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关键词:'H31859'
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Susana Sadler Simões et al.
Forensic science international, 243, 117-125 (2014-08-16)
An UPLC-MS/MS method using ESI+ionization and MRM was developed and fully validated according to international guidelines for the qualitative and quantitative analysis of nine synthetic cannabinoids and/or their metabolites in urine samples (1mL). Prior to extraction the samples were subjected
Jens Halvard Grønlien et al.
European journal of pharmacology, 647(1-3), 37-47 (2010-09-08)
Genistein and 5-hydroxyindole (5-HI) potentiate the α7 nicotinic acetylcholine receptor current by primarily increasing peak amplitude, a property of type I α7 positive allosteric modulation. In this study, the effects of these two compounds were investigated at two different α7/5-HT(3)
Xiang-Qun Hu et al.
Neuropharmacology, 54(8), 1153-1165 (2008-04-26)
Allosteric modulation of ligand-gated ion channels can play important roles in shaping synaptic transmission. The function of the 5-hydroxytryptamine (serotonin) type 3 (5-HT(3)) receptor, a member of the Cys-loop ligand-gated ion channel superfamily, is modulated by a variety of compounds
Beatriz E Nielsen et al.
Cellular and molecular life sciences : CMLS, 75(13), 2457-2471 (2018-01-10)
The α7 nicotinic receptor is a promising drug target for neurological and inflammatory disorders. Although it is the homomeric member of the family, a novel α7β2 heteromeric receptor has been discovered. To decipher the functional contribution of the β2 subunit
Eva-Maria Karg et al.
Journal of medicinal chemistry, 52(11), 3474-3483 (2009-06-06)
Pharmacological suppression of leukotriene biosynthesis by inhibitors of 5-lipoxygenase (5-LO) is a strategy to intervene with inflammatory and allergic disorders. We recently presented 2-amino-5-hydroxy-1H-indoles as efficient 5-LO inhibitors in cell-based and cell-free assays. Structural optimization led to novel benzo[g]indole-3-carboxylates exemplified
Gretchen Y López-Hernández et al.
Neuropharmacology, 56(4), 821-830 (2009-08-26)
One approach for the identification of therapeutic agents for Alzheimer's disease has focused on the research of alpha7 nAChR-selective agonists such as the partial agonists 3-(4-hydroxy,2-methoxybenzylidene)anabaseine (4OH-GTS-21) and, more recently, 2-[2-(4-bromophenyl)-2-oxoethyl]-1-methyl pyridinium (S 24795). An alternative approach for targeting alpha7
Piotr Luliński et al.
Talanta, 129, 155-164 (2014-08-17)
A 2-(4-methoxyphenyl)ethylamine imprinted polymer (MIP) was successfully applied for the selective separation of tyramine. A computational analysis was used to predict the affinity of the polymer matrix towards tyramine and a preliminary experimental evaluation was made for the target analyte.
Tsukasa Sasaki et al.
Chirality, 22(2), 258-261 (2009-06-06)
A solution of optically pure kynurenine (KYN), i.e., D-KYN or L-KYN, was administered intravenously to male Sprague-Dawley rats (10 mg kg(-1) ml(-1)). The time-course of changes in the concentrations of urinary monoamines and their metabolites such as 5-hydroxytryptamine (5-HT), 5-hydroxyindole
Eric T Ritschdorff et al.
Analytical chemistry, 81(21), 8790-8796 (2009-10-31)
We demonstrate the feasibility for minimizing electrophoretic analysis times of transient chemical species by inducing nascent, oppositely charged photochemical products to migrate in opposite directions from their point of creation. In this approach, separate probe sites are positioned within an
Jeffrey S Thinschmidt et al.
Brain research, 1203, 51-60 (2008-03-07)
One approach to treatment of negative cognitive effects associated with Alzheimer's disease and schizophrenia may involve activation of neuronal alpha7 nicotinic acetylcholine receptors (nAChRs). We used the alpha7-selective partial agonist 3-(4-hydroxy, 2-methoxy-benzylidene)anabaseine (4OH-GTS-21), the alpha7 modulator 5-hydroxyindole (5-HI), and recombinant
Damon Borg et al.
Journal of analytical toxicology, 41(1), 6-16 (2016-09-30)
Synthetic cannabinoids are a group of psychoactive compounds that mimic the effects of Δ9-tetrahydrocannabinol, the primary psychoactive constituent of marijuana (Cannabis sativa L). The Drug Enforcement Administration has classified many of the most common cannabinoids as Schedule 1 controlled substances.
Ruth Livingstone et al.
The Journal of chemical physics, 135(19), 194307-194307 (2011-11-25)
Time-resolved photoelectron spectroscopy was used to obtain new information about the dynamics of electronic relaxation in gas-phase indole and 5-hydroxyindole following UV excitation with femtosecond laser pulses centred at 249 nm and 273 nm. Our analysis of the data was
Aman Kumar et al.
Cell host & microbe, 28(1), 41-53 (2020-06-11)
The gut-brain axis is crucial to microbial-host interactions. The neurotransmitter serotonin is primarily synthesized in the gastrointestinal (GI) tract, where it is secreted into the lumen and subsequently removed by the serotonin transporter, SERT. Here, we show that serotonin decreases
Sung Jin Bae et al.
Biological & pharmaceutical bulletin, 33(4), 550-555 (2010-04-23)
5-Hydroxyindole (5HI), a metabolite of tryptophan, is involved in learning and memory, central neuron system regulation, and anti-oxidant activity. However, its protective action in mitochondrial function is not clear. Here, we tested whether 5HI protects against tert-butylhydroperoxide (t-BHP)-induced oxidative damage
Uday Praful Kundap et al.
Pharmaceuticals (Basel, Switzerland), 13(6) (2020-05-30)
Epilepsy is a serious neurological disorder affecting around 70 million people globally and is characterized by spontaneous recurrent seizures. Recent evidence indicates that dysfunction in metabolic processes can lead to the alteration of neuronal and network excitability, thereby contributing to
Studies on the pharmacological properties of oxindole (2-hydroxyindole) and 5-hydroxyindole: are they involved in hepatic encephalopathy?
F Moroni et al.
Advances in experimental medicine and biology, 420, 57-73 (1997-01-01)
P Aparoy et al.
Bioorganic & medicinal chemistry letters, 21(1), 456-462 (2010-11-19)
In this study, comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were performed on a series of 2-substituted 5-hydroxyindole-3-carboxylate derivatives as potent 5-LOX inhibitors with IC(50) values ranging from 0.031 to 13.4 μM. Two datasets of
Jian Mao et al.
Se pu = Chinese journal of chromatography, 27(2), 216-219 (2009-07-25)
A simple method was developed for the analysis of 6-hydroxy-1-methyl-1,2,3,4-tetrahydro-beta-carboline (6-OH-MTHbetaC), 5-hydroxytryptamine (5-HT) and 5-hydroxyindole acetic acid (5-HIAA) in rat brain by high performance liquid chromatography with electrochemical detection (HPLC-ECD). The separation of the sample was performed on a Discovery
David Robinson et al.
The journal of physical chemistry. B, 113(8), 2535-2541 (2009-02-07)
We have investigated the absorption and emission spectrum of 5-hydroxyindole in the gas phase and in various solvents. 5-Hydroxyindole is the fluorophore of the non-natural amino acid 5-hydroxytryptophan, which has attracted recent interest as a novel intrinsic probe for protein
Martin Švidrnoch et al.
Talanta, 150, 568-576 (2016-02-04)
Perfluoroheptanoic acid was employed as a volatile micellar phase in background electrolyte for micellar electrokinetic chromatography-tandem mass spectrometry separation and determination of 15 selected naphthoyl- and phenylacetylindole- synthetic cannabinoids and main metabolites derived from JWH-018, JWH-019, JWH-073, JWH-200 and JWH-250.
Abdelahad Khajo et al.
PloS one, 6(9), e25092-e25092 (2011-10-04)
Certain fungi thrive in highly radioactive environments including the defunct Chernobyl nuclear reactor. Cryptococcus neoformans (C. neoformans), which uses L-3,4-dihydroxyphenylalanine (L-DOPA) to produce melanin, was used here to investigate how gamma radiation under aqueous aerobic conditions affects the properties of
Diane Latawiec et al.
PloS one, 5(2), e9234-e9234 (2010-02-20)
The action of dopamine on the aggregation of the unstructured alpha-synuclein (alpha-syn) protein may be linked to the pathogenesis of Parkinson's disease. Dopamine and its oxidation derivatives may inhibit alpha-syn aggregation by non-covalent binding. Exploiting this fact, we applied an
Junxia Zheng et al.
Chemical biology & drug design, 78(2), 314-321 (2011-05-24)
A series of indole and related benzo[g]indole compounds displaying potent activities against 5-lipoxygenase were selected to establish three-dimensional quantitative structure-activity relationships using comparative molecular field analysis and comparative molecular similarity indices analysis methods. A training set of 37 active compounds
Walid M Al-Ghoul et al.
International journal of biological sciences, 6(3), 282-293 (2010-06-23)
Melatonin is a possible protective agent in postburn gut pathophysiological dynamics. We investigated the role of endogenously-produced versus exogenously-administered melatonin in a major thermal injury rat model with well-characterized gut inflammatory complications. Our rationale is that understanding in vivo melatonin
Rui Shen Ong et al.
Drug testing and analysis, 12(2), 195-214 (2019-10-09)
We describe the validation of a method for the simultaneous analysis of 29 synthetic cannabinoids (SCs) and metabolites, 4 amphetamines, and 2 cannabinoids in human whole blood. This method enables one analysis to cover what previously required multiple analyses for
Kenichiro Todoroki
Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, 131(8), 1207-1211 (2011-08-02)
Fluorescence-derivatization-HPLC methods are powerful tools for performing the analysis of bioactive compounds with high sensitivity and selectivity. In this paper, the author reviews the development of the following four types of novel fluorescence-derivatization-HPLC analytical systems: (1) simultaneous HPLC analysis of
Matthew LaPorte et al.
The Journal of organic chemistry, 78(1), 167-174 (2012-11-10)
A convergent approach provides a convenient access to synthetically and biologically useful 3,4-disubstituted 5-hydroxyindoles. The one-pot procedure uses microwave heating to initiate an intramolecular [4 + 2]-cycloaddition of an alkynol segment onto a furan followed by a fragmentation, aromatization, and
E Albiñana et al.
Pflugers Archiv : European journal of physiology, 469(5-6), 779-795 (2017-02-09)
Choline is present at cholinergic synapses as a product of acetylcholine degradation. In addition, it is considered a selective agonist for α5 and α7 nicotinic acetylcholine receptors (nAChRs). In this study, we determined how choline affects action potentials and excitatory
Matthew R Skelton et al.
PloS one, 6(1), e16187-e16187 (2011-01-21)
Mutations in the creatine (Cr) transporter (CrT; Slc6a8) gene lead to absence of brain Cr and intellectual disabilities, loss of speech, and behavioral abnormalities. To date, no mouse model of CrT deficiency exists in which to understand and develop treatments
Anthony R Horner et al.
Journal of chromatography. A, 1589, 73-82 (2019-01-11)
Predicting retention and enthalpy allows for the simulation and optimization of advanced chromatographic techniques including gradient separations, temperature-assisted solute focusing, multidimensional liquid chromatography, and solvent focusing. In this paper we explore the fits of three expressions for retention as a
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