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https://www.readbyqxmd.com/read/28110124/monoanionic-99m-tc-tricarbonyl-aminopolycarboxylate-complexes-with-uncharged-pendant-groups-radiosynthesis-and-evaluation-as-potential-renal-tubular-tracers
#1
Malgorzata Lipowska, Jeffrey Klenc, Nashwa Jarkas, Luigi G Marzilli, Andrew T Taylor
INTRODUCTION: (99m)Tc(CO)3-nitrilotriacetic acid, (99m)Tc(CO)3(NTA), is a new renal tubular agent with pharmacokinetic properties comparable to those of (131)I-OIH but the clearance of (99m)Tc(CO)3(NTA) and (131)I-OIH is still less than the clearance of PAH, the gold standard for the measurement of effective renal plasma flow. At physiological pH, dianionic (99m)Tc(CO)3(NTA) has a mononegative inner metal-coordination sphere and a mononegative uncoordinated carboxyl group. To evaluate alternate synthetic approaches, we assessed the importance of an uncoordinated carboxyl group, long considered essential for tubular transport, by evaluating the pharmacokinetics of three analogs with the (99m)Tc(CO)3(NTA) metal-coordination sphere but with uncharged pendant groups...
December 27, 2016: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28109947/design-and-synthesis-of-benzodiazepine-analogs-as-isoform-selective-human-lysine-deacetylase-inhibitors
#2
D Rajasekhar Reddy, Flavio Ballante, Nancy J Zhou, Garland R Marshall
A comprehensive investigation was performed to identify new benzodiazepine (BZD) derivatives as potent and selective human lysine deacetylase inhibitors (hKDACis). A total of 108 BZD compounds were designed, synthesized and from that 104 compounds were biologically evaluated against human lysine deacetylases (hKDACs) 1, 3 and 8 (class I) and 6 (class IIb). The most active compounds showed mid-nanomolar potencies against hKDACs 1, 3 and 6 and micromolar activity against hKDAC8, while a promising compound (6q) showed selectivity towards hKDAC3 among the different enzyme isoforms...
December 18, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28109826/biological-relevance-of-effects-following-chronic-administration-of-octamethylcyclotetrasiloxane-d4-in-fischer-344-rats
#3
Wolfgang Dekant, Anthony R Scialli, Kathy Plotzke, James E Klaunig
Octamethylcyclotetrasiloxane (D4) is a cyclic siloxane primarily used as a monomer or intermediate in the production of silicone polymers resulting in potential exposure of workers, and potential low level inhalation or dermal exposure for consumers and the general public. Following a two-year inhalation toxicity study with D4 in rats, increases in uterine endometrial cystic hyperplasia and adenomas were observed at the highest concentration of D4 administered (700ppm). No other neoplasms were increased with D4 treatment...
January 18, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28108939/exploration-of-sar-for-novel-2-benzylbenzimidazole-analogs-as-inhibitor-of-transcription-factor-nf-%C3%AE%C2%BAb
#4
PullaReddy Boggu, Eeda Venkateswararao, Manoj Manickam, Youngsoo Kim, Sang-Hun Jung
A novel series of 2-benzylbenzimidazole analogs was designed, synthesized and investigated for their in vitro activities against LPS induced NF-κB inhibition in RAW 264.7 cells using the SEAP assay. Among them, 4-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6e, >100% inhibition at 30 μM, IC50 = 3.0 μM), 4-((5-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6j, 96% inhibition at 30 μM, IC50 = 4.0 μM) and 2-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6k, 95% inhibition at 30 μM, IC50 = 5...
January 20, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28108668/ultraviolet-and-yellow-reflectance-but-not-fluorescence-is-important-for-visual-discrimination-of-conspecifics-by-heliconius-erato
#5
Susan D Finkbeiner, Dmitry A Fishman, Daniel Osorio, Adriana D Briscoe
Toxic Heliconius butterflies have yellow hindwing bars that - unlike their closest relatives - reflect ultraviolet (UV) and long wavelength light, and also fluoresce. The pigment in the yellow scales is 3-hydroxy-DL-kynurenine (3-OHK), found also in the hair and scales of a variety of animals. In other butterflies like pierids with color schemes characterized by independent sources of variation in UV and human-visible yellow/orange, behavioral experiments have generally implicated the UV component as most relevant to mate choice...
January 20, 2017: Journal of Experimental Biology
https://www.readbyqxmd.com/read/28108651/roflumilast-and-aquaporin-2-regulation-in-rat-renal-inner-medullary-collecting-duct
#6
Ezigbobiara N Umejiego, Yanhua Wang, Mark A Knepper, Chung-Lin Chou
Roflumilast is a cyclic nucleotide phosphodiesterase inhibitor that is FDA-approved for treatment of chronic obstructive pulmonary disease. With a view toward possible use for treatment of patients with X-linked nephrogenic diabetes insipidus (NDI) due to hemizygous mutations in the V2 vasopressin receptor, this study sought to determine the effect of roflumilast on aquaporin-2 (AQP2) phosphorylation, AQP2 trafficking, and water permeability in the rat inner medullary collecting duct (IMCD). In the presence of the vasopressin analog dDAVP (0...
January 2017: Physiological Reports
https://www.readbyqxmd.com/read/28108318/response-inhibition-set-shifting-and-complex-executive-function-in-patients-with-chronic-lower-back-pain
#7
Rytis Masiliūnas, Dalia Vitkutė, Edgaras Stankevičius, Vaidas Matijošaitis, Kęstutis Petrikonis
OBJECTIVE: The aim of our study was to evaluate how response inhibition, set shifting, and complex executive function (represented by risky decision-making) are altered in chronic lower back pain patients. MATERIALS AND METHODS: A total of 29 patients with chronic lower back pain (CLBP >6 months) aged 49-69 years and 30 healthy volunteers matched for age, gender, and education were enrolled in a case-control study. The study was conducted in the Departments of Neurology and Neurosurgery of Panevėžys Regional Hospital, Lithuania...
January 2, 2017: Medicina
https://www.readbyqxmd.com/read/28108278/comparison-of-the-redox-chemistry-of-sulfur-and-selenium-containing-analogs-of-uracil
#8
N Connor Payne, Andrew Geissler, Aileen Button, Alexandru R Sasuclark, Alayne L Schroll, Erik L Ruggles, Vadim N Gladyshev, Robert J Hondal
Selenium is present in proteins in the form of selenocysteine, where this amino acid serves catalytic oxidoreductase functions. The use of selenocysteine in nature is strongly associated with redox catalysis. However, selenium is also found in a 2-selenouridine moiety at the wobble position of tRNA(Glu), tRNA(Gln) and tRNA(Lys). It is thought that the modifications of the wobble position of the tRNA improves the selectivity of the codon-anticodon pair as a result of the physico-chemical changes that result from substitution of sulfur and selenium for oxygen...
January 17, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28108224/effectiveness-of-monotherapy-and-combined-therapy-with-calcitonin-and-minodronic-acid-hydrate-a-bisphosphonate-for-early-treatment-in-patients-with-new-vertebral-fractures-an-open-label-randomized-parallel-group-study
#9
Shinya Tanaka, Akira Yoshida, Shinjiro Kono, Manabu Ito
BACKGROUND: Evidence related to the effectiveness of combination drug therapy for the treatment of osteoporosis is currently considered insufficient. Therefore, this study was performed to clarify the effects of monotherapy, and combination therapy, with a bisphosphonate (minodronic acid hydrate), a bone resorption inhibitor, and calcitonin (elcatonin), which is effective for the alleviation of pain due to vertebral fractures in osteoporotic patients. METHODS: Study participants comprised of 51 female subjects with post-menopausal osteoporosis, whose main complaint was acute lower back pain caused by vertebral fractures...
January 18, 2017: Journal of Orthopaedic Science: Official Journal of the Japanese Orthopaedic Association
https://www.readbyqxmd.com/read/28108028/comparison-of-ca-2-puffs-evoked-by-extracellular-agonists-and-photoreleased-ip3
#10
REVIEW
Jeffrey T Lock, Ian F Smith, Ian Parker
The inositol trisphosphate (IP3) signaling pathway evokes local Ca(2+) signals (Ca(2+) puffs) that arise from the concerted openings of clustered IP3 receptor/channels in the ER membrane. Physiological activation is triggered by binding of agonists to G-protein-coupled receptors (GPCRs) on the cell surface, leading to cleavage of phosphatidyl inositol bisphosphate and release of IP3 into the cytosol. Photorelease of IP3 from a caged precursor provides a convenient and widely employed means to study the final stage of IP3-mediated Ca(2+) liberation, bypassing upstream signaling events to enable more precise control of the timing and relative concentration of cytosolic IP3...
December 5, 2016: Cell Calcium
https://www.readbyqxmd.com/read/28107938/nucleotide-base-analog-pyrrolo-deoxycytidine-as-fluorescent-probe-signal-for-enzyme-free-and-signal-amplified-nucleic-acids-detection
#11
Zhijuan Duan, Zhuo Li, Jianyuan Dai, Hongfei He, Dan Xiao
In the present work, an enzyme-free and signal amplified nucleic acids detection method based on the fluorescent nucleotide base analog pyrrolo-deoxycytidine (P-dC) and catalyzed hairpin assembly (CHA) has been developed. In the CHA signal amplification system, two hairpin auxiliary probes, H1 and H2, which containing a fluorescent P-dC at the end of the stem, respectively, were used as the fluorescent probes. The fluorescence of P-dC in H1 and H2 was quenched owing to the stacking interaction among the bases in the stem...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28107687/do-recreational-cannabis-users-unlicensed-and-licensed-medical-cannabis-users-form-distinct-groups
#12
Sharon R Sznitman
BACKGROUND: This study aims to gain a more nuanced perspective on the differences between recreationally and medically motivated cannabis use by distinguishing between people who use cannabis for recreational purposes, unlicensed and licensed medical users. METHODS: Data collection was conducted online from a convenience sample of 1479 Israeli cannabis users. Multinomial regression analysis compared unlicensed medical users (38%) with recreational (42%) and licensed medical (5...
January 17, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28107509/development-of-combining-of-human-bronchial-mucosa-models-with-xposeali%C3%A2-for-exposure-of-air-pollution-nanoparticles
#13
Jie Ji, Anna Hedelin, Maria Malmlöf, Vadim Kessler, Gulaim Seisenbaeva, Per Gerde, Lena Palmberg
BACKGROUND: Exposure to agents via inhalation is of great concerns both in workplace environment and in the daily contact with particles in the ambient air. Reliable human airway exposure systems will most likely replace animal experiment in future toxicity assessment studies of inhaled agents. METHODS: In this study, we successfully established a combination of an exposure system (XposeALI) with 3D models mimicking both healthy and chronic bronchitis-like mucosa by co-culturing human primary bronchial epithelial cells (PBEC) and fibroblast at air-liquid interface (ALI)...
2017: PloS One
https://www.readbyqxmd.com/read/28107377/hbeag-seroconversion-in-hbeag-positive-chronic-hepatitis-b-patients-receiving-long-term-nucleos-t-ide-analog-treatment-a-systematic-review-and-network-meta-analysis
#14
Tongjing Xing, Hongtao Xu, Lin Cao, Maocong Ye
BACKGROUND: HBeAg seroconversion is an important intermediate outcome in HBeAg-positive chronic hepatitis B (CHB) patients. This study aimed to compare the effect of nucleos(t)ide analogs (NAs) on HBeAg seroconversion in treating CHB with lamivudine, adefovir, telbivudine, entecavir, and tenofovir. METHODS: Network meta-analysis of NA treatment-induced HBeAg seroconversion after 1-2 years of treatment was performed. In addition, NA treatment-induced HBeAg seroconversion after 3-5 years of treatment was systematically evaluated...
2017: PloS One
https://www.readbyqxmd.com/read/28107217/reliability-and-validity-of-athletes-disability-index-questionnaire
#15
Pardis Noormohammadpour, Alireza Hosseini Khezri, Farzin Farahbakhsh, Mohammad Ali Mansournia, Matthew Smuck, Ramin Kordi
OBJECTIVE: The purpose of this study was to evaluate validity and reliability of a new proposed questionnaire for assessment of functional disability in athletes with low back pain (LBP). DESIGN: Validity and reliability study. SETTING: Elite athletes participating in different fields of sports. PARTICIPANTS: Participants were 165 male and female athletes (between 12 and 50 years old) with LBP. INTERVENTIONS: Athlete Disability Index (ADI) Questionnaire which is developed by the authors for assessing LBP-related disability in athletes, Oswestry Disability Index (ODI), and the Roland-Morris Disability Questionnaire (RDQ)...
January 17, 2017: Clinical Journal of Sport Medicine: Official Journal of the Canadian Academy of Sport Medicine
https://www.readbyqxmd.com/read/28107018/structure-wettability-and-thermal-stability-of-organic-thin-films-on-gold-generated-from-the-molecular-self-assembly-of-unsymmetrical-oligo-ethylene-glycol-spiroalkanedithiols
#16
Pawilai Chinwangso, Han Ju Lee, Andrew C Jamison, Maria D Marquez, Chul Soon Park, T Randall Lee
Organic thin-films on gold were prepared from a set of new, custom-designed bidentate alkanethiols possessing a mixture of normal alkane and methoxy-terminated tri(ethyleneglycol) chains. The new unsymmetrical spiroalkanedithiol adsorbates were of the form [CH3O(CH2CH2O)3(CH2)5]-[CH3(CH2)n+1]C[CH2SH]2 where n = 3 and 14; designated EG3C7-C7 and EG3C7-C18, respectively. Their corresponding self-assembled monolayers (SAMs) on gold were characterized and compared with monothiol SAMs derived from an analogous normal alkanethiol (C18SH) and an alkanethiol terminated with an oligo(ethylene glycol) (OEG) moiety (i...
January 20, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28106986/microwave-assisted-synthesis-of-nacopo4-red-phase-and-initial-characterization-as-high-voltage-cathode-for-sodium-ion-batteries
#17
Arturo Gutierrez, Soojeong Kim, Timothy T Fister, Christopher S Johnson
Transition metal-containing polyanion compounds are attractive for use as cathode materials in sodium-ion batteries (SIB) because they possess elevated higher intrinsic electrochemical potentials versus oxide analogs given the same M(n+/(n+1)+) redox couple, which leads to higher energy densities. NaMPO4 (M = transition metal) compounds have a driving force to form into the electrochemically inactive maricite phase when using conventional methods. Herein we report on the synthesis of a NaCoPO4 (NCP) polymorph ("Red"-phase) by a microwave-assisted solvothermal process at 200 °C using tetraethylene glycol as the solvent...
January 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28106956/comparisons-of-weight-changes-between-sglt2-inhibitors-treatment-and-glp-1-analogs-treatment-in-type-2-diabetes-patients-a-meta-analysis
#18
REVIEW
Xiaoling Cai, Liwei Ji, Yifei Chen, Wenjia Yang, Lingli Zhou, Xueyao Han, Simin Zhang, Linong Ji
To evaluate the efficacy of weight changes from baseline of the SGLT2 inhibitors treatment and GLP-1 analogs treatment after comparisons with placebo in type 2 diabetes patients and the associated factors MATERIALS AND METHODS: Studies were searched from when recording began, June 2004, until June 2015, and re-searched on July 2016, and placebo-controlled randomized trials in type 2 diabetes patients with a study length ≥12 weeks were included RESULTS: A total of 97 RCTs were included. Compared with placebo, treatment with SGLT2 inhibitors was associated with a significant greater decrease in weight change from baseline, (weighted mean differences (WMD), -2...
January 20, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28106785/ketamine-analog-methoxetamine-induced-inflammation-and-dysfunction-of-bladder-in-rats
#19
Qiang Wang, Qinghui Wu, Junpeng Wang, Yang Chen, Guihao Zhang, Jiawei Chen, Jie Zhao, Peng Wu
The novel synthetic psychoactive ketamine analog methoxetamine is reportedly being used for recreational purposes. As ketamine use can result in urinary dysfunction, we conducted the present study to investigate how methoxetamine affects the bladder. A cystometry investigation showed that female Sprague-Dawley rats experienced increased micturition frequency bladder dysfunction after receiving a daily intraperitoneal injection of 30 mg/kg methoxetamine or ketamine for periods of 4 or 12 weeks. Histologic examinations of rat bladder tissue revealed damaged urothelium barriers, as well as evidence of inflammatory cell infiltration and matrix deposition...
January 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28106652/prospective-outcomes-of-a-pelvic-floor-rehabilitation-program-including-vaginal-electrogalvanic-stimulation-for-urinary-defecatory-and-pelvic-pain-symptoms
#20
Jennifer J Schmitt, Ruchira Singh, Amy L Weaver, Kristin C Mara, Randina R Harvey-Springer, Felecia R Fick, John A Occhino
OBJECTIVES: This study evaluated our experience after implementing a pelvic floor rehabilitation program including behavioral modification, biofeedback, and vaginal electrogalvanic stimulation (EGS). METHODS: This prospective cohort study evaluated outcomes of patients with pelvic floor dysfunction (urinary or defecatory dysfunction, pelvic pain/dyspareunia) who underwent pelvic floor rehabilitation. Patients received 4 to 7 sessions (1 every 2 weeks) including biofeedback and concluded with 30 minutes of vaginal EGS...
January 18, 2017: Female Pelvic Medicine & Reconstructive Surgery
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