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1,066 results for “Antagonistic”
Alpha-2 Adrenoreceptor Antagonist Yohimbine Potentiates Consolidation of Conditioned Fear (Open Data and Open Materials)
<p><strong>Open Data and Open Materials of: Sperl, M. F. J., Panitz, C., Skoluda, N., Nater, U. M., Pizzagalli, D. A., Hermann, C., & Mueller, E. M. (2022). Alpha-2 adrenoreceptor antagonist yohimbine potentiates consolidation of conditioned fear. <em>International Journal of Neuropsychopharmacology</em>, 25(9), 759–773.</strong></p> <p><em>Background:</em> Hyperconsolidation of aversive associations and poor extinction learning have been hypothesized to be crucial in the acquisition of pathological fear. Previous animal and human research points to the potential role of the catecholaminergic system, particularly noradrenaline and dopamine, in acquiring emotional memories. Here, we investigated in a between-participants design with 3 groups whether the noradrenergic alpha-2 adrenoreceptor antagonist yohimbine and the dopaminergic D2-receptor antagonist sulpiride modulate long-term fear conditioning and extinction in humans.<br><em>Methods:</em> Fifty-five healthy male students were recruited. The final sample consisted of n = 51 participants who were explicitly aware of the contingencies between conditioned stimuli (CS) and unconditioned stimuli after fear acquisition. The participants were then randomly assigned to 1 of the 3 groups and received either yohimbine (10 mg, n = 17), sulpiride (200 mg, n = 16), or placebo (n = 18) between fear acquisition and extinction. Recall of conditioned (non-extinguished CS+ vs CS−) and extinguished fear (extinguished CS+ vs CS−) was assessed 1 day later, and a 64-channel electroencephalogram was recorded.<br><em>Results:</em> The yohimbine group showed increased salivary alpha-amylase activity, confirming a successful manipulation of central noradrenergic release. Elevated fear-conditioned bradycardia and larger differential amplitudes of the N170 and late positive potential components in the event-related brain potential indicated that yohimbine treatment (compared with a placebo and sulpiride) enhanced fear recall during day 2.<br><em>Conclusions:</em> These results suggest that yohimbine potentiates cardiac and central electrophysiological signatures of fear memory consolidation. They thereby elucidate the key role of noradrenaline in strengthening the consolidation of conditioned fear associations, which may be a key mechanism in the etiology of fear-related disorders.</p>
Dataset for article: Pro-cognitive effects of dual tacrine derivatives acting as cholinesterase inhibitors and NMDA receptor antagonists
<p>Figure 1. Chemical structures of tacrine (<strong>a</strong>) and its derivatives created by introducing substituents on the aromatic core and/or altering the size of the cycloalkyl moiety attached to the aromatic region: 7-MEOTA (<strong>b</strong>), K1578 (7-chloro-1<em>H</em>,2<em>H</em>,3<em>H</em>-cyclopenta[<em>b</em>]quinolin-9-amine; <strong>c</strong>), K1592 (1-chloro-6<em>H</em>,7<em>H</em>,8<em>H</em>,9<em>H</em>,10<em>H</em>-cyclohepta[<em>b</em>]quinolin-11-amine; <strong>d</strong>), K1594 (6-methyl-1,2,3,4-tetrahydroacridin-9-amine; <strong>e</strong>), and K1599 (7-methoxy-1<em>H</em>,2<em>H</em>,3<em>H</em>-cyclopenta[<em>b</em>]quinolin-9-amine; <strong>f</strong>). Compounds in this study were used in the form of hydrochloride salts.</p> <p>Figure_2_values. Test results. Morris water maze: scopolamine-induced model of cognitive deficit in the acquisition and reversal phases. The graphs show the effects of K1578 (<strong>a</strong>), K1592 (<strong>b</strong>), K1594 (<strong>c</strong>), and K1599 (<strong>d</strong>) on escape latency during the acquisition phase, where none of the compounds ameliorated the deficit of spatial learning. The remaining graphs display the effects of K1578 (<strong>e</strong>), K1592 (<strong>f</strong>), K1594 (<strong>g</strong>), and K1599 (<strong>h</strong>) in the reversal phase, where K1578 (1 mg/kg) and K1599 (at both doses), and marginally K1592 (1 mg/kg; see in the text), mitigated the scopolamine-induced deficit of reversal learning. VEH – vehicle, the numbers in brackets denote the dose applied (mg/kg). Data are presented as the mean + SEM, * vs. VEH, * p < 0.05, ** p < 0.01, *** p < 0.001. <em>n</em> = 6–9 animals per group. Statistical significance was determined using two-way repeated measures ANOVA (a–d) or ANOVA (e, f, h) followed by Dunnett’s multiple comparisons tests.</p> <p>Figure-3_values. Test results. Morris water maze: MK-801-induced model of cognitive deficit in the acquisition phase. The graphs illustrate the effects of the compounds K1578 (<strong>a</strong>), K1592 (<strong>b</strong>), K1594 (<strong>c</strong>), and K1599 (<strong>d</strong>) on escape latency. Only K1599 (1 mg/kg) ameliorated the MK-801-induced deficit of spatial learning. VEH – vehicle, the numbers in brackets denote the dose (mg/kg). Data are presented as the mean + SEM, * vs. VEH, * p < 0.05, ** p < 0.01. <em>n</em> = 5–7 animals per group. Statistical significance was determined using two-way repeated measures ANOVA followed by Dunnett’s multiple comparisons tests.</p> <p>Figure_4_values. Open field test. The results demonstrate the effects of K1578 (<strong>a</strong>), K1592 (<strong>b</strong>), K1594 (<strong>c</strong>), and K1599 (<strong>d</strong>) on the distance moved by intact and MK-801-treated animals. VEH – vehicle, the numbers in brackets denote the dose (mg/kg). Data are presented as the mean + SEM, * vs. VEH group of the corresponding phenotype, * p < 0.05, ** p < 0.01, **** p < 0.0001. <em>n</em> = 6–14 animals per group. A significant effect of both factors (treatment and phenotype) was determined using two-way ANOVA, followed by Dunnett’s multiple comparisons tests.</p> <p>Figure-5_values. Acetylcholinesterase activity. The results document the effect of the compounds (1 mg/kg ip) on AChE activity in the hippocampus (<strong>a</strong>), prefrontal cortex (<strong>b</strong>), striatum (<strong>c</strong>), and whole brain sample (<strong>d</strong>). K1578 and K1599 decreased AChE activity in the striatum. VEH – vehicle. Data are presented as the median with minimum to maximum range, * vs. VEH, *** p < 0.001, **** p < 0.0001. VEH samples AChE enzyme activities reached the following absolute values (a) 15.19 ± 3.09 U/mg protein, (b) 9.810 ± 1.54 U/mg protein, (c) 26.05 ± 3.27 U/mg protein, and (d) 27.38 ± 3.36 U/mg protein. Significance was determined by ANOVA (graphs c, d), followed by Dunnett’s multiple comparisons tests.</p> <p>Figure_6_values. Electrophysiology: Inhibition of GluN1/GluN2A receptors by K1599. Representative whole-cell patch-clamp recordings measured from HEK293 cells expressing the GluN1/GluN2A receptors held at a membrane voltage of −80 mV and +60 mV; 30 μM K1599 was applied as indicated. Results summarizing the relative inhibition induced by 30 µM K1599, measured at the indicated membrane potentials. <em>n</em> ≥ 5 cells per each condition.</p> <p>Table_1. The rats were pseudo-randomly assigned to one of the 18 treatment groups listed in. Each group received two injections: one containing the study compound and another containing either MK-801 or scopolamine, as indicated by the group name. The vehicle group (VEH) received the DMSO vehicle (2.5 mL/kg) and saline. The “scopolamine” and “MK-801” groups received scopolamine or MK-801, respectively, along with the DMSO vehicle (2.5 mL/kg).</p> <p>Table 2. Treatment groups and <em>n</em> in biochemical experiments - AChE activity assay.</p>
Cell growth dataset for "Suppression of bacterial cell death underlies the antagonistic interaction between ciprofloxacin and tetracycline in Escherichia coli"
<div>This dataset contains growth data of <em>E. coli</em> cells measured by optical density at a wavelenght of 600 nm (OD600) to determine the conditions where the combination of ciprofloxacin (CIP) and tetracycline (TET) is antagonistic (or suppressive), using a medium that supports fast, intermediate and slow growth (M9 based medium supplemented with: glucose and amino acid, glucose, and glycerol, respectively).</div> <div>Two types of assays were performed: a checkerboard assay with a 2-dimension gradient of antibiotic concentrations shown in "Fig-S1-Growth_rates-Checkerboard_assay.zip", and bulk growth rates assay shown in "Fig-S2-Bulk_doubling_rates-Bioreactor.zip". </div> <div>These experiments are presented in the supplementary figures of the following manuscript published as preprint in bioRxiv: https://doi.org/10.1101/2024.04.18.590101.</div> <div> </div> <p><strong>Fig-S1-Growth_rates-Checkerboard_assay.zip:</strong></p> <div>- growth-OD600-Blank_correct.xlsx: contains the blank corrected (subtracted by initial OD of sterile medium) OD600 data for each well measured in the checkerboard assay. The negative control is named as "Blank B" in the spreasheet and the antibiotic concentrations for each well is defined in column C (Content).</div> <div>- growth_data.xlsx: contains the processed data from "Growth-OD600-Blank_correct.xlsx":growth curves were smoothed with a 5-window moving median and outliers corrected using the filloutliers function in MATLAB. Outliers that were missed were manually corrected.</div> <div>- time_h.xlsx: contains the time in hours used by the matlab function to build the dose response figure S1B.</div> <div>- analysis_code_checkerboard_assay.m: matlab function used to build the dose response figure S1B.</div> <p> </p> <p><strong>Fig-S2-Bulk_doubling_rates-Bioreactor.zip:</strong></p> <p>- "bulk_doubling rates_gly/glu/gluaa.csv": contains the calculated doubling rates for each of three experimental replicates (rows) and for each antibiotic treatment (columns: Ctrl, CIP, TET, CIP-TET) as shown in Figure S2. These values were used to calculated the Bliss independence (for further details see https://gitlab.com/MEKlab/single-cell-suppression-2024/figure plotting.ipynb<br> - Folders containing OD600 measurements and calculated growth rates for each growth medium, which are further separated into folders for each experimental replicate. Each replicate folder is labelled as the date the experiment was performed (denoted as "*" hereon). Each contains the following: raw optical density data (*.txt files), summary of experiment and results (*.docx file), the function compute_growth_rates.m, and the script Growth_curves_*.m.</p> <div>For more information on methods, strains used and table header descriptions, please refer to the README.txt. </div>
Data from: Exploring hymenopteran parasitoid communities and their hosts: A comparative study of farmland and semi-natural ecotones with focus on pentatomoid bugs and their antagonists
<p>Here, we provide abundance data, the respective R-script and R-readable data files from a small-scale study on hymenopteran parasitoid communities and their hosts, with special focus on pentatomoid bugs and their egg parasitoids. This comparative study was conducted in farmland and semi-natural ecotones from June to September 2020 in South Tyrol, Italy. The fauna was sampled during four sampling events with sweep netting, beat netting, yellow pan traps, Malaise traps and visual inspections. Arthropods were identified to order level, hymenopteran parasitoids to family level, pentatomoid bugs to species level and egg parasitoids of pentatomoids as far as possible to species level. If identification was not possible, pentatomoid parasitoids were left at genus level. The abundance data collected with each survey method were pooled per survey events and survey site.</p>
Sexually antagonistic selection on educational attainment and body size in Estonian children
<p>Natural selection is a key mechanism of evolution, which results from the differential reproduction of phenotypes. We describe fecundity selection at different parity transitions on 15 anthropometric traits and educational attainment in Estonian children, who were born between 1938 and 1962 and measured at around 13 years of age (Juhan Aul’s database). The sample sizes reach up to 7000 in boys and 10 000 in girls. The direction of selection on educational attainment and bodily traits was sexually antagonistic, and it occurred via different parity transitions in boys and girls. Compared to boys with primary education, obtaining tertiary education was associated with 3.5 times and secondary education two times higher odds of becoming a father. Transition to motherhood was not related to educational attainment, while education above primary was associated with lower odds (OR = 0.5 – 0.7) to progression to parities above one and two. Selection on anthropometric traits occurred almost exclusively via childlessness in boys, while among the girls, most of the traits that were associated with becoming a mother were additionally associated with a transition from one child to higher parities. Male (but not female) fitness was thus primarily determined by traits related to mating success. Selection favoured stronger and larger boys and smaller girls. Selection on girls favoured some traits that associate with perceived femininity while other feminine traits were selected against.</p> <p>This record includes the data and R code to reproduce the statistical analyses the results are based on. </p> <p> </p>
Beyond depression and anxiety; a systematic review about the role of corticotropin-releasing hormone antagonists in diseases of the pelvic and abdominal organs-Worksheets
<p>This file has several worksheets corresponding to the data used for the review with the same table as indicated in the file</p>
Systematic review reveals sexually antagonistic knockouts in model organisms data and code
<p>R Code and data for manuscript titled "Systematic review reveals sexually antagonistic knockouts in model organisms".</p> <p>Drosophila data is from Ruzicka, F., Hill, M.S., Pennell, T.M., Flis, I., Ingleby, F.C., Mott, R., Fowler, K., Morrow, E.H., Reuter, M., 2019. Genome-wide sexually antagonistic variants reveal long-standing constraints on sexual dimorphism in fruit flies. PLoS Biol. 17, e3000244.</p> <p>https://journals.plos.org/plosbiology/article?id=10.1371/journal.pbio.3000244</p> <p>Human data is from Harper, J.A., Janicke, T., Morrow, E.H., 2021. Systematic review reveals multiple sexually antagonistic polymorphisms affecting human disease and complex traits. Evolution 75, 3087–3097. https://doi.org/10.1111/evo.14394</p> <p>https://onlinelibrary.wiley.com/doi/full/10.1111/evo.14394</p>
Raw diffraction images of endothelin ETB receptor bound to clinical antagonist bosentan and its analog
<p>Diffraction images of endothelin ET<sub>B</sub> receptor bound to bosentan (PDB code 5XPR) and K-8794 (5X93).</p> <p>Bosentan is an oral medication approved for the treatment of pulmonary arterial hypertension. K-8794 is the ETB-selective high-affinity analog of bosentan.</p> <p>Two datasets of 5X93 were collected with helical method, while for 5XPR 16 small-wedge (10°/crystal) datasets were collected automatically using ZOO system. In both cases the diffraction images were collected from loop-harvested microcrystals using MX225HS CCD detector at a wavelength of 1 Å on BL32XU, SPring-8.</p> <p>For 5XPR, 14 datasets were merged at 3.6 Å resolution in the published result (Shihoya et al. NSMB 2017) using KAMO; see processing note: https://github.com/keitaroyam/yamtbx/wiki/Processing-ETBR-bonsentan-data-(5XPR)</p> <p>NOTE</p> <ul> <li> <p>Most frames have (relatively weak) lipid rings.</p> </li> </ul> <ul> <li> <p>There is the indexing ambiguity problem in 5XPR (space group P3<sub>2</sub>21) that should be resolved before merging.</p> </li> <li> <p>5xpr_bosentan/bosentan-1425-01/multi_002_000019.img.bz2 is missing (probably due to a detector problem)</p> </li> </ul>
Raw diffraction images of human orexin 2 receptor bound to the subtype-selective antagonist EMPA
<p>Human orexin 2 receptor (OX2R) is a member of G protein-coupled receptors (GPCR). OX2R plays important roles in modulating feeding behavior and regulating the sleep-wake cycle.</p> <p>805 small-wedge (1-6°/crystal) datasets collected from loop-harvested microcrystals using MX225HS CCD detector at a wavelength of 1 Å on BL32XU, SPring-8. The crystals belonged to space group C2 with unit cell parameters a=94.1, b=75.5, c=95.9 Å, β=111.4°.</p> <p>631 datasets were merged at 1.96 Å resolution in the published result (Suno et al. Structure 2017; PDB code: 5WQC) using KAMO; see https://github.com/keitaroyam/yamtbx/wiki/Processing-OX2R-data-(5WQC)</p> <p>Note</p> <ul> <li>Most frames have lipid rings.</li> <li>One dataset (not included in the published result) was lost for some reason (so 804 datasets are available).</li> </ul>
Phenotypic divergence of traits that mediate antagonistic and mutualistic interactions between island and continental populations of the tropical plant, Tribulus cistoides (Zygophyllaceae)
<p><span><strong>Premise</strong>:</span><span> Island systems have long served as a model for evolutionary processes due to their unique species interactions. Many studies of the evolution of species interactions on islands have focused on endemic taxa. Fewer studies have focused on how antagonistic and mutualistic interactions shape the phenotypic divergence of widespread non-endemic species living on island populations. </span></p> <p><span><strong>Methods</strong>:</span><span> We used the widespread plant <em>Tribulus</em> <em>cistoides</em> (Zygophyllaceae) to test phenotypic divergence in traits that mediate antagonistic interactions with vertebrate granivores (birds) and mutualistic interactions with pollinators and how this is explained by bioclimatic variables. We used both herbarium specimens and field-collected samples to compare phenotypic divergence between continental and island populations. </span></p> <p><span><strong>Results</strong>:</span><span> Fruits from island populations were larger than on continents, but the presence of lower spines on mericarps was lower on islands. The presence of spines was largely explained by environmental variation among islands. Petal length was on average 9% smaller on island than continental populations, an effect that was especially accentuated on the Galápagos Islands. </span></p> <p><span><strong>Conclusions</strong>:</span><span> <em>Tribulus</em> <em>cistoides</em> exhibits phenotypic divergence between island and continental habitats for antagonistic traits (seed defence) and mutualistic traits (floral traits). Further, the evolution of phenotypic traits that mediate antagonistic and mutualistic interactions depended on the abiotic characteristics of specific islands. This study shows the potential of using a combination of herbarium and field samples for comparative studies on a globally distributed species to test phenotypic divergence on island habitats.</span></p>
Figs 6–8 in A new species of Xenomyia Malloch, 1921 (Diptera: Muscidae) from South Africa, a probable natural antagonist of blackflies (Diptera: Simuliidae)
Figs 6–8. Xenomyia osculata sp. n. ♂ (paratype). 6. Sternite 5, dorsal view. 7. Hypandrium and aedeagus, lateral view. 8. Hypandrium and some aedeagal processes, dorsal view. a - epiphallus; b - phallapodeme; c - postgonite (paramere); d - praegonite (gonopod).
Figs 3–5 in A new species of Xenomyia Malloch, 1921 (Diptera: Muscidae) from South Africa, a probable natural antagonist of blackflies (Diptera: Simuliidae)
Figs 3–5. Xenomyia osculata sp. n. ♂ (paratype). 3. Head, lateral view. 4. Fore femur, posterior view. 5. Wing.
De Novo KOR Antagonists Datasets
<p>Datasets used as input, generated or analyzed in the manuscript <strong>De Novo Design of </strong><strong>κ</strong><strong>-Opioid Receptor Antagonists Using a Generative Deep Learning Framework</strong>:</p> <p>1. Pre-training Dataset #1 (4.6 million compounds from ZINC 20): zinc20_train.csv (494 MB)<br> 2. Pre-training test set (0.5 million compounds from ZINC 20): zinc20_test.csv (55 MB)<br> 3. Pre-training test scaffolds set (0.5 million compounds from ZINC 20): zinc20_test_scaffolds.csv (57 MB)<br> 4. Pre-training Dataset #2 (2,056 compounds from ChEMBL with IC50 data): chembl30_kor_inhibitors.csv (144 KB)<br> 5. 169 compounds prioritized for chemical synthesis on the basis of their similarity to JDTic's interactions with KOR: prioritized_169candidates_from1M_by_SIFt_Tc.csv (17 KB)<br> <br> All datasets are in Simplified Molecular Input Line Entry System (SMILES) format.</p>
Structure-Based Discovery of Mouse Trace Amine-Associated Receptor 5 Antagonists
<p>Topology, parameter and coordinates files of the Molecular dynamics (MD) simulations of mTAAR5 3D models in complex with the three novel antagonists (Compound 9, 10 and 11, Table S4). We used ACEMD3 (v3.5.1) as a molecular engine, CHARMM36 as force field. The three replicas of 200 ns (xtc files) were concatened in a single trajectory for each system. Water molecules, ions, and membrane atoms (POPC: phosphatidylcholine) atoms were removed from the original trajectories and topology before the upload.</p>
Edoxaban Treatment Versus Vitamin K Antagonist in Patients With Atrial Fibrillation Undergoing Percutaneous Coronary Intervention
ClinicalTrials.gov study NCT02866175. IPD Sharing: YES. Countries: 18. Publications: 3.
Edoxaban Treatment Versus Vitamin K Antagonist (VKA) in Patients With Atrial Fibrillation (AF) Undergoing Catheter Ablation
ClinicalTrials.gov study NCT02942576. IPD Sharing: YES. Countries: 11. Publications: 10.
Pre-IVF Treatment With a GnRH Antagonist in Women With Endometriosis
ClinicalTrials.gov study NCT04173169. IPD Sharing: YES. Countries: 1. Publications: 2.
Antagonistic effects of predator colour morph abundance and saliency on prey anti-predator responses
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Phenotypic divergence of traits that mediate antagonistic and mutualistic interactions between island and continental populations of the tropical plant, Tribulus cistoides (Zygophyllaceae)
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Data from: Managing friends and foes: Sanctioning mutualists in mixed‐infection nodules trades off with defense against antagonists
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Allen Brain Atlas
Allen Brain Atlas is an Allen Institute collection of brain map atlases, datasets, APIs, and analysis tools covering mouse, human, and non-human primate brain resources.
Annotated Behaviour and Observability Dataset (ABODe)
ABODe is a University of Edinburgh DataShare dataset for behavior classification in group-housed mice using home-cage video, identities, bounding boxes, ground-plate positions, and annotator labels.
DANDI Archive for NWB datasets
DANDI is a BRAIN Initiative archive for publishing and sharing neurophysiology data, including electrophysiology, optophysiology, and behavioral data packaged as NWB and related standards.
International Brain Laboratory public data
The International Brain Laboratory public data releases expose standardized mouse decision-making experiments, including Neuropixels recordings, widefield calcium imaging, behavior, and session metadata accessed through the ONE API.
OpenNeuro
OpenNeuro is a free, open platform for sharing neuroimaging datasets, with public search, dataset pages, and download paths for web, S3, DataLad, and the OpenNeuro CLI.