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1. Design and application of intramolecular vinylogous Michael reaction for the construction of 2-alkenyl indoles

Author:
Harish, Battu; Yadav, Sanjay; Suresh, Surisetti
Source:
Chemical communications 2021 v.57 no.2 pp. 231-234
ISSN:
1364-548X
Subject:
antagonists,   etc   ; chemical reactions; indoles;     Show all 3 Subjects
Abstract:
... A base-mediated transformation based on a designed intramolecular vinylogous Michael addition (intra-VMA) is presented to access 3-substituted 2-alkenyl indole derivatives. The reaction represents the first example of the intra-VMA for the construction of indoles. A one-pot N-allylation of ortho-tosylamidocinnamates/congeners with γ-bromocrotonates followed by intra-VMA has been described to provi ...
DOI:
10.1039/d0cc06564a

2. Impact of endocrine-disrupting chemicals on steroidogenesis and consequences on testicular function

Author:
Walker, Casandra; Garza, Samuel; Papadopoulos, Vassilios; Culty, Martine
Source:
Molecular and cellular endocrinology 2021 v.527 pp. 111215
ISSN:
0303-7207
Subject:
hormone antagonists,   etc   ; phthalates; steroidogenesis; testes;     Show all 4 Subjects
Abstract:
... Testicular steroidogenesis is a tightly regulated process that produces the androgens important for the development, maintenance and function of the male reproductive system. These androgens are also essential for overall health, and well-being. Disruptions in the ability of the testis to form steroids can result in developmental abnormalities, dysfunction, and infertility. Endocrine-disrupting ch ...
DOI:
10.1016/j.mce.2021.111215

3. Enabling the inclusion of non-hydrolysed sulfated long term anabolic steroid metabolites in a screening for doping substances by means of gas chromatography quadrupole time-of-flight mass spectrometry

Author:
Albertsdóttir, Aðalheiður Dóra; Van Gansbeke, Wim; Van Eenoo, Peter; Polet, Michael
Source:
Journal of chromatography 2021 v.1642 pp. 462039
ISSN:
0021-9673
Subject:
beta-adrenergic antagonists,   etc   ; excretion; metabolites;     Show all 3 Subjects
Abstract:
... The World Anti-Doping Agency (WADA) publishes yearly their prohibited list, and sets a minimum required performance limit for each substance. To comply with these stringent requirements, the anti-doping laboratories have at least two complementary methods for their initial testing procedure (ITP), one using gas chromatography – mass spectrometry (GC-MS) and the other using liquid chromatography-MS ...
DOI:
10.1016/j.chroma.2021.462039

4. Pre-training naltrexone increases conditioned fear learning independent of adolescent alcohol consumption history

Author:
Pajser, Alisa; Fisher, Hayley; Pickens, Charles L.
Source:
Physiology & behavior 2021 v.229 pp. 113212
ISSN:
0031-9384
Subject:
antagonists,   etc   ; adolescents; alcohol drinking; alcohols; fearfulness; males;     Show all 6 Subjects
Abstract:
... Our previous research has shown a relationship between low voluntary alcohol consumption and high conditioned fear in male Long Evans rats. Here, we examined whether differences in the endogenous opioid systems might be responsible for these differences. Rats received 6 weeks of chronic intermittent to 20% alcohol (v/v) or water-only from PND 26–66. Based on their consumption during the last 2 wee ...
DOI:
10.1016/j.physbeh.2020.113212

5. Odor coding in the mammalian olfactory epithelium

Author:
Kurian, Smija M.; Naressi, Rafaella G.; Manoel, Diogo; Barwich, Ann-Sophie; Malnic, Bettina; Saraiva, Luis R.
Source:
Cell and tissue research 2021 v.383 no.1 pp. 445-456
ISSN:
0302-766X
Subject:
antagonists,   etc   ; mammals; mucosa; odor compounds; odors; research;     Show all 6 Subjects
Abstract:
... Noses are extremely sophisticated chemical detectors allowing animals to use scents to interpret and navigate their environments. Odor detection starts with the activation of odorant receptors (ORs), expressed in mature olfactory sensory neurons (OSNs) populating the olfactory mucosa. Different odorants, or different concentrations of the same odorant, activate unique ensembles of ORs. This mechan ...
DOI:
10.1007/s00441-020-03327-1

6. Co-invalidation of Prnp and Sprn in FVB/N mice affects reproductive performances and highlight complex biological relationship between PrP and Shadoo

Author:
Castille, Johan; Passet, Bruno; Makhzami, Samira; Vilotte, Marthe; Moazami-Goudarzi, Katayoun; Truchet, Sandrine; Daniel-Carlier, Nathalie; Gaillard, Anne-Laure; Andréoletti, Olivier; Vaiman, Daniel; Beauvallet, Christian; Vaiman, Anne; Floriot, Sandrine; Calvel, Pierre; Mouillet-Richard, Sophie; Duchesne, Amandine; Béringue, Vincent; Vilotte, Jean-Luc
Source:
Biochemical and biophysical research communications 2021 v.551 pp. 1-6
ISSN:
0006-291X
Subject:
antagonists,   etc   ; embryogenesis; genetic background; lactation; mice; phenotype; research; transcriptomics;     Show all 8 Subjects
Abstract:
... Shadoo and PrP belongs to the same protein family, whose biological function remains poorly understood. Previous experiments reported potential functional redundancies or antagonisms between these two proteins, depending on the tissue analysed. While knockdown experiments suggested the requirement of Shadoo in the absence of PrP during early mouse embryogenesis, knockout ones, on the contrary, hig ...
DOI:
10.1016/j.bbrc.2021.03.013

7. Stimulation of brain α7-nicotinic acetylcholine receptors suppresses the rat micturition through brain GABAergic receptors

Author:
Shimizu, Yohei; Shimizu, Takahiro; Zou, Suo; Ono, Hideaki; Hata, Yurika; Yamamoto, Masaki; Aratake, Takaaki; Shimizu, Shogo; Higashi, Youichirou; Karashima, Takashi; Saito, Motoaki
Source:
Biochemical and biophysical research communications 2021 v.548 pp. 84-90
ISSN:
0006-291X
Subject:
antagonists,   etc   ; acetylcholine; adrenalectomy; agonists; brain; epinephrine; males; norepinephrine; rats; research;     Show all 10 Subjects
Abstract:
... Brain nicotinic acetylcholine receptors (nAChRs) reportedly suppress the micturition, but the mechanisms responsible for this suppression remain unclear. We previously reported that intracerebroventricularly administered (±)-epibatidine (non-selective nAChR agonist) activated the sympatho-adrenomedullary system, which can affect the micturition. Therefore, we investigated (1) whether intracerebrov ...
DOI:
10.1016/j.bbrc.2021.02.051

8. Stereoselective benzilic acid rearrangements: new advances on an old story

Author:
Burke, Anthony J.; Moutayakine, Amina
Source:
Chemical communications 2021 v.57 no.21 pp. 2585-2590
ISSN:
1364-548X
Subject:
antagonists,   etc   ; Lewis acids; mineralocorticoid receptors; polyketides; stereoselective synthesis; stereoselectivity;     Show all 6 Subjects
Abstract:
... The benzilic acid rearrangement (BAR) is the oldest rearrangement on record. It is a powerful synthetic tool for accessing significant biologically active molecules. The reaction is both catalytic (generally Lewis acid) and stereoselective, recently the first catalytic asymmetric version was reported with astonshing results (ees of up to 97%) to give chiral tartronic esters. In this unique highlig ...
DOI:
10.1039/d0cc07905g

9. Linking hyperosmotic stress and apoptotic sensitivity

Author:
Stöhr, Daniela; Rehm, Markus
Source:
TheFEBS journal 2021 v.288 no.6 pp. 1800-1803
ISSN:
1742-464X
Subject:
antagonists,   etc   ; apoptosis; colorectal neoplasms; head and neck squamous cell carcinoma;     Show all 4 Subjects
Abstract:
... Cellular responses to hypertonic stress and how these are linked to the induction of or sensitisation to cell death signals are incompletely understood and rarely studied in cancer. Using cell lines derived from head and neck squamous cell carcinoma (HNSCC), Heimer et al. demonstrate that hypertonic environments neutralise the antiapoptotic Bcl‐2 family member Mcl‐1 by upregulating its antagonist ...
DOI:
10.1111/febs.15520

10. The VP3 Protein of Bluetongue Virus Associates with the MAVS Complex and Interferes with the RIG-I-Signaling Pathway

Author:
Pourcelot, Marie; Amaral Moraes, Rayane; Fablet, Aurore; Bréard, Emmanuel; Sailleau, Corinne; Viarouge, Cyril; Postic, Lydie; Zientara, Stéphan; Caignard, Grégory; Vitour, Damien
Source:
Viruses 2021 v.13 no.2
ISSN:
1999-4915
Subject:
antagonists,   etc   ; Bluetongue virus; Culicoides; arboviruses; coprecipitation; luciferase; mitochondria; structural proteins;     Show all 8 Subjects
Abstract:
... Bluetongue virus (BTV), an arbovirus transmitted by Culicoides biting midges, is a major concern of wild and domestic ruminants. While BTV induces type I interferon (alpha/beta interferon [IFN-α/β]) production in infected cells, several reports have described evasion strategies elaborated by this virus to dampen this intrinsic, innate response. In the present study, we suggest that BTV VP3 is a ne ...
DOI:
10.3390/v13020230

11. Trends, new insights and perspectives in the treatment of hospital effluents

Author:
Verlicchi, Paola
Source:
Current opinion in environmental science & health 2021 v.19 pp. 100217
ISSN:
2468-5844
Subject:
beta-adrenergic antagonists,   etc   ; analgesics; antibiotic resistance; drug therapy; hospitals; oxidation;     Show all 6 Subjects
Abstract:
... Recently, investigations of hospital effluent management and treatment have not only interested research groups with acquired experience in the field, but have also attracted the interest of new groups over the world. The most recent literature provides new insights into the occurrence of pharmaceuticals and other contaminants of emerging concern, pathogens, viruses, and antibiotic-resistant bacte ...
DOI:
10.1016/j.coesh.2020.10.005

12. The modulation of the spatial reference memory by the orexinergic system of the dorsal raphe nucleus

Author:
Khodabande, Fateme; Akbari, Esmaeil; Ardeshiri, Motahareh Rouhi
Source:
Life sciences 2021 v.265 pp. 118777
ISSN:
0024-3205
Subject:
antagonists,   etc   ; brain stem; hypothalamus; innervation; neuropeptides; pathophysiology; sleep; spatial memory;     Show all 8 Subjects
Abstract:
... The dorsal raphe nucleus (DRN) is a brainstem nucleus involved in the pathophysiology of the depression, through its serotoninergic innervation. Furthermore, depressive symptoms in patients are also associated with some memory and sleep complaints. Anatomical evidence confirmed the presence of projections from the lateral hypothalamus to serotonergic neurons of the dorsal raphe nucleus (DRN). Thes ...
DOI:
10.1016/j.lfs.2020.118777

13. Transcriptomic and proteomic analysis of the mechanisms involved in enhanced disease resistance of strawberries induced by Rhodotorula mucilaginosa cultured with chitosan

Author:
Gu, Ning; Zhang, Xiaoyun; Gu, Xiangyu; Zhao, Lina; Godana, Esa Abiso; Xu, Meiqiu; Zhang, Hongyin
Source:
Postharvest biology and technology 2021 v.172 pp. 111355
ISSN:
0925-5214
Subject:
antagonists; fungal antagonists,   etc   ; Rhodotorula rubra; biological control; cell walls; chitosan; disease resistance; gene expression; induced resistance; proteomics; signal transduction; strawberries; technology; transcriptomics; yeasts;     Show all 15 Subjects
Abstract:
... Rhodotorula mucilaginosa cultured in a medium amended with chitosan significantly enhances biological control efficacy against postharvest fungal diseases of strawberries. The molecular mechanisms underlying the enhanced disease resistance of strawberries, however, have not been explored. In this study, a transcriptomic and proteomic approach was used to analyze the induced resistance response in ...
DOI:
10.1016/j.postharvbio.2020.111355

14. 6-Nitrodopamine is released by human umbilical cord vessels and modulates vascular reactivity

Author:
Britto-Júnior, José; Coelho-Silva, Weverton C.; Murari, Guilherme Figueiredo; Serpellone Nash, Charles Elliot; Mónica, Fabíola Z.; Antunes, Edson; De Nucci, Gilberto
Source:
Life sciences 2021 v.276 pp. 119425
ISSN:
0024-3205
Subject:
antagonists,   etc   ; dopamine; endothelium; epinephrine; haloperidol; humans; nitric oxide; norepinephrine; tandem mass spectrometry; umbilical arteries; umbilical cord;     Show all 11 Subjects
Abstract:
... Human umbilical cord vessels (HUCV) release dopamine and nitric oxide (NO). This study aims to verify whether HUCV release nitrocatecholamines such as 6-nitrodopamine (6-ND).Liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) was used to identify 6-ND release from HUCV rings incubated in Krebs-Henseileit's solution. Vascular reactivity of HUCV rings was tested (with and without en ...
DOI:
10.1016/j.lfs.2021.119425

15. Role of changes in plasma prolactin concentrations on ram and buck sperm cryoresistance

Author:
Flores-Gil, V.N.; Toledano-Díaz, A.; Velázquez, R.; Oteo, M.; López-Sebastián, A.; Santiago-Moreno, J.
Source:
Domestic animal endocrinology 2021 v.76 pp. 106624
ISSN:
0739-7240
Subject:
antagonists,   etc   ; agonists; bromocriptine; dopamine; freeze-thaw cycles; head; prolactin; rams; secretion; spermatozoa; summer;     Show all 11 Subjects
Abstract:
... Seasonal endocrine changes may modify sperm cryoresistance in certain small ruminant species. The present work examines the effect of prolactin (PRL) on ram and buck sperm cryoresistance. A dopamine agonist (bromocriptine [BCR] 60 mg i.m. twice per week from May 15 to June 15, that is, approaching the summer solstice) or antagonist (sulpiride [SLP] 100 mg s.c. daily from December 15 to January 15, ...
DOI:
10.1016/j.domaniend.2021.106624

16. Himalayan bioactive molecules as potential entry inhibitors for the human immunodeficiency virus

Author:
Kumar Bhardwaj, Vijay; Purohit, Rituraj; Kumar, Sanjay
Source:
Food chemistry 2021 v.347 pp. 128932
ISSN:
0308-8146
Subject:
antagonists,   etc   ; Human immunodeficiency virus; active sites; chemokines; food chemistry; humans; phthalates; thermodynamics;     Show all 8 Subjects
Abstract:
... The human immunodeficiency virus interacts with the cluster of differentiation 4 receptors and one of the two chemokine receptors (CCR5 and CXCR4) to gain entry in human cells. Both the co-receptors are essential for viral entry, replication, and are considered critical targets for antiviral drugs. In this study, bioactive molecules from different Himalayan plants were screened considering their p ...
DOI:
10.1016/j.foodchem.2020.128932

17. Direct and maternal genetic components for body weight traits in Markhoz goat

Author:
Latifi, Meysam; Naderi, Yousef; Bohlouli, Mehdi; Sadeghi, Saadat
Source:
Tropical animal health and production 2021 v.53 no.2 pp. 234
ISSN:
0049-4747
Subject:
antagonists,   etc   ; Bayesian theory; animal health; body weight; covariance; goats; models; variance; Iran;     Show all 9 Subjects
Abstract:
... The aim of the study was to estimate the (co)variance components and genetic trends of direct and maternal genetic effects in Markhoz goat using random regression (RR) models. A total of 16,283 body weight trait records from birth to 400 days of age were obtained from 3476 Markhoz kids. Kids were from 223 bucks and 1217 does raised in the Markhoz goat breeding station in Sanandaj, Iran. The fixed ...
DOI:
10.1007/s11250-021-02614-5

18. Determination of finerenone – a novel, selective, nonsteroidal mineralocorticoid receptor antagonist – in human plasma by high-performance liquid chromatography-tandem mass spectrometry and its application to a pharmacokinetic study in venous and capillary human plasma

Author:
Rohde, Gabriele; Loewen, Stephanie; Heinig, Roland
Source:
Journal of chromatography 2021 v.1172 pp. 122643
ISSN:
1570-0232
Subject:
antagonists,   etc   ; acetonitrile; heparin; humans; ionization; isotope labeling; kidney diseases; lithium; mineralocorticoid receptors; pharmacokinetics; tandem mass spectrometry;     Show all 11 Subjects
Abstract:
... A straightforward and rapid high-performance liquid chromatography–tandem mass spectrometry (HPLC–MS/MS) assay allowing the sensitive and selective quantitation of finerenone (BAY 94–8862) in lithium heparin human plasma is described. Finerenone is a novel, selective, nonsteroidal mineralocorticoid receptor antagonist that is in phase III clinical trials for the treatment of chronic kidney disease ...
DOI:
10.1016/j.jchromb.2021.122643

19. Polycation fluorination improves intraperitoneal siRNA delivery in metastatic pancreatic cancer

Author:
Hang, Yu; Tang, Siyuan; Tang, Weimin; Větvička, David; Zhang, Chuhan; Xie, Ying; Yu, Fei; Yu, Ao; Sil, Diptesh; Li, Jing; Singh, Rakesh K.; Oupický, David
Source:
Journal of controlled release 2021 v.333 pp. 139-150
ISSN:
0168-3659
Subject:
antagonists,   etc   ; adenocarcinoma; cations; cholesterol; hydrophilicity; hydrophobicity; metastasis; models; mortality; pancreatic neoplasms; serum albumin; therapeutics; transfection;     Show all 13 Subjects
Abstract:
... Pancreatic ductal adenocarcinoma (PDAC) is a growing medical problem associated with extensive metastasis and high mortality. Intraperitoneal (IP) administration of therapeutics promises to help the treatment of cancers originated from organs in the peritoneal cavity. In this study, we evaluated how physicochemical properties of self-assembled polycation/siRNA nanoparticles affect their IP deliver ...
DOI:
10.1016/j.jconrel.2021.03.028

20. Neuroprotective effect of magnesium supplementation on cerebral ischemic diseases

Author:
Xu, Runnan; Wang, Liping; Sun, Liyuan; Dong, Jianghui
Source:
Life sciences 2021 v.272 pp. 119257
ISSN:
0024-3205
Subject:
antagonists,   etc   ; blood; calcium; death; encephalopathy; hypothermia; intravenous injection; ischemia; magnesium; mortality; neuroprotective effect; prognosis; stroke;     Show all 13 Subjects
Abstract:
... Ischemic encephalopathy is associated with a high mortality and rate of disability. The most common type of ischemic encephalopathy, ischemic stroke, is the second leading cause of death in the world. At present, the main treatment for ischemic stroke is to reopen blocked blood vessels. However, despite revascularization, many patients are not able to achieve good functional results. At the same t ...
DOI:
10.1016/j.lfs.2021.119257