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Pharmacology Research & Perspectives

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https://www.readbyqxmd.com/read/30263124/real-time-examination-of-camp-activity-at-relaxin-family-peptide-receptors-using-a-bret-based-biosensor
#1
Adam L Valkovic, Miranda B Leckey, Alice R Whitehead, Mohammed A Hossain, Asuka Inoue, Martina Kocan, Ross A D Bathgate
Relaxin family peptide (RXFPs) 1-4 receptors modulate the activity of cyclic adenosine monophosphate (cAMP) to produce a range of physiological functions. RXFP1 and RXFP2 increase cAMP via Gαs , whereas RXFP3 and RXFP4 inhibit cAMP via Gαi/o . RXFP1 also shows a delayed increase in cAMP downstream of Gαi3 . In this study we have assessed whether the bioluminescence resonance energy transfer (BRET)-based biosensor CAMYEL (cAMP sensor using YFP-Epac-Rluc), which allows real-time measurement of cAMP activity in live cells, will aid in understanding ligand- and cell-specific RXFP signaling...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30258633/methods-for-the-assessment-of-selection-bias-in-drug-safety-during-pregnancy-studies-using-electronic-medical-data
#2
Mireille E Schnitzer, Lucie Blais
Electronic health data are routinely used for population drug studies. Due to the ethical dilemma in carrying out experimental drug studies on pregnant women, the effects of medication usage during pregnancy on fetal and maternal outcomes are largely evaluated using this data collection medium. One major limitation in this type of study is the delayed inclusion of pregnancies in the cohort. For example, in the province of Quebec, Canada, a major pregnancy cohort only captured pregnancies after 20 weeks gestation...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30239534/corrigendum
#3
(no author information available yet)
[This corrects the article DOI: 10.1002/prp2.2.70.].
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30237892/14-15-epoxyeicosatrienoic-acid-produced-by-cytochrome-p450s-enhances-neurite-outgrowth-of-pc12-and-rat-hippocampal-neuronal-cells
#4
Ami Oguro, Takumi Inoue, Suguru N Kudoh, Susumu Imaoka
Polyunsaturated fatty acids, such as arachidonic acid, are accumulated in brain and induce neuronal differentiation. Arachidonic acid is metabolized to epoxyeicosatrienoic acids (EETs) and hydroxyeicosatetraenoic acids (HETEs) by cytochrome P450s. In this study, we found that 14,15-EET and 20-HETE-enhanced NGF-induced rat pheochromocytoma PC12 cell neurite outgrowth even at the concentration of 100 nmol L-1 . LC-MS analysis revealed that 14,15-EET was effectively produced from arachidonic acid by rat CYP2C11, 2C13, and 2C23, and these P450s were expressed in PC12 cells...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30221006/pharmacokinetics-of-metformin-in-patients-with-chronic-kidney-disease-stage-4-and-metformin-na%C3%A3-ve-type-2-diabetes
#5
Ajith M Dissanayake, Mark C Wheldon, Christopher J Hood
The pharmacokinetics of metformin therapy in patients with chronic kidney disease stage 4 (CKD-4) were studied using data from the largest Phase I consecutive cohort trial yet performed in this population. Eighteen metformin-naïve men and women with Type 2 Diabetes and creatinine clearance (CrCl) in the range 18-49 mL/min (eGFR 15-29 mL/min/1.73 m2 ) were allocated to daily immediate-release metformin of 250 mg, 500 mg, or 1000 mg. A first-dose profile and trough concentrations for 4 weeks were taken on all patients...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30214813/elevated-4%C3%AE-hydroxycholesterol-cholesterol-ratio-in-anorexia-nervosa-patients
#6
Kristine Hole, Petra L Heiberg, Caroline Gjestad, Lise L Mehus, Øyvind Rø, Espen Molden
Recent studies have shown that the cytochrome P450 (CYP) 3A phenotype marker 4β-hydroxycholesterol/cholesterol (4βOHC/C) ratio is negatively correlated with body weight in healthy volunteers, and that obese patients have lower 4βOHC levels than healthy controls. However, 4βOHC/C ratio in underweight patients has yet to be reported. The aim of this study was to examine potential differences in CYP3A activity between underweight patients with anorexia nervosa and normal-weight volunteers by measuring plasma 4βOHC/C ratio...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30151213/small-molecule-neuromedin-u-receptor-2-agonists-suppress-food-intake-and-decrease-visceral-fat-in-animal-models
#7
Catherine M Sampson, James M Kasper, Daniel E Felsing, Sweta R Raval, Na Ye, Pingyuan Wang, Igor Patrikeev, Erik Rytting, Jia Zhou, John A Allen, Jonathan D Hommel
Obesity is a growing public health concern, with 37.5% of the adult population in need of therapeutics that are more efficacious with a better side effect profile. An innovative target in this regard is neuromedin U, a neuropeptide shown to suppress food intake and attenuate weight gain in animal models. These effects of neuromedin U on feeding behavior are thought to be related to agonism at the centrally expressed neuromedin U receptor 2 (NMUR2). As peptides present unique challenges that limit their therapeutic potential, the discovery of small-molecule NMUR2 agonists is needed to validate the targets therapeutic value, but to date, none have been evaluated in any animal model of disease...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30151212/tolerability-pharmacokinetics-and-pharmacodynamics-of-mirogabalin-in-healthy-subjects-results-from-phase-1-studies
#8
Karen Brown, Jeanne Mendell, Shoichi Ohwada, Ching Hsu, Ling He, Vance Warren, Victor Dishy, Hamim Zahir
Three phase 1 pharmacokinetic (PK)/pharmacodynamics (PD) studies were conducted in healthy men and women to further characterize the safety, tolerability, and PK/PD of mirogabalin administration with or without food and to guide the dose selection and regimen for phase 2 and 3 clinical development. The 3 studies included 2 randomized, double-blind, placebo-controlled, single- and multiple-ascending-dose studies, and 1 open-label, crossover study to evaluate the PK of mirogabalin administered under fasting and fed (high-fat meal) conditions...
October 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30156005/vancomycin-therapeutic-drug-monitoring-and-population-pharmacokinetic-models-in-special-patient-subpopulations
#9
Joaquim F Monteiro, Siomara R Hahn, Jorge Gonçalves, Paula Fresco
Vancomycin is a fundamental antibiotic in the management of severe Gram-positive infections. Inappropriate vancomycin dosing is associated with therapeutic failure, bacterial resistance and toxicity. Therapeutic drug monitoring (TDM) is acknowledged as an important part of the vancomycin therapy management, at least in specific patient subpopulations, but implementation in clinical practice has been difficult because there are no consensus and agglutinator documents. The aims of the present work are to present an overview of the current knowledge on vancomycin TDM and population pharmacokinetic (PPK) models relevant to specific patient subpopulations...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30073087/serious-hepatotoxicity-following-use-of-isoniazid-preventive-therapy-in-hiv-patients-in-eritrea
#10
Mulugeta Russom, Merhawi Debesai, Mehari Zeregabr, Araia Berhane, Theodros Tekeste, Teklezghi Teklesenbet
WHO information note indicates that isoniazid preventive therapy (IPT) is generally safe with little risk of hepatotoxicity. However, when the policy of IPT for HIV patients was introduced in Eritrea, frequent IPT-associated hepatotoxicity and fatality have been reported to the Pharmacovigilance Centre. The aim of the study is to assess the causal association of IPT and hepatotoxicity and identify possible risk factors in patients on Highly Active Anti-retroviral Therapy (HAART). This is a case series assessment of spontaneously reported cases to the Eritrean Pharmacovigilance Centre...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30062014/application-of-nsmol-coupled-with-lc-ms-bioanalysis-for-monitoring-the-fc-fusion-biopharmaceuticals-etanercept-and-abatacept-in-human-serum
#11
Noriko Iwamoto, Kotoko Yokoyama, Megumi Takanashi, Atsushi Yonezawa, Kazuo Matsubara, Takashi Shimada
The principle of nano-surface and molecular-orientation limited (nSMOL) proteolysis has a unique characteristic Fab-selective proteolysis for antibody bioanalysis that is independent of a variety of monoclonal antibodies by the binding antibody Fc via Protein A/G in a pore with 100 nm diameter and modified trypsin immobilization on the surface of nanoparticles with 200 nm diameter. Since minimizing peptide complexity and protease contamination while maintaining antibody sequence specificity enables a rapid and broad development of optimized methods for liquid chromatography-mass spectrometry (LC-MS) bioanalysis, the application of regulatory LC-MS for monitoring antibody biopharmaceuticals is expected...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/30009034/screening-of-anticancer-drugs-to-detect-drug-induced-interstitial-pneumonia-using-the-accumulated-data-in-the-electronic-medical-record
#12
Yoshie Shimai, Toshihiro Takeda, Katsuki Okada, Shirou Manabe, Kei Teramoto, Naoki Mihara, Yasushi Matsumura
Because drug-induced interstitial pneumonia (DIP) is a serious adverse drug reaction, its quantitative risk with individual medications should be taken into due consideration when selecting a medicine. We developed an algorithm to detect DIP using medical record data accumulated in a hospital. Chest computed tomography (CT) is mainly used for the diagnosis of IP, and chest X-ray reports, KL-6, and SP-D values are used to support the diagnosis. The presence of IP in the reports was assessed by a method using natural language-processing, in which IP was estimated according to the product of the likelihood ratio of characteristic keywords in each report...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29992026/enantioselective-pharmacokinetics-of-tramadol-and-its-three-main-metabolites-impact-of-cyp2d6-cyp2b6-and-cyp3a4-genotype
#13
Pernilla Haage, Robert Kronstrand, Martin Josefsson, Simona Calistri, Ron H N van Schaik, Henrik Green, Fredrik C Kugelberg
Tramadol is a complex drug, being metabolized by polymorphic enzymes and administered as a racemate with the (+)- and (-)-enantiomers of the parent compound and metabolites showing different pharmacological effects. The study aimed to simultaneously determine the enantiomer concentrations of tramadol, O -desmethyltramadol, N -desmethyltramadol, and N,O -didesmethyltramadol following a single dose, and elucidate if enantioselective pharmacokinetics is associated with the time following drug intake and if interindividual differences may be genetically explained...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29983986/drug-conjugates-an-emerging-approach-to-treat-breast-cancer
#14
Mahmud Hasan, Rehana K Leak, Robert E Stratford, Darius P Zlotos, Paula A Witt-Enderby
Breast cancer treatment using a single drug is associated with a high failure rate due, in part, to the heterogeneity of drug response within individuals, nonspecific target action, drug toxicity, and/or development of resistance. Use of dual-drug therapies, including drug conjugates, may help overcome some of these roadblocks by more selective targeting of the cancer cell and by acting at multiple drug targets rather than one. Drug-conjugate approaches include linking drugs to antibodies (antibody-drug conjugates), radionuclides (radioimmunoconjugates), nanoparticles (nanoparticle-drug conjugates), or to other drugs (drug-drug conjugates)...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29951207/potential-role-for-histone-deacetylation-in-chronic-diazepam-induced-downregulation-of-%C3%AE-1-gaba-a-receptor-subunit-expression
#15
James Auta, Eleonora Gatta, John M Davis, Subhash C Pandey, Alessandro Guidotti
Corroborating evidence indicate that the downregulation of GABAA receptor subunit expression may underlie tolerance to the anticonvulsant and anxiolytic actions of benzodiazepine (BZ) ligands that act as full allosteric modulators (FAMs) of GABA actions at a variety of GABAA receptor subtypes. We and others have shown that 10-14 days treatment with increasing doses of diazepam (a FAM) resulted in anticonvulsant tolerance and decreased the expression of the α1 GABAA receptor subunit mRNA and protein in frontal cortex...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29938113/the-g-protein-coupled-estrogen-receptor-agonist-g-1-attenuates-bk-channel-activation-in-cerebral-arterial-smooth-muscle-cells
#16
Kirk W Evanson, Jacob A Goldsmith, Payal Ghosh, Michael D Delp
The G protein-coupled estrogen receptor (GPER) is a significant modulator of arterial contractility and blood flow. The GPER-specific activator, G-1, has been widely used to characterize GPER function in a variety of tissue types. Large conductance, calcium (Ca2+ )-activated K+ (BK) channels are sensitive to 17β-estradiol (17β-E2) and estrogenic compounds (e.g., tamoxifen, ICI 182 780) that target estrogen receptors. The purpose of this study was to investigate the effects of G-1 on BK channel activation and function in cerebral arterial myocytes...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29930812/the-safety-tolerability-and-pharmacokinetic-profile-of-gsk2838232-a-novel-2nd-generation-hiv-maturation-inhibitor-as-assessed-in-healthy-subjects
#17
Mark Johnson, Roxanne C Jewell, Amanda Peppercorn, Elizabeth Gould, Jianfeng Xu, Yu Lou, Matthew Davies, Sandra Baldwin, Allan R Tenorio, Matthew Burke, Jerry Jeffrey, Brian A Johns
This work aimed to assess the safety, tolerability, pharmacokinetics (PK), and relative bioavailability of GSK2838232, an investigational HIV maturation inhibitor. GSK2838232 was administered over four dose-escalation studies in healthy subjects which assessed single oral doses (5-250 mg) and repeat doses (up to 200 mg once or twice daily) ±100 mg ritonavir (RTV) once daily. GSK2838232 administration (up to 250 mg) to 124 subjects across four studies resulted in few mild adverse events (AEs) with similar frequencies to placebo...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29930811/evaluation-of-morphine-like-effects-of-the-mixed-mu-delta-agonist-morphine-6-o-sulfate-in-rats-drug-discrimination-and-physical-dependence
#18
Jai Shankar K Yadlapalli, Shoban Babu Bommagani, Ryan D Mahelona, Anqi Wan, Brenda M Gannon, Narsimha R Penthala, Maxim Dobretsov, Peter A Crooks, William E Fantegrossi
Morphine-6-O-sulfate (M6S) is as a mixed-action mu/delta (μ/δ) opioid receptor agonist with high potency and analgesic efficacy. These studies used assays of drug discrimination and schedule-controlled responding to assess abuse-liability, tolerance, and physical dependence as compared to morphine in rats. Attempts to train 0.3 mg/kg (IP) M6S from saline failed, but all rats rapidly acquired the discrimination when the training dose was changed to 3.0 mg/kg morphine, and substitution tests showed that morphine and fentanyl both fully substituted for the training dose, M6S and M3A6S (3-O-acetyl ester of M6S) only partially substituted, and salvinorin A did not elicit morphine-like effects...
July 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29864245/no-effect-of-thymosin-beta-4-on-the-expression-of-the-transcription-factor-islet-1-in-the-adult-murine-heart
#19
Florian Weinberger, Philipp Nicol, Jutta Starbatty, Mandy Stubbendorff, Peter M Becher, Sonja Schrepfer, Thomas Eschenhagen
The transcription factor Islet-1 marks a progenitor cell population of the second heart field during cardiogenesis. In the adult heart Islet-1 expression is limited to the sinoatrial node, the ventricular outflow tract, and parasympathetic ganglia. The regenerative effect in the injured mouse ventricle of thymosin beta-4 (TB4), a 43-aminoacid peptide, was associated with increased Islet-1 immunostaining, suggesting the induction of an Islet-1-positive progenitor state by TB4. Here we aimed to reassess this effect in a genetic model...
June 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29864244/effect-of-a-mitochondrial-targeted-coenzyme-q-analog-on-pancreatic-%C3%AE-cell-function-and-energetics-in-high-fat-fed-obese-mice
#20
Yumi Imai, Brian D Fink, Joseph A Promes, Chaitanya A Kulkarni, Robert J Kerns, William I Sivitz
We recently reported that mitoquinone (mitoQ, 500 μmol/L) added to drinking water of C57BL/6J mice attenuated weight gain and reduced oxidative stress when administered to high-fat (HF) fed mice. Here, we examined the effects of mitoQ administered to HF fed mice on pancreatic islet morphology, dynamics of insulin secretion, and islet mitochondrial metabolism. C57BL/6J mice were fed HF for 130 days while we administered vehicle (cyclodextrin [CD]) or mitoQ added to the drinking water at up to 500 μmol/L...
June 2018: Pharmacology Research & Perspectives
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