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Pharmaceuticals

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https://www.readbyqxmd.com/read/28902172/behavioral-and-neurochemical-consequences-of-pentylenetetrazol-induced-kindling-in-young-and-middle-aged-rats
#1
Alexandre Ademar Hoeller, Cristiane Ribeiro de Carvalho, Pedro Leite Costa Franco, Douglas Affonso Formolo, Alexandre Kracker Imthon, Henrique Rodighero Dos Santos, Ingrid Eidt, Gabriel Roman Souza, Leandra Celso Constantino, Camila Leite Ferreira, Rui Daniel Prediger, Rodrigo Bainy Leal, Roger Walz
(1) Objectives: Epilepsy disorder is likely to increase with aging, leading to an increased incidence of comorbidities and mortality. In spite of that, there is a lack of information regarding this issue and little knowledge of cognitive and emotional responses in aging subjects following epileptogenesis. We investigated whether and how aging distress epilepsy-related behavioral and biochemical outcomes are associated with cognition and emotion. (2) Methods: Young and middle-aged Wistar rats (3 or 12 months old) were treated with pentylenetetrazol (PTZ, 35 mg/kg) and injected on alternated days for 20 (young rats) and 32 days (middle-aged rats)...
September 13, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28872590/synthesis-of-nitric-oxide-donors-derived-from-piloty-s-acid-and-study-of-their-effects-on-dopamine-secretion-from-pc12-cells
#2
Daniele Sanna, Gaia Rocchitta, Maria Serra, Marcello Abbondio, Pier Andrea Serra, Rossana Migheli, Lidia De Luca, Eugenio Garribba, Andrea Porcheddu
This study investigated the mechanisms and kinetics of nitric oxide (NO) generation by derivatives of Piloty's acid (NO-donors) under physiological conditions. In order to qualitatively and quantitatively measure NO release, electron paramagnetic resonance (EPR) was carried out with NO spin trapping. In addition, voltammetric techniques, including cyclic voltammetry and constant potential amperometry, were used to confirm NO release from Piloty's acid and its derivatives. The resulting data showed that Piloty's acid derivatives are able to release NO under physiological conditions...
September 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28820457/role-of-cyp2c9-cyp2c19-and-ephx-polymorphism-in-the-pharmacokinetic-of-phenytoin-a-study-on-uruguayan-caucasian-subjects
#3
Natalia Guevara, Cecilia Maldonado, Manuel Uría, Raquel González, Manuel Ibarra, Silvana Alvariza, Antonella Carozzi, Carlos Azambuja, Pietro Fagiolino, Marta Vázquez
Phenytoin (PHT) oxidative route leads to its main metabolite p-hydroxyphenytoin (p-HPPH), by means of CYP2C9 and CYP2C19. Formation of p-HPPH proceeds via a reactive arene-oxide intermediate. This intermediate can also be converted into PHT dihydrodiol by microsomal epoxide hydrolase (EPHX). The three enzymes are polymorphically expressed and the genetic variants are responsible for changes in the enzyme activity. In order to evaluate the effect that these polymorphisms have on PHT metabolism, PHT and p-HPPH plasma concentrations were measured and the genotype for the three enzymes was assessed in 50 Uruguayan epileptic patients...
August 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28809784/folate-receptor-positive-gynecological-cancer-cells-in-vitro-and-in-vivo-characterization
#4
Klaudia Siwowska, Raffaella M Schmid, Susan Cohrs, Roger Schibli, Cristina Müller
The folate receptor (FR) is expressed in a variety of gynecological cancer types. It has been widely used for tumor targeting with folic acid conjugates of diagnostic and therapeutic probes. The cervical KB tumor cells have evolved as the standard model for preclinical investigations of folate-based (radio) conjugates. In this study, a panel of FR-expressing human cancer cell lines-including cervical (HeLa, KB, KB-V1), ovarian (IGROV-1, SKOV-3, SKOV-3.ip), choriocarcinoma (JAR, BeWo) and endometrial (EFE-184) tumor cells-was investigated in vitro and for their ability to grow as xenografts in mice...
August 15, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28792472/glycosaminoglycan-interactions-with-chemokines-add-complexity-to-a-complex-system
#5
REVIEW
Amanda E I Proudfoot, Zoë Johnson, Pauline Bonvin, Tracy M Handel
Chemokines have two types of interactions that function cooperatively to control cell migration. Chemokine receptors on migrating cells integrate signals initiated upon chemokine binding to promote cell movement. Interactions with glycosaminoglycans (GAGs) localize chemokines on and near cell surfaces and the extracellular matrix to provide direction to the cell movement. The matrix of interacting chemokine-receptor partners has been known for some time, precise signaling and trafficking properties of many chemokine-receptor pairs have been characterized, and recent structural information has revealed atomic level detail on chemokine-receptor recognition and activation...
August 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28792452/complexes-of-oligoribonucleotides-with-d-mannitol-inhibit-hemagglutinin-glycan-interaction-and-suppress-influenza-a-virus-h1n1-a-fm-1-47-infectivity-in-vitro
#6
Nataliia Melnichuk, Larisa Semernikova, Zenoviy Tkachuk
The influenza virus hemagglutinin (HA) mediates both receptor (glycan) binding and membrane fusion for cell entry and has been the basis for subtyping influenza viruses. The oligoribonucleotides-d-mannitol (ORNs-d-M) complexes possess an anti-influenza activity in vitro and in vivo. In the present studies, we have found that ORNs-d-M interferes with hemagglutinin (HA)-glycan interaction and suppress viral infection in host cells. HA-glycan interactions were evaluated to indirectly quantify the amount of influenza virus titer by an agglutination assay...
August 9, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28763030/the-binding-effect-of-proteins-on-medications-and-its-impact-on-electrochemical-sensing-antipsychotic-clozapine-as-a-case-study
#7
George E Banis, Thomas Winkler, Patricia Barton, Sheryl E Chocron, Eunkyoung Kim, Deanna L Kelly, Gregory F Payne, Hadar Ben-Yoav, Reza Ghodssi
Clozapine (CLZ), a dibenzodiazepine, is demonstrated as the optimal antipsychotic for patients suffering from treatment-resistant schizophrenia. Like many other drugs, understanding the concentration of CLZ in a patient's blood is critical for managing the patients' symptoms, side effects, and overall treatment efficacy. To that end, various electrochemical techniques have been adapted due to their capabilities in concentration-dependent sensing. An open question associated with electrochemical CLZ monitoring is whether drug-protein complexes (i...
August 1, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28758969/assessment-of-bone-metastases-in-patients-with-prostate-cancer-a-comparison-between-99m-tc-bone-scintigraphy-and-68-ga-ga-psma-pet-ct
#8
Lena Thomas, Caroline Balmus, Hojjat Ahmadzadehfar, Markus Essler, Holger Strunk, Ralph A Bundschuh
PURPOSE: Bone scintigraphy is the standard of reference in bone metastases in prostate cancer patients. However, new radiotracers employed in prostate-specific membrane antigen (PSMA)-ligands has led to the growing importance of PET/CT as diagnostic tool. The aim of our study was to investigate the difference between bone scan and PSMA-PET/CT for the detection of bone metastases in prostate cancer. METHODS: Thirty patients with bone metastases originating from prostate cancer were examined by (99m)Tc-MDP bone scan and (68)Ga-PSMA-PET/CT within an average of 21 days...
July 31, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28758946/hippocampal-proteome-of-rats-subjected-to-the-li-pilocarpine-epilepsy-model-and-the-effect-of-carisbamate-treatment
#9
José Eduardo Marques-Carneiro, Daniele Suzete Persike, Julia Julie Litzahn, Jean-Christophe Cassel, Astrid Nehlig, Maria José da Silva Fernandes
In adult rats, the administration of lithium-pilocarpine (LiPilo) reproduces most clinical and neuropathological features of human temporal lobe epilepsy (TLE). Carisbamate (CRS) possesses the property of modifying epileptogenesis in this model. Indeed, about 50% of rats subjected to LiPilo status epilepticus (SE) develop non-convulsive seizures (NCS) instead of motor seizures when treated with CRS. However, the mechanisms underlying these effects remain unknown. The aim of this study was to perform a proteomic analysis in the hippocampus of rats receiving LiPilo and developing motor seizures or NCS following CRS treatment...
July 30, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28737679/modernization-of-enoxaparin-molecular-weight-determination-using-homogeneous-standards
#10
Katelyn M Arnold, Stephen J Capuzzi, Yongmei Xu, Eugene N Muratov, Kevin Carrick, Anita Y Szajek, Alexander Tropsha, Jian Liu
Enoxaparin is a low-molecular weight heparin used to treat thrombotic disorders. Following the fatal contamination of the heparin supply chain in 2007-2008, the U.S. Pharmacopeia (USP) and U.S. Food and Drug Administration (FDA) have worked extensively to modernize the unfractionated heparin and enoxaparin monographs. As a result, the determination of molecular weight (MW) has been added to the monograph as a measure to strengthen the quality testing and to increase the protection of the global supply of this life-saving drug...
July 22, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28726739/5-aza-2-2-difluroro-deoxycytidine-nuc013-a-novel-nucleoside-dna-methyl-transferase-inhibitor-and-ribonucleotide-reductase-inhibitor-for-the-treatment-of-cancer
#11
Richard Daifuku, Zhenbo Hu, Yogen Saunthararajah
Tumor suppressor genes can be silenced genetically as well as epigenetically. One approach to reversing epigenetic suppression of tumor suppressor genes is to inhibit DNA methyl transferase. 5-aza-2',2'-diflurorodeoxycytidine (NUC013) is a novel DNA methyl transferase and ribonucleotide reductase inhibitor that is a more potent inhibitor of growth than decitabine in the NCI 60 cancer cell line panel. NUC013 is more active than decitabine against p53-null/mutant cancer cell lines (p = 0.027) but is even more so against p53 wild-type (WT) cell lines (p = 0...
July 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28684697/transient-receptor-potential-trp-channels-in-drug-discovery-old-concepts-new-thoughts
#12
EDITORIAL
Susan Huang, Arpad Szallasi
2017 marks the 20th anniversary of the molecular cloning by David Julius and colleagues (1997) of the long sought-after capsaicin receptor, now known as TRPV1 (Transient Receptor Potential Vanilloid 1) [1]. This seminal discovery has opened up a "hot" new field of basic research and launched drug discovery efforts into the large family (by the latest count 28 mammalian members, 27 in humans) of TRP ion channels [2]. Indeed, it took less than a decade for the first potent, small molecule TRPV1 antagonists to enter phase 1 clinical trials [3]...
July 6, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28684694/neuroprotective-effects-of-%C3%AE-caryophyllene-against-dopaminergic-neuron-injury-in-a-murine-model-of-parkinson-s-disease-induced-by-mptp
#13
Juan M Viveros-Paredes, Rocio E González-Castañeda, Juerg Gertsch, Veronica Chaparro-Huerta, Rocio I López-Roa, Eduardo Vázquez-Valls, Carlos Beas-Zarate, Antoni Camins-Espuny, Mario E Flores-Soto
Parkinson's disease (PD) is one of the most common neurodegenerative disorders and is characterized by the loss of dopaminergic neurons in the substantia nigra (SN). Although the causes of PD are not understood, evidence suggests that its pathogenesis is associated with oxidative stress and inflammation. Recent studies have suggested a protective role of the cannabinoid signalling system in PD. β-caryophyllene (BCP) is a natural bicyclic sesquiterpene that is an agonist of the cannabinoid type 2 receptor (CB2R)...
July 6, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28684690/pharmaceuticals-impact-factor-or-citescore%C3%A2
#14
EDITORIAL
Jean Jacques Vanden Eynde
n/a.
July 6, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28678209/nanofiber-scaffolds-as-drug-delivery-systems-to-bridge-spinal-cord-injury
#15
REVIEW
Angela Faccendini, Barbara Vigani, Silvia Rossi, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Marcella Caramella, Franca Ferrari
The complex pathophysiology of spinal cord injury (SCI) may explain the current lack of an effective therapeutic approach for the regeneration of damaged neuronal cells and the recovery of motor functions. A primary mechanical injury in the spinal cord triggers a cascade of secondary events, which are involved in SCI instauration and progression. The aim of the present review is to provide an overview of the therapeutic neuro-protective and neuro-regenerative approaches, which involve the use of nanofibers as local drug delivery systems...
July 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28678205/synthesis-and-antiproliferative-activity-of-novel-heterocyclic-indole-trimethoxyphenyl-conjugates
#16
Michael M Cahill, Kevin D O'Shea, Larry T Pierce, Hannah J Winfield, Kevin S Eccles, Simon E Lawrence, Florence O McCarthy
The synthesis and biological evaluation of a series of novel heterocyclic indole derivatives is described. The consolidation of the combretastatin and bisindolylmaleimide templates towards the inclusion of a novel heterocyclic ring proffered a versatile pharmacophore with which to pursue chemical diversification. Given literature precedent, maleimide was initially investigated in this role and the bioactivity assessed by measurement of NCI-60 cell panel growth. Subsequently, a range of 5-aminopyrazoles was designed and developed to explore the specific effect of heterocycle hydrogen bonding on cell growth...
July 5, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28671597/precipitation-and-neutralization-of-heparin-from-different-sources-by-protamine-sulfate
#17
John Hogwood, Barbara Mulloy, Elaine Gray
Current therapeutic unfractionated heparin available in Europe and US is of porcine mucosal origin. There is now interest, specifically in the US, to use bovine mucosa as an additional source for the production of heparin. The anticoagulant action of heparin can be neutralized by protamine sulfate, and in this study the ability of protamine to bind and neutralize the anticoagulant activities of heparin from porcine mucosa, bovine mucosa and bovine lung were assessed. Protamine sulfate was able to bind and precipitate similar amounts of heparins from different sources on a mass basis...
July 2, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28672834/individual-and-combined-effects-of-engineered-peptides-and-antibiotics-on-pseudomonas-aeruginosa-biofilms
#18
Biswajit Mishra, Guangshun Wang
Pseudomonas aeruginosa is involved in a variety of difficult-to-treat infections frequently due to biofilm formation. To identify useful antibiofilm strategies, this article evaluated efficacy of two newly engineered cationic antimicrobial peptides (17BIPHE2 and DASamP2), traditional antibiotics, and their combinations against biofilms at different stages. 17BIPHE2 is designed based on the 3D structure of human cathelicidin LL-37 and DASamP2 is derived from database screening. While both peptides show effects on bacterial adhesion, biofilm formation, and preformed biofilms, select antibiotics only inhibit biofilm formation, probably due to direct bacterial killing...
June 25, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28635674/exploring-wound-healing-genomic-machinery-with-a-network-based-approach
#19
Francesca Vitali, Simone Marini, Martina Balli, Hanne Grosemans, Maurilio Sampaolesi, Yves A Lussier, Maria Gabriella Cusella De Angelis, Riccardo Bellazzi
The molecular mechanisms underlying tissue regeneration and wound healing are still poorly understood despite their importance. In this paper we develop a bioinformatics approach, combining biology and network theory to drive experiments for better understanding the genetic underpinnings of wound healing mechanisms and for selecting potential drug targets. We start by selecting literature-relevant genes in murine wound healing, and inferring from them a Protein-Protein Interaction (PPI) network. Then, we analyze the network to rank wound healing-related genes according to their topological properties...
June 21, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28635637/a-short-term-biological-indicator-for-long-term-kidney-damage-after-radionuclide-therapy-in-mice
#20
Giovanni Pellegrini, Klaudia Siwowska, Stephanie Haller, Daniel J Antoine, Roger Schibli, Anja Kipar, Cristina Müller
Folate receptor (FR)-targeted radionuclide therapy using folate radioconjugates is of interest due to the expression of the FR in a variety of tumor types. The high renal accumulation of radiofolates presents, however, a risk of radionephropathy. A potential option to address this challenge would be to use radioprotectants, such as amifostine. Methods for early detection of kidney damage that-in this case-cannot be predicted based on dose estimations, would facilitate the development of novel therapies. The aim of this study was, therefore, to assess potentially changing levels of plasma and urine biomarkers and to determine DNA damage at an early stage after radiofolate application...
June 21, 2017: Pharmaceuticals
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