric Zn(2+) complex with a 2,2'-bipyridyl linker (Zn2L(1)), cyanuric acid (CA), and a Cu(2+) ion automatically assemble in aqueous solution to form 4:4:4 complex 3, which selectively catalyzes the hydrolysis of mono(4-nitrophenyl)phosphate (MNP) at neutral pH. Herein, we report that the use of barbital (Bar) instead of CA for the self-assembly with Zn2L(1) and Cu(2+) induces 2:2:2 complexation of these components, and not the 4:4:4 complex, to form supramolecular complex 6 a, the structure and equilibrium characteristics of which were studied by analytical and physical measurements. The finding show that 6 a also accelerates the hydrolysis of MNP, similarly to 3. Moreover, inspired by the crystal structure of 6 a, we prepared barbital units that contain functional groups on their side chains in an attempt to produce supramolecular phosphatases that possess functional groups near the Cu2(µ-OH)2 catalytic core so as to mimic the catalytic center of alkaline phosphatase (AP).


Assuntos
Barbital/química , Cobre/química , Compostos Heterocíclicos/química , Zinco/química , Cristalografia por Raios X , Ciclamos , Espectrofotometria Ultravioleta , Água/química
9.
Mol Pharm ; 11(1): 338-50, 2014 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-24283960

RESUMO

Barbital is a hypnotic agent that has been intensely studied for many decades. The aim of this work was to establish a clear and comprehensible picture of its polymorphic system. Four of the six known solid forms of barbital (denoted I(0), III, IV, and V) were characterized by various analytical techniques, and the thermodynamic relationships between the polymorph phases were established. The obtained data permitted the construction of the first semischematic energy/temperature diagram for the barbital system. The modifications I(0), III, and V are enantiotropically related to one another. Polymorph IV is enantiotropically related to V and monotropically related to the other two forms. The transition points for the pairs I(0)/III, I(0)/V, and III/IV lie below 20 °C, and the transition point for IV/V is above 20 °C. At room temperature, the order of thermodynamic stability is I(0) > III > V > IV. The metastable modification III is present in commercial samples and has a high kinetic stability. The solid-state NMR spectra provide information on aspects of crystallography (viz., the asymmetric units and the nature of hydrogen bonding). The known correlation between specific N-H···O═C hydrogen bonding motifs of barbiturates and certain IR characteristics was used to predict the H-bonded pattern of polymorph IV.


Assuntos
Barbital/química , Cristalização , Varredura Diferencial de Calorimetria , Cristalografia por Raios X , Ligação de Hidrogênio , Espectroscopia de Ressonância Magnética , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Análise Espectral Raman , Termodinâmica , Difração de Raios X
11.
Artigo em Inglês | MEDLINE | ID: mdl-23220533

RESUMO

Copper guanine and barbital complexes were prepared and characterized by elemental analyses and spectral measurements. The data typified the formation of stoichiometries 1:1 (M:L) with possible Cu-Cu interaction "association". The complexes are with different geometries: square planar, square pyramidal and tetrahedral. The mode of bonding was identified by IR spectra. EPR spectra of the powdered complexes were recorded at X band at the room temperature. Different ESR parameters were calculated and discussed: g(//), g(⊥), A(//), [g], G, F, K, α(2). Molecular modeling techniques and quantum chemical methods have been performed for copper complexes to correlate the chemical structures of the complexes with their physical molecular properties. Bond lengths, bond orders, bond angles, dihedral angles, close contact, dipole moment (µ), sum of the total negative charge (STNC), electronegativity (χ), chemical potential (Pi), global hardness (η), softness (σ), the highest occupied molecular orbital energy (E(HOMO)), the lowest unoccupied molecular orbital energy (E(LUMO)) and the energy gap (ΔE) were calculated using PM3 semi-empirical and Molecular Mechanics (MM+) methods. The study displays a good correlation between the theoretical and experimental data which confirms the reliability of the quantum chemical methods.


Assuntos
Barbital/química , Complexos de Coordenação/química , Cobre/química , Guanina/química , Espectroscopia de Ressonância de Spin Eletrônica , Modelos Moleculares , Teoria Quântica , Espectrofotometria Infravermelho
12.
Se Pu ; 29(11): 1082-6, 2011 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-22393695

RESUMO

A simple, precise and sensitive gas chromatography-mass spectrometry (GC-MS) method coupled with pulse splitless injection technique was developed for the determination of 10 sedative-hypnotics (barbital, amobarbital, phenobarbital, oxazepam, diazepam, nitrazepam, clonazepam, estazolam, alprazolam, triazolam) in human plasma. The drugs spiked in plasma were extracted with ethyl acetate after alkalization with 0.1 mol/L NaOH solution. The organic solvent was evaporated under nitrogen stream, and the residues were redissolved by ethyl acetate. The separation was performed on an HP-5MS column (30 m x 250 microm x 0.25 microm). The analytes were determined and identified using selected ion monitoring (SIM) mode and scan mode, respectively. The internal standard method was used for the determination. The target analytes were well separated from each other on their SIM chromatograms and also on the total ion current (TIC) chromatograms. The blank extract from human plasma gave no peaks that interfered with all the analytes on the chromatogram. The calibration curves for 10 sedative-hypnotics showed excellent linearity. The correlation coefficients of all the drugs were higher than 0.9954. The recoveries of the drugs spiked in human plasma ranged from 92.28% to 111.7%, and the relative standard deviations (RSDs) of intra-day and inter-day determinations were from 4.09% to 14.26%. The detection limits ranged from 2 to 20 microg/L. The method is simple, reliable, rapid and sensitive for the determination and the quantification of 10 sedative-hypnotics in human plasma and seems to be useful in the practice of clinical toxicological cases.


Assuntos
Cromatografia Gasosa-Espectrometria de Massas/métodos , Hipnóticos e Sedativos/sangue , Barbital/sangue , Estazolam/sangue , Humanos , Oxazepam/sangue
13.
Anal Chim Acta ; 679(1-2): 1-6, 2010 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-20951851

RESUMO

A rapid method for sensitive ultraviolet detection of multiple psychotropic drugs in human plasma was developed on a low-cost and expediently fabricated hybrid microfluidic device. The device was composed of one fused-silica capillary with a sampling fracture, a poly(methyl methacrylate) board with four reservoirs, and a printed circuit board. At the optimal separation and detection conditions, the baseline separation of three kinds of psychotropic drugs including barbiturates (phenobarbital and barbital), benzodiazepines (nitrazepam, clonazepam, chlordiazepoxide, alprazolam and diazepam) and tricyclic antidepressant drugs (amitriptyline) was achieved within 200 s with separation efficiency up to 3.80 × 10(5) plates m(-1). The linear ranges for ultraviolet detection were from 2.0 to 1000.0 µg mL(-1) for chlordiazepoxide and 1.0 to 1000.0 µg mL(-1) for other seven drugs. Combining with solid-phase extraction, this novel protocol could successfully be used to screen naturally existing psychotropic drugs in a known human plasma sample. The minimum detectable concentration was down to 27 ng mL(-1) for phenobarbital spiked in plasma. This work provided a promising way to initially screen different psychotropic drugs with high resolution, rapid separation and low-cost.


Assuntos
Eletroforese em Microchip/instrumentação , Eletroforese em Microchip/métodos , Técnicas Analíticas Microfluídicas/instrumentação , Psicotrópicos/sangue , Amitriptilina/sangue , Barbital/sangue , Benzodiazepinas/sangue , Equipamentos Descartáveis , Desenho de Equipamento , Feminino , Humanos , Limite de Detecção , Masculino , Fenobarbital/sangue , Fotometria , Reprodutibilidade dos Testes , Extração em Fase Sólida
14.
J Phys Chem A ; 114(34): 9237-45, 2010 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-20681553

RESUMO

A computational study of the structural and thermochemical properties of N-phenyl (open) and N-alkyl (cyclic) ureas, through the use of M05-2X and B3LYP density functional theory calculations has been carried out. The consistency of the literature experimental results has been confirmed, and using mainly isodesmic reactions, the unknown Delta(f)H(0)(g) of the other urea derivatives were estimated. The experimental results together with the theoretical information have permitted the study of the effect of phenyl, p- and m-chlorophenyl, alkyl, and carbonyl substitutions on the thermodynamical stability of urea and its cyclic derivatives. The peculiar behavior of the N-tert-butyl substituent in cyclic ureas has been related to geometric deformations.


Assuntos
Barbital/química , Carbanilidas/química , Hidantoínas/química , Imidazolidinas/química , Compostos de Metilureia/química , Teoria Quântica , Temperatura , Ureia/química , Modelos Moleculares , Conformação Molecular , Compostos de Fenilureia/química , Termodinâmica
15.
Se Pu ; 28(1): 23-33, 2010 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-20458916

RESUMO

A rapid method for the simultaneous determination of 42 psychoactive drugs and their metabolites (barbitals, benzodiazepines, tricyclic antidepressants, phenothiazines, etc. ) in human plasma and urine was developed using ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). After a simple protein precipitation step, the analysis of the drugs and the metabolites was achieved on an Acquity UPLC BEH C18 column by using the gradient elution with ammonium acetate and methanol-acetonitrile (1: 1, v/v) as the mobile phases, and detected by electrospray ionization-tandem mass spectrometry in the multiple reaction monitoring (MRM) mode operated simultaneously in both positive and negative modes by rapid switching, and quantified by matrix-match standard solution. The average recoveries were 60.2% - 125% and 64.5% - 126% for the drugs in plasma and urine except those of perphenazine, thioridazine and chloropromazine in plasma were 37.6% - 57.5%, 36.3% - 48.3%, 52.4% -67.4%, respectively; trazodone and diazepam in urine were 100% -142% and 108% - 177%, respectively. The relative standard deviations (RSDs) of all the drugs in plasma and urine were within 0.8% - 26% and 2.6%18% (n = 6), respectively. The detection limits of the 4 barbitals ranged from 20 to 100 mg/L and those of the other drugs ranged from 0.05 to 2.0 mg/L. The method is simple, selective and sensitive to detect drugs for both clinical and forensic purposes.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Psicotrópicos/sangue , Psicotrópicos/urina , Espectrometria de Massas em Tandem/métodos , Antidepressivos Tricíclicos/sangue , Antidepressivos Tricíclicos/urina , Barbital/sangue , Barbital/urina , Benzodiazepinas/sangue , Benzodiazepinas/urina , Análise Química do Sangue/métodos , Humanos , Psicotrópicos/metabolismo
16.
J Chromatogr A ; 1217(17): 2821-31, 2010 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-20227703

RESUMO

This work describes a liquid chromatography-tandem mass spectrometry (LC-MS/MS) procedure for multiplex screening, ultratrace quantification and reliable confirmation of barbital series residues in animal-derived food matrices. The method is developed based on a distinct dependency of the electrospray ionization (ESI) response of nine structural homologues on LC eluent properties and gas-phase ion chemistry during the ESI process. The "wrong-way-round" negative ionization aspect has been explored to optimize the compatibility of the hyphenated LC-MS/MS technique, which facilitates detection limits at 30-100-fold lower than 0.01 ppm without derivatization or post-column basification step. A mobile phase using methanol modified with 0.01% acetic acid is adopted to achieve an approximately 2-9-fold increase in signal-to-noise ratio over the results under suboptimal conditions. There is no significant differential matrix effects or deuterium isotope effects on chromatographic retention and ESI responsiveness at all levels across the different analyte-matrix pairs. Mean recoveries ranged from 79.6% (barbital) to 108% (secobarbital) at fortified levels of 0.5-20 ng/g within relative standard deviations less than 11%. Between-run repeatability and within-laboratory reproducibility were 3-11% and 5-13%, respectively. An ion ratio criterion for valid detection limit data for simultaneous screening of homologous multiresidues in complex sample matrices is proposed. The satisfactory applicability of the newly described procedure to 43 real samples including pork, poultry meat, swine liver, fish tissue and shrimp muscle demonstrated the LC-MS/MS technique with facile sample handling can serve as an attractive alternative analytical method accepted for regulatory purpose.


Assuntos
Barbital/análise , Cromatografia Líquida/métodos , Resíduos de Drogas/análise , Carne/análise , Espectrometria de Massas em Tandem/métodos , Animais , Peixes , Hipnóticos e Sedativos/análise , Limite de Detecção , Aves Domésticas , Suínos
17.
Toxins (Basel) ; 2(4): 552-71, 2010 04.
Artigo em Inglês | MEDLINE | ID: mdl-22069599

RESUMO

The potent experimental renal carcinogenesis of ochratoxin A (OTA) in male rats makes the dietary contaminant a potential factor in human oncology. We explored whether the tumour promoter sodium barbitate could shorten the otherwise long latency between exposure to toxin and tumourigenesis. Young rats, of a hybrid in which mononuclear leukaemia was rare, were given feed contaminated (5 ppm) with OTA for 36 weeks to initiate renal tumourigenesis. Some individuals were thereafter given sodium barbitate (500 ppm in drinking water) for life. Pathological outcomes were studied at or near the end of natural life. Renal tumours in males given barbitate became evident after latency of one year, but only slightly before those without barbitate. In contrast, female mammary tumourigenesis was advanced by at least 6 months synchronously in all rats given the OTA-barbitate regimen compared to tumourigenesis in controls. Diagnosis of malignant mammary angiosarcoma in a female given the OTA-barbitate regimen is a new finding in the rat. The long latency of OTA-induced renal tumourigenesis was not notably susceptible to accelerated promotion by barbitate, contrasting with an apparently marked effect of barbitate on development of mammary tumours.


Assuntos
Barbital/toxicidade , Neoplasias Renais/induzido quimicamente , Neoplasias Mamárias Experimentais/induzido quimicamente , Micotoxinas/toxicidade , Ocratoxinas/toxicidade , Animais , Feminino , Masculino , Ocratoxinas/sangue , Projetos Piloto , Ratos , Ratos Endogâmicos F344 , Ratos Sprague-Dawley
18.
Hybridoma (Larchmt) ; 28(2): 145-8, 2009 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-19382846

RESUMO

In this study, we prepared monoclonal antibodies against morphine, methadone, babital, methamphetamine, and phencyclidine, then developed a dot-ELISA method by such antibodies to test their efficacy in clinical application and the screening of urine samples. It was found that there were 36 narcotics-positive drug users, including 28 morphine positive, six methamphetamine positive, and two positive for both. All the results were confirmed by commercial drug testing kits.


Assuntos
Anticorpos Monoclonais/biossíntese , Barbital/imunologia , Ensaio de Imunoadsorção Enzimática/métodos , Metadona/imunologia , Metanfetamina/imunologia , Morfina/imunologia , Fenciclidina/imunologia , Detecção do Abuso de Substâncias/métodos , Anticorpos Monoclonais/urina , Humanos
19.
Cell Mol Biol (Noisy-le-grand) ; 55(1): 23-8, 2009 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-19267998

RESUMO

The N-methyl-diethyl-aspartate (NMDA) receptor has been reported to play an important role in several acute and chronic neuropathologic syndromes. 5-aminolevulinic acid (ALA) accumulates in acute porphyrias due to a deficiency in the heme biosynthetic pathway. Considering that glutamate uptake inhibition caused by ALA could be one of the reasons conducing to porphyric neuropathy, it was of interest to evaluate the effect of porphyrinogenic agents on NMDA glutamatergic system. To this end receptor levels and apparent affinity (Kd) were analyzed in mice brain cortex and cerebellum. NMDA levels were diminished after chronic Isoflurane anaesthesia in brain cortex. In cerebellum, a diminution was observed after acute Enflurane and Isoflurane and allylisopropylacetamide, while ethanol administration showed a significant increase. ALA administration diminished NMDA levels only in cerebellum. Affinity constant was only reduced in brain cortex after chronic Isoflurane treatment. In conclusion, glutamatergic system appears to be involved in the action of some of the porphyrinogenic drugs studied mainly in cerebellum. Receptors regulation should therefore be considered an important mechanism in the cellular response to specific drugs, with the aim of designing new therapies and elucidating the mechanisms leading to porphyric neuropathy and acute attack triggering.


Assuntos
Porfirinogênios/farmacologia , Ácido Aminolevulínico/farmacologia , Animais , Barbital/farmacologia , Cerebelo/efeitos dos fármacos , Cerebelo/metabolismo , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/metabolismo , Enflurano/farmacologia , Etanol/farmacologia , Griseofulvina/farmacologia , Isoflurano/farmacologia , Masculino , Camundongos , Receptores de N-Metil-D-Aspartato/metabolismo
20.
Immunopharmacol Immunotoxicol ; 30(3): 489-501, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-18668394

RESUMO

Larrea divaricata is a plant widely used in folk medicine in Argentina. This work aimed to study the mechanisms of decoction activity on the release of oxygen reactive species. Decoction increased the binding of zymosan-FITC and superoxide production. Cadmium decreased the superoxide production as well as malonate and barbital. Decoction decreased the release of hydrogen peroxide. Decoction increased the reduction of MTT but not when malonate and barbital were included. Together, decoction increased the expression of dectin-1 leading to increased superoxide production. It is possible that decoction increases the activity of peroxidase, and decreases the Cu, Zn-superoxide dismutase.


Assuntos
Peróxido de Hidrogênio/metabolismo , Larrea , Macrófagos Peritoneais/efeitos dos fármacos , Extratos Vegetais/farmacologia , Receptores de Complemento/efeitos dos fármacos , Superóxidos/metabolismo , Animais , Barbital/farmacologia , Cloreto de Cádmio/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Feminino , Larrea/química , Lectinas Tipo C , Macrófagos Peritoneais/metabolismo , Masculino , Malonatos/farmacologia , Proteínas de Membrana/metabolismo , Camundongos , Proteínas do Tecido Nervoso/metabolismo , Componentes Aéreos da Planta , Receptores de Complemento/metabolismo , Zimosan/metabolismo
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