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Article ; Online: Uso de antagonistas de receptores N-metil-D-aspartato en la analgesia postoperatoria de la cirugía proctológica

Carlos Gilberto Nieto Monteagudo / Osmany Cruz García / Greter Nieto Martínez / Lester Álvarez Hurtado / Yassel Cruz Hernández / Marlon Cruz Hernández

Acta Médica del Centro, Vol 16, Iss 3, Pp 465-

2022 Volume 478

Abstract: Introducción: la utilización de antagonistas de receptores N-metil-D-aspartato ha mejorado ... de los antagonistas de receptores N-metil-D-aspartato en la analgesia postoperatoria de la cirugía proctológica ...

Abstract	Introducción: la utilización de antagonistas de receptores N-metil-D-aspartato ha mejorado la analgesia postoperatoria y disminuido los requerimientos de otros analgésicos. Objetivo: evaluar la utilidad de los antagonistas de receptores N-metil-D-aspartato en la analgesia postoperatoria de la cirugía proctológica. Métodos: se realizó un estudio cuasi experimental en 100 pacientes sometidos a cirugía proctológica, los que se dividieron en dos grupos. El grupo K recibió analgesia postoperatoria con ketamina en bolo y en infusión y el grupo KS recibió ketamina y sulfato de magnesio en bolo y en infusión en las primeras 12 horas postquirúrgicas. Se evaluaron en el postoperatorio el comportamiento de la tensión arterial media, la frecuencia cardíaca, la saturación pulsátil de oxígeno, el nivel de sedación, la puntuación en la escala analógica visual para el dolor, los bolos suplementarios de analgesia de rescate y los efectos adversos. Resultados: el comportamiento de la tensión arterial media fue más favorable en el grupo KS. El comportamiento de la frecuencia cardíaca, la saturación pulsátil de oxígeno, el nivel de sedación, la evaluación del dolor por la escala analógica visual, la analgesia de rescate y los efectos adversos fueron similares, estadísticamente, en ambos grupos, aunque con mejores resultados en el grupo KS. Conclusiones: la ketamina y el sulfato de magnesio fueron útiles en la analgesia postoperatoria de la cirugía proctológica y la asociación ketamina-sulfato de magnesio aportó mejores resultados.
Keywords	receptores n-metil-d-aspartato ; ketamina ; sulfato de magnesio ; analgesia postoperatoria ; cirugía proctológica ; Medicine ; R
Language	Spanish
Publishing date	2022-05-01T00:00:00Z
Publisher	Editorial Ciencias Médicas
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: N-Acetyl-D-Glucosamine-Loaded Chitosan Filaments Biodegradable and Biocompatible for Use as Absorbable Surgical Suture Materials.

da Silva, Milena Costa / da Silva, Henrique Nunes / Alves Leal Cruz, Rita de Cássia / Sagoe Amoah, Solomon Kweku / de Lima Silva, Suédina Maria / Lia Fook, Marcus Vinícius

Materials (Basel, Switzerland)

2019 Volume 12, Issue 11

Abstract: The aim of this study was to prepare chitosan (CS) filaments incorporated with N-acetyl-D ... indicated in the U.S. Pharmacopeia (1.7 N) for suture number 6-0 (filament diameter of 100-149 μm ...

Abstract	The aim of this study was to prepare chitosan (CS) filaments incorporated with N-acetyl-D-Glucosamine (GlcNAc), using the wet spinning method, in order to combine the GlcNAc pharmacological properties with the CS biological properties for use as absorbable suture materials. The filaments were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), uniaxial tensile testing, in vitro biodegradation, and through in vitro drug release and cytotoxicity studies. It was observed that the addition of GlcNAc did not alter the morphology of the filaments. The CS and CS/GlcNAc filaments presented diameters 145 µm and 148 µm, respectively, and the surfaces were homogeneous. Although the mechanical resistance of the chitosan filaments decreased with the incorporation of the GlcNAc drug, this property was greater than the mean values indicated in the U.S. Pharmacopeia (1.7 N) for suture number 6-0 (filament diameter of 100-149 μm). The biodegradation of the CS filaments was accelerated by the addition of GlcNAc. After 35 days, the CS/GlcNAc filaments degradability was at its total, and for the CS filaments it was acquired in 49 days. The in vitro kinetic of the release process was of the zero-order and Hopfenberg models, controlled by both diffusion and erosion process. The in vitro cytotoxicity data of the CS and CS/GlcNAc filaments toward L929 cells showed that these filaments are nontoxic to these cells. Thus, the GlcNAc-loaded CS filaments might be promising as absorbable suture materials. In addition, this medical device may be able to enhance healing processes, relieve pain, and minimize infection at the surgery site due the prolonged release of GlcNAc.
Language	English
Publishing date	2019-06-04
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2487261-1
ISSN	1996-1944
ISSN	1996-1944
DOI	10.3390/ma12111807
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Article ; Online: Encefalitis autoinmune mediada por anticuerpos contra el receptor N-metil-D-aspartato

Henry Palomino-Lescano / Darwin Segura-Chávez / Darko Quispe-Orozco / Sheila Castro-Suarez / Walter De la Cruz / Willy Zapata-Luyo / José Delgado-Ríos / Juan Cam / Marcela Alvarado-Morales / Lippmann Paredes-Carcasi / Iván Cornejo-Herrera / María Meza-Vega

Revista Peruana de Medicina Experimental y Salud Pública, Vol 36, Iss 1, Pp 138-

reporte de cuatro casos en Perú

2019 Volume 44

Abstract: La encefalitis autoinmune por anticuerpos contra el receptor N-metil-D-aspartato (anti-NMDAR ...

Abstract	La encefalitis autoinmune por anticuerpos contra el receptor N-metil-D-aspartato (anti-NMDAR) es un desorden mediado por anticuerpos contra antígenos de superficie neuronal, cuyo diagnóstico temprano y tratamiento oportuno mejoran el pronóstico de la enfermedad. Se presentan cuatro casos con el diagnóstico definitivo de encefalitis autoinmune por anti-NMDAR, tratados en el Instituto Nacional de Ciencias Neurológicas en Lima-Perú. Todos los pacientes presentaron crisis epilépticas y tres casos desarrollaron un estado epiléptico refractario. Asimismo, tres pacientes presentaron alteraciones neuropsiquiátricas, discinesias y disautonomías. Dos casos requirieron soporte ventilatorio. Todos presentaron un electroencefalograma anormal, dos casos tuvieron pleocitosis en líquido cefalorraquídeo, y sólo uno mostró anormalidades cerebrales en la resonancia magnética. Respecto al tratamiento, todos los pacientes recibieron inmunoterapia con metilprednisolona y sólo dos de ellos requirieron plasmaféresis por respuesta ineficaz al tratamiento con corticoides. A los 12 meses del alta hospitalaria, tres pacientes quedaron libre de crisis epilépticas y sólo un caso no logró la independencia funcional. Estos casos muestran que la encefalitis anti-NMDAR es una condición tratable y su reconocimiento temprano junto con un tratamiento adecuado (inmunoterapia/plasmaféresis) son esenciales para una evolución favorable.
Keywords	informes de casos ; encefalitis antirreceptor n-metil-d-aspartato ; perú ; Medicine ; R ; Medicine (General) ; R5-920
Language	Spanish
Publishing date	2019-03-01T00:00:00Z
Publisher	Instituto Nacional de Salud
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: D-optimal designs and N-way techniques to determine sulfathiazole in milk by molecular fluorescence spectroscopy.

Morales, Rocío / Ortiz, M Cruz / Sarabia, Luis A / Sánchez, M Sagrario

Analytica chimica acta

2011 Volume 707, Issue 1-2, Page(s) 38–46

Abstract: ... To do this, two chemometric tools are used together: a D-optimal design for studying the effect ... with UHT milk, 4:6 rate for TCA:milk volumes and 40 μL of fluorescamine. In UHT milk, the mean recovery (n=5 ...

Abstract	The present work proposes an analytical procedure to determine sulfathiazole in milk by using molecular fluorescence spectroscopy. For this sulfonamide the European Union in Regulation 37/2010 has established a maximum residue limit in milk of 100 μg kg(-1). The study includes the effect of six factors on the recovery of sulfathiazole. The factors are: (i) The one related to the matrix depending on the heat treatment of the milk (UHT, pasteurized); (ii) Those related to the protein precipitation step, namely the ratio between the volume of trichloroacetic acid (TCA) and milk, centrifugation speed and temperature; (iii) Those affecting the derivatization reaction: derivatization time and volume of fluorescamine. To do this, two chemometric tools are used together: a D-optimal design for studying the effect of the factors on the recovery of sulfathiazole, considerably reducing the number of needed experiments; and the second-order property of the PARAFAC (Parallel Factor Analysis) decomposition that avoids the need of fitting a new calibration model each time that the experimental conditions change. It has been found that the type of milk, the TCA:milk ratio and the volume of fluorescamine have significant effect on the response. The rest of factors and interactions are not significant. The best recovery is obtained with UHT milk, 4:6 rate for TCA:milk volumes and 40 μL of fluorescamine. In UHT milk, the mean recovery (n=5) in the optimal conditions is 88.7% (RSD=12.4%). As some non-linear behaviour may occur when using fluorescence spectroscopy, the calibration model that relates the fluorescence spectra with the concentration is computed by a partial least squares regression and a multi-layer feed-forward neural network. In both cases, the proposed procedures have been validated according to Decision 2002/657/EC, concluding that the two are accurate although the calibration model built with the neural network has better figures of merit, the decision limit (CCα) for x(0)=100 μg L(-1) is 103.3 μg L(-1) and the detection capability (CCβ) is 106.5 μg L(-1), with the probabilities of false noncompliance (α) and false compliance (β) equal to 5%.
MeSH term(s)	Animals ; Chemistry Techniques, Analytical/methods ; Drug Residues/analysis ; Food Contamination/analysis ; Milk/chemistry ; Neural Networks (Computer) ; Spectrometry, Fluorescence/methods ; Sulfathiazoles/analysis
Chemical Substances	Sulfathiazoles ; sulfathiazole (Y7FKS2XWQH)
Language	English
Publishing date	2011-11-30
Publishing country	Netherlands
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1483436-4
ISSN	1873-4324 ; 0003-2670
ISSN (online)	1873-4324
ISSN	0003-2670
DOI	10.1016/j.aca.2011.09.014
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Article: Intensified Microwave-Assisted N-Acylation Procedure – Synthesis and Activity Evaluation of TRPC3 Channel Agonists with a 1,3-Dihydro-2H-benzo[d]imidazol-2-one Core

Guedes de la Cruz, Gema / Svobodova, Barbora / Lichtenegger, Michaela / Tiapko, Oleksandra / Groschner, Klaus / Glasnov, Toma

Synlett

2016 Volume 28, Issue 06, Page(s) 695–700

Abstract: ... amidation procedure for the synthesis of 1,3-dihydro-2 H -benzo[ d ]imidazol-2-one-based agonists of TRPC3/6 ...

Abstract	Upon controlled microwave heating and using cyanuric chloride as a coupling reagent, an efficient amidation procedure for the synthesis of 1,3-dihydro-2 H -benzo[ d ]imidazol-2-one-based agonists of TRPC3/6 ion channels has been developed. Compared to the few conventional protocols, a drastic reduction in processing time from ca. 2 days down to 10 minutes was achieved accompanied by significantly improved product yields. The robustness of the method was confirmed by 18 additional examples including aromatic, aliphatic, and heterocyclic amines and acids. The obtained agonists were screened for biological activity at 1 μM concentration and few structure–activity relations have been established.
Keywords	microwave synthesis ; acylation ; amides ; Ca ; -signaling ; TRPC ion channels ; agonist
Language	English
Publishing date	2016-12-08
Publisher	© Georg Thieme Verlag
Publishing place	Stuttgart ; New York
Document type	Article
ZDB-ID	2042012-2
ISSN	1437-2096 ; 0936-5214
ISSN (online)	1437-2096
ISSN	0936-5214
DOI	10.1055/s-0036-1589472
Database	Thieme publisher's database

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Article ; Online: O-GlcNAc-selective-N-acetyl-beta-D-glucosaminidase activity and mRNA expression in muscle is related to glucosamine-induced insulin resistance.

Durán-Reyes, Genoveva / Pascoe-Lira, Dalila / García-Macedo, Rebeca / Medina-Navarro, Rafael / Rosales-Torres, Ana María / Vergara-Onofre, Marcela / Foyo-Niembro, Enrique / Gutiérrez-Rodríguez, Margarita Eugenia / García-Gutiérrez, María Trinidad Adriana / Valladares-Salgado, Adán / Kumate, Jesús / Cruz, Miguel

Pharmacology

2010 Volume 85, Issue 2, Page(s) 121–130

Abstract: ... acetylglucosaminylated modified proteins (O-GlcNAcylated proteins). The role played by O-GlcNAc-selective-N-acetyl-beta-D ... Glucosamine (GlcN)-induced insulin resistance is associated with an increase in O-linked-N ... glucosaminidase (O-GlcNAcase), which removes O-N-acetyl-glucosamine residues from O-GlcNAcylated proteins, has not ...

Abstract	Glucosamine (GlcN)-induced insulin resistance is associated with an increase in O-linked-N-acetylglucosaminylated modified proteins (O-GlcNAcylated proteins). The role played by O-GlcNAc-selective-N-acetyl-beta-D-glucosaminidase (O-GlcNAcase), which removes O-N-acetyl-glucosamine residues from O-GlcNAcylated proteins, has not yet been demonstrated. We investigated whether GlcN-induced whole-body insulin resistance is related to tissue O-GlcNAcase activity and mRNA expression. GlcN (30 mumol/kg/min) or physiological saline (control) was intravenously infused into Sprague-Dawley rats for 2 h. After GlcN treatment, rats were subjected to the following: intravenous glucose tolerance test, insulin tolerance test or removal of the liver, muscle and pancreas. GlcN was found to provoke hyperglycemia compared to control (8.6 +/- 0.41 vs. 4.82 +/- 0.17 mM, p < 0.001). The insulin resistance index (HOMA-IR) increased (15.76 +/- 1.47 vs. 10.14 +/- 1.41, p < 0.001) and the beta-cell function index (HOMA-beta) diminished (182.69 +/- 22.37 vs. 592.01 +/- 103, p < 0.001). Liver glucose concentration was higher in the GlcN group than in the control group (0.37 +/- 0.04 vs. 0.24 +/- 0.038 mmol/g dry weight, p < 0.001). Insulin release index (insulin/glucose) was less in the GlcN group than in the control (2.2 +/- 0.1 vs. 8 +/- 0.8 at 120 min, p < 0.001). In the GlcN group, muscle O-GlcNAcase activity diminished (0.28 +/- 0.019 vs. 0.36 +/- 0.018 nmol of p-nitrophenyl/mg protein/min, p < 0.001), and K(m) increased (1.51 +/- 0.11 vs. 1.12 +/- 0.1 mM, p < 0.001) compared to the control. In the GlcN group, O-GlcNAcase activity/mRNA expression was altered (0.6 +/- 0.07 vs. 1 +/- 0.09 of control, p < 0.05). In conclusion, O-GlcNAcase activity is posttranslationally inhibited during GlcN-induced insulin resistance.
MeSH term(s)	Acetylglucosaminidase/biosynthesis ; Acetylglucosaminidase/genetics ; Acetylglucosaminidase/metabolism ; Animals ; Gene Expression Regulation, Enzymologic ; Glucosamine/toxicity ; Insulin Resistance/physiology ; Male ; Muscle, Skeletal/drug effects ; Muscle, Skeletal/enzymology ; RNA, Messenger/biosynthesis ; Rats ; Rats, Sprague-Dawley ; beta-N-Acetylhexosaminidases/antagonists & inhibitors ; beta-N-Acetylhexosaminidases/biosynthesis ; beta-N-Acetylhexosaminidases/genetics ; beta-N-Acetylhexosaminidases/metabolism
Chemical Substances	RNA, Messenger ; hexosaminidase C (EC 3.2.1.50) ; Acetylglucosaminidase (EC 3.2.1.52) ; beta-N-Acetylhexosaminidases (EC 3.2.1.52) ; Glucosamine (N08U5BOQ1K)
Language	English
Publishing date	2010
Publishing country	Switzerland
Document type	Comparative Study ; Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	206671-3
ISSN	1423-0313 ; 0031-7012
ISSN (online)	1423-0313
ISSN	0031-7012
DOI	10.1159/000279329
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Article: D-optimal designs and N-way techniques to determine sulfathiazole in milk by molecular fluorescence spectroscopy

Morales, Rocío / Ortiz, M. Cruz / Sarabia, Luis A / Sánchez, M. Sagrario

Analytica chimica acta. 2011 Nov. 30, v. 707, no. 1-2

2011

Abstract: ... To do this, two chemometric tools are used together: a D-optimal design for studying the effect ... with UHT milk, 4:6 rate for TCA:milk volumes and 40μL of fluorescamine. In UHT milk, the mean recovery (n=5 ...

Abstract	The present work proposes an analytical procedure to determine sulfathiazole in milk by using molecular fluorescence spectroscopy. For this sulfonamide the European Union in Regulation 37/2010 has established a maximum residue limit in milk of 100μgkg⁻¹. The study includes the effect of six factors on the recovery of sulfathiazole. The factors are: (i) The one related to the matrix depending on the heat treatment of the milk (UHT, pasteurized); (ii) Those related to the protein precipitation step, namely the ratio between the volume of trichloroacetic acid (TCA) and milk, centrifugation speed and temperature; (iii) Those affecting the derivatization reaction: derivatization time and volume of fluorescamine. To do this, two chemometric tools are used together: a D-optimal design for studying the effect of the factors on the recovery of sulfathiazole, considerably reducing the number of needed experiments; and the second-order property of the PARAFAC (Parallel Factor Analysis) decomposition that avoids the need of fitting a new calibration model each time that the experimental conditions change. It has been found that the type of milk, the TCA:milk ratio and the volume of fluorescamine have significant effect on the response. The rest of factors and interactions are not significant. The best recovery is obtained with UHT milk, 4:6 rate for TCA:milk volumes and 40μL of fluorescamine. In UHT milk, the mean recovery (n=5) in the optimal conditions is 88.7% (RSD=12.4%). As some non-linear behaviour may occur when using fluorescence spectroscopy, the calibration model that relates the fluorescence spectra with the concentration is computed by a partial least squares regression and a multi-layer feed-forward neural network. In both cases, the proposed procedures have been validated according to Decision 2002/657/EC, concluding that the two are accurate although the calibration model built with the neural network has better figures of merit, the decision limit (CCα) for x₀=100μgL⁻¹ is 103.3μgL⁻¹ and the detection capability (CCβ) is 106.5μgL⁻¹, with the probabilities of false noncompliance (α) and false compliance (β) equal to 5%.
Keywords	European Union ; UHT milk ; centrifugation ; chemometrics ; compliance ; derivatization ; factor analysis ; fluorescence ; fluorescence emission spectroscopy ; heat treatment ; least squares ; maximum residue limits ; milk ; neural networks ; sulfathiazole ; temperature ; trichloroacetic acid
Language	English
Dates of publication	2011-1130
Size	p. 38-46.
Publishing place	Elsevier B.V.
Document type	Article
ZDB-ID	1483436-4
ISSN	1873-4324 ; 0003-2670
ISSN (online)	1873-4324
ISSN	0003-2670
DOI	10.1016/j.aca.2011.09.014
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Article: Validation of an analytical method for quality control of residual solvents (n-hexane and acetone) in D-002: new active ingredient from beeswax.

Antolín, Ernesto Méndez / Quiñónez, Yaisme Balcinde / Canavaciolo, Víctor González / Cruz, Esperanza Rodríguez

Journal of pharmaceutical and biomedical analysis

2008 Volume 47, Issue 3, Page(s) 646–650

Abstract: ... simultaneously residual n-hexane and acetone in D-002 using the headspace gas chromatography (HS/GC) is described ... D-002 is a new natural product consisting of a mixture of aliphatic fatty alcohols, which shows ... The very poor solubility of D-002 in most solvents did necessary sample preparations in solid state. Limit ...

Abstract	D-002 is a new natural product consisting of a mixture of aliphatic fatty alcohols, which shows antioxidant and anti-ulcer effects in experimental models. A new validated methodology for determining simultaneously residual n-hexane and acetone in D-002 using the headspace gas chromatography (HS/GC) is described. The very poor solubility of D-002 in most solvents did necessary sample preparations in solid state. Limit test conditions allowed a detection of residual n-hexane and acetone more sensitively than that recommended for such purposes in the general method of the European Pharmacopoeia. Validation assays, applied to both D-002 residual solvents, proved: suitable sensitivity; very high linearity (correlation coefficients > or =0.999, R.S.D. of slopes < or =0.8% and R.S.D. of response factors < or =5% and no biases) and accuracy (average recoveries between 94.7 and 100.1%); and precision was < or =2.1%. The method was found suitable for quality control and stability studies of this new product.
MeSH term(s)	Acetone/analysis ; Chromatography, Gas ; Fatty Alcohols/analysis ; Fatty Alcohols/standards ; Hexanes/analysis ; Quality Control ; Solvents/analysis
Chemical Substances	D 002 ; Fatty Alcohols ; Hexanes ; Solvents ; Acetone (1364PS73AF) ; n-hexane (2DDG612ED8)
Language	English
Publishing date	2008-07-15
Publishing country	England
Document type	Journal Article ; Validation Studies
ZDB-ID	604917-5
ISSN	1873-264X ; 0731-7085
ISSN (online)	1873-264X
ISSN	0731-7085
DOI	10.1016/j.jpba.2008.02.003
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Article: Toxicity of beta-amyloid in HEK293 cells expressing NR1/NR2A or NR1/NR2B N-methyl-D-aspartate receptor subunits.

Domingues, A / Almeida, S / da Cruz e Silva, E F / Oliveira, C R / Rego, A C

Neurochemistry international

2007 Volume 50, Issue 6, Page(s) 872–880

Abstract: ... from overactivation of N-methyl-D-aspartate (NMDA) receptors and elevation of intracellular calcium ... However, the heterogeneity of the NMDA receptors, frequently composed of NR1 and NR2A-D subunits, has been less studied ... expressing NR1/NR2A. MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate ...

Abstract	Neurotoxicity induced by beta-amyloid peptide (Abeta) involves glutamate toxicity, resulting from overactivation of N-methyl-D-aspartate (NMDA) receptors and elevation of intracellular calcium. However, the heterogeneity of the NMDA receptors, frequently composed of NR1 and NR2A-D subunits, has been less studied. Thus, we determined the contribution of NMDA receptor subtypes on Abeta(1-40) toxicity in HEK293 cells transiently expressing NR1/NR2A or NR1/NR2B subunits. Analysis of lactate dehydrogenase (LDH) release and trypan blue exclusion revealed an increase in Abeta(1-40) toxicity upon NR1/NR2A expression, compared to NR1/NR2B, indicating loss of plasma membrane integrity. Furthermore, Abeta(1-40) decreased intracellular ATP in cells expressing NR1/NR2A. MK-801 ((+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate), a noncompetitive NMDA receptor antagonist, partially prevented the decrease in cell viability and the energy impairment. These differences were not accounted for by the activation of caspases 2, 3, 8 and 9 or calpains or by DNA fragmentation, excluding the hypothesis of apoptosis. Functional NR1/NR2A and NR1/NR2B receptor subtypes were further evidenced by single-cell calcium imaging. Stimulation of NR1/NR2A receptors with NMDA/glycine revealed an increase in intracellular calcium in cells pre-exposed to Abeta(1-40). Opposite effects were observed upon activation of NR1/NR2B receptors. These results suggest that NR1/NR2A-composed NMDA receptors mediate necrotic cell death in HEK293 cells exposed to Abeta(1-40) through changes in calcium homeostasis.
MeSH term(s)	Adenosine Triphosphate/metabolism ; Amyloid beta-Peptides/toxicity ; Blotting, Western ; Calcium/metabolism ; Caspases/metabolism ; Cell Line ; Cell Survival/physiology ; DNA Fragmentation ; Dizocilpine Maleate/pharmacology ; Excitatory Amino Acid Antagonists/pharmacology ; Humans ; Immunohistochemistry ; L-Lactate Dehydrogenase/metabolism ; Receptors, N-Methyl-D-Aspartate/genetics ; Receptors, N-Methyl-D-Aspartate/metabolism ; Stimulation, Chemical ; Transfection
Chemical Substances	Amyloid beta-Peptides ; Excitatory Amino Acid Antagonists ; NR2A NMDA receptor ; NR2B NMDA receptor ; Receptors, N-Methyl-D-Aspartate ; Dizocilpine Maleate (6LR8C1B66Q) ; Adenosine Triphosphate (8L70Q75FXE) ; L-Lactate Dehydrogenase (EC 1.1.1.27) ; Caspases (EC 3.4.22.-) ; Calcium (SY7Q814VUP)
Language	English
Publishing date	2007-05
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	283190-9
ISSN	1872-9754 ; 0197-0186
ISSN (online)	1872-9754
ISSN	0197-0186
DOI	10.1016/j.neuint.2007.03.001
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Article: Effects of the abused solvent toluene on recombinant N-methyl-D-aspartate and non-N-methyl-D-aspartate receptors expressed in Xenopus oocytes.

Cruz, S L / Mirshahi, T / Thomas, B / Balster, R L / Woodward, J J

The Journal of pharmacology and experimental therapeutics

1998 Volume 286, Issue 1, Page(s) 334–340

Abstract: ... the function of ionotropic glutamate receptors. Oocytes were injected with mRNA for specific N-methyl-D ...

Abstract	Previous studies have shown that toluene, which is commonly abused, depresses neuronal activity and causes behavioral effects in both animals and man similar to those observed for ethanol. In this study, the oocyte expression system was used to test the hypothesis that toluene, like ethanol, inhibits the function of ionotropic glutamate receptors. Oocytes were injected with mRNA for specific N-methyl-D-aspartate (NMDA) or non-NMDA subunits and currents were recorded using conventional two-electrode voltage clamp. To enhance the low water solubility of toluene, drug solutions were prepared by mixing toluene with alkamuls (ethoxylated castor oil) at a 1:1 ratio (v:v) and diluting this mixture to the appropriate concentration with barium-containing normal frog Ringer solution. Alkamuls, up to 0.1%, had no significant effects on membrane leak currents or on NMDA-induced currents. Toluene, up to approximately 9 mM, had only minor effects on membrane leak currents but dose-dependently inhibited NMDA-mediated currents in oocytes. The inhibition of NMDA receptor currents by toluene was rapid, reversible and the potency for toluene's effects was subunit dependent. The NR1/2B subunit combination was the most sensitive with an IC50 value for toluene-induced inhibition of 0.17 mM. The NR1/2A and NR1/2C receptors were 6- and 12-fold less sensitive with IC50 values of 1.4 and 2.1 mM, respectively. In contrast, toluene up to approximately 9 mM did not inhibit kainate-induced currents in oocytes expressing GluR1, GluR1(+)R2 or GluR6 subunits. These results suggest that some of the effects of toluene on neuronal activity and behavior may be mediated by inhibition of NMDA receptors.
MeSH term(s)	Anesthetics, Inhalation/toxicity ; Animals ; Behavior, Animal/drug effects ; Dose-Response Relationship, Drug ; Ethanol/toxicity ; Female ; Oocytes/metabolism ; Receptors, N-Methyl-D-Aspartate/chemistry ; Receptors, N-Methyl-D-Aspartate/drug effects ; Receptors, N-Methyl-D-Aspartate/physiology ; Recombinant Proteins/drug effects ; Toluene/toxicity ; Xenopus laevis
Chemical Substances	Anesthetics, Inhalation ; Receptors, N-Methyl-D-Aspartate ; Recombinant Proteins ; Toluene (3FPU23BG52) ; Ethanol (3K9958V90M)
Language	English
Publishing date	1998-07
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, P.H.S.
ZDB-ID	3106-9
ISSN	1521-0103 ; 0022-3565
ISSN (online)	1521-0103
ISSN	0022-3565
Database	MEDical Literature Analysis and Retrieval System OnLINE

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