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Pharmacology Research & Perspectives

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https://www.readbyqxmd.com/read/29638269/ajulemic-acid-potential-treatment-for-chronic-inflammation
#1
REVIEW
Sumner H Burstein
Ajulemic acid (AJA, CT-3, IP-751, JBT-101, anabasum) is a first-in-class, synthetic, orally active, cannabinoid-derived drug that preferentially binds to the CB2 receptor and is nonpsychoactive. In preclinical studies, and in Phase 1 and 2 clinical trials, AJA showed a favorable safety, tolerability, and pharmacokinetic profile. It also demonstrated significant efficacy in preclinical models of inflammation and fibrosis. It suppresses tissue scarring and stimulates endogenous eicosanoids that resolve chronic inflammation and fibrosis without causing immunosuppression...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29636977/electrical-dynamics-of-isolated-cerebral-and-skeletal-muscle-endothelial-tubes-differential-roles-of-g-protein-coupled-receptors-and-k-channels
#2
Md A Hakim, John N Buchholz, Erik J Behringer
Electrical dynamics of freshly isolated cerebral endothelium have not been determined independently of perivascular nerves and smooth muscle. We tested the hypothesis that endothelium of cerebral and skeletal muscle arteries differentially utilizes purinergic and muscarinic signaling pathways to activate endothelium-derived hyperpolarization. Changes in membrane potential ( V m ) were recorded in intact endothelial tubes freshly isolated from posterior cerebral and superior epigastric arteries of male and female C57BL/6 mice (age: 3-8 months)...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29610666/revisiting-the-putative-role-of-heme-as-a-trigger-of-inflammation
#3
Florence Vallelian, Christian A Schaer, Jeremy W Deuel, Giada Ingoglia, Rok Humar, Paul W Buehler, Dominik J Schaer
Activation of the innate immune system by free heme has been proposed as one of the principal consequences of cell-free hemoglobin (Hb) exposure. Nonetheless, in the absence of infection, heme exposures within a hematoma, during hemolysis, or upon systemic administration of Hb (eg, as a Hb-based oxygen carrier) are typically not accompanied by uncontrolled inflammation, challenging the assumption that heme is a major proinflammatory mediator in vivo. Because of its hydrophobic nature, heme liberated from oxidized hemoglobin is rapidly transferred to alternative protein-binding sites (eg, albumin) or to hydrophobic lipid compartments minimizing protein-free heme under in vivo equilibrium conditions...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29610665/rifampin-modulation-of-xeno-and-endobiotic-conjugating-enzyme-mrna-expression-and-associated-micrornas-in-human-hepatocytes
#4
Brandon T Gufford, Jason D Robarge, Michael T Eadon, Hongyu Gao, Hai Lin, Yunlong Liu, Zeruesenay Desta, Todd C Skaar
Rifampin is a pleiotropic inducer of multiple drug metabolizing enzymes and transporters. This work utilized a global approach to evaluate rifampin effects on conjugating enzyme gene expression with relevance to human xeno- and endo-biotic metabolism. Primary human hepatocytes from 7 subjects were treated with rifampin (10 μmol/L, 24 hours). Standard methods for RNA-seq library construction, EZBead preparation, and NextGen sequencing were used to measure UDP-glucuronosyl transferase UGT, sulfonyltransferase SULT, N acetyltransferase NAT, and glutathione-S-transferase GST mRNA expression compared to vehicle control (0...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29545948/the-drug-interaction-potential-of-daprodustat-when-coadministered-with-pioglitazone-rosuvastatin-or-trimethoprim-in-healthy-subjects
#5
Stephen Caltabiano, Kelly M Mahar, Karyn Lister, David Tenero, Ramiya Ravindranath, Borut Cizman, Alexander R Cobitz
This study was conducted to evaluate the likelihood of daprodustat to act as a perpetrator in drug-drug interactions (DDI) with the CYP2C8 enzyme and OATP1B1 transporter using the probe substrates pioglitazone and rosuvastatin as potential victims, respectively. Additionally, this study assessed the effect of a weak CYP2C8 inhibitor, trimethoprim, as a perpetrator of a DDI with daprodustat. This was a two-part study: Part A assessed the effect of coadministration of daprodustat on the pharmacokinetics of pioglitazone and rosuvastatin in 20 subjects; Part B assessed the coadministration of trimethoprim on the pharmacokinetics of daprodustat in 20 subjects...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29541476/antidyslipidemic-potential-of-a-novel-farnesoid-x-receptor-antagonist-in-a-hamster-model-of-dyslipidemia-comparative-studies-of-other-nonstatin-agents
#6
Emiko Shinozawa, Yuichiro Amano, Hiroko Yamakawa, Megumi Haba, Mitsuyuki Shimada, Ryuichi Tozawa
We attempted to clarify the therapeutic capability of antagonists of the farnesoid X receptor (FXR), a nuclear receptor that regulates lipid and bile acid metabolism. Herein, we report the antidyslipidemic effects of a novel synthesized FXR antagonist, compound-T1, utilizing a dyslipidemic hamster model. Compound-T1 selectively inhibited chenodeoxycholic acid-induced FXR activation (IC50 , 2.1 nmol·L-1 ). A hamster model of diet-induced hyperlipidemia was prepared to investigate the antidyslipidemic effects of compound-T1 through comparative studies of the nonstatin lipid-modulating agents ezetimibe, cholestyramine, and torcetrapib...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29541475/metformin-normalizes-the-structural-changes-in-glycogen-preceding-prediabetes-in-mice-overexpressing-neuropeptide-y-in-noradrenergic-neurons
#7
Liisa Ailanen, Natalia N Bezborodkina, Laura Virtanen, Suvi T Ruohonen, Anastasia V Malova, Sergey V Okovityi, Elizaveta Y Chistyakova, Eriika Savontaus
Hepatic insulin resistance and increased gluconeogenesis are known therapeutic targets of metformin, but the role of hepatic glycogen in the pathogenesis of diabetes is less clear. Mouse model of neuropeptide Y (NPY) overexpression in noradrenergic neurons (OE-NPYD βH ) with a phenotype of late onset obesity, hepatosteatosis, and prediabetes was used to study early changes in glycogen structure and metabolism preceding prediabetes. Furthermore, the effect of the anti-hyperglycemic agent, metformin (300 mg/kg/day/4 weeks in drinking water), was assessed on changes in glycogen metabolism, body weight, fat mass, and glucose tolerance...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29511567/rna-expression-profiling-in-sulfamethoxazole-treated-patients-with-a-range-of-in-vitro-lymphocyte-cytotoxicity-phenotypes
#8
Jennifer M Reinhart, Warren Rose, Daniel J Panyard, Michael A Newton, Tyler K Liebenstein, Jeremiah Yee, Lauren A Trepanier
The lymphocyte toxicity assay (LTA) is a proposed surrogate marker of sulfonamide antibiotic hypersensitivity. In the LTA, peripheral blood mononuclear cells (PBMCs) undergo apoptosis more readily in hypersensitive versus tolerant patients when exposed to drug-hydroxylamine metabolites in vitro. The purpose of this study was to identify key gene transcripts associated with increased cytotoxicity from sulfamethoxazole-hydroxylamine in human PBMCs in the LTA. The LTA was performed on PBMCs of 10 patients hypersensitive to trimethoprim-sulfamethoxazole (HS) and 10 drug-tolerant controls (TOL), using two cytotoxicity assays: YO-PRO (n = 20) and MTT (n = 12)...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29511566/assessment-of-self-reporting-reading-of-medicine-s-labels-and-the-resources-of-information-about-medicines-in-general-public-in-malaysia
#9
Omar T Dawood, Mohamed A Hassali, Fahad Saleem, Inas R Ibrahim
This study was undertaken to assess the people's self-reported reading of medicine labels and its associated factors and to assess the sources of information about medicines among general public. A cross-sectional study was carried out among general public in the State of Penang, Malaysia. A total of 888 participants were conveniently selected and completed the survey. A self-administered questionnaire was used to obtain the data from all the participants. Most of the participants (74.2%) reported that they have adequate information about medicines provided on their medicine labels...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29484189/race-affects-svr12-in-a-large-and-ethnically-diverse-hepatitis-c-infected-patient-population-following-treatment-with-direct-acting-antivirals-analysis-of-a-single-center-department-of-veterans-affairs-cohort
#10
Jihane N Benhammou, Tien S Dong, Folasade P May, Jenna Kawamoto, Ram Dixit, Samuel Jackson, Vivek Dixit, Debika Bhattacharya, Steven B Han, Joseph R Pisegna
Hepatitis C virus (HCV) infection is a major cause of chronic liver disease. HCV cure has been linked to improved patient outcomes. In the era of direct-acting antivirals (DAAs), HCV cure has become the goal, as defined by sustained virological response 12 weeks (SVR12) after completion of therapy. Historically, African-Americans have had lower SVR12 rates compared to White people in the interferon era, which had been attributed to the high prevalence of non-CC interleukin 28B (IL28B) type. Less is known about the association between race/ethnicity and SVR12 in DAA-treated era...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29468071/dietary-tetrahydrocurcumin-reduces-renal-fibrosis-and-cardiac-hypertrophy-in-5-6-nephrectomized-rats
#11
Wei Ling Lau, Mahyar Khazaeli, Javad Savoj, Kasim Manekia, Maria Bangash, Roshni G Thakurta, Anhthu Dang, Nosratola D Vaziri, Bhupinder Singh
Tetrahydrocurcumin (THC) is the principal metabolite of curcumin and has antioxidant properties. In the present investigation, the effect of THC on renal and cardiovascular outcomes was studied in rats with chronic kidney disease (CKD). CKD rats were randomized following 5/6 nephrectomy to a special diet for 9 weeks which contained 1% THC (CKD+THC group). Low-dose polyenylphosphatidylcholine was used as a lipid carrier to increase bioavailability. Endpoints included tail blood pressure, normalized heart weight, plasma and urine biochemical data, and kidney tissue analyses...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29468070/reduced-alcohol-seeking-in-male-offspring-of-sires-exposed-to-alcohol-self-administration-followed-by-punishment-imposed-abstinence
#12
Erin J Campbell, Jeremy P M Flanagan, Nathan J Marchant, Andrew J Lawrence
Emerging evidence has demonstrated that paternal alcohol use can modify the behavior of offspring, particularly male offspring. However, preclinical studies to date have not used voluntary self-administration of alcohol to examine alcohol-related behaviors in offspring. Here, we tested the hypothesis that paternal alcohol self-administration followed by punishment-imposed abstinence alters alcohol consumption and seeking in male offspring. Male inbred alcohol preferring iP rats were trained to self-administer alcohol in one context followed by punishment-imposed suppression of alcohol-seeking in a different context using contingent footshock...
April 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417765/conflicting-evidence-for-the-role-of-jnk-as-a-target-in-breast-cancer-cell-proliferation-comparisons-between-pharmacological-inhibition-and-selective-shrna-knockdown-approaches
#13
Rachel A Wood, Mark J Barbour, Gwyn W Gould, Margaret R Cunningham, Robin J Plevin
As a target, the JNK pathway has been implicated in roles including cell death, proliferation, and inflammation in variety of contexts which span cardiovascular disease, neurodegenerative pathologies, and cancer. JNK1 and JNK2 have recently been demonstrated to function independently, highlighting a new parameter in the study of the JNK pathway. In order for JNK1 and JNK2-specific roles to be defined, better tools need to be employed. Previous studies have relied upon the broad spectrum JNK inhibitor, SP600125, to characterize the role of JNK signaling in a number of cell lines, including the breast cancer cell line MCF-7...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417764/prospective-evaluation-of-ceftriaxone-use-in-medical-and-emergency-wards-of-gondar-university-referral-hospital-ethiopia
#14
Asnakew Achaw Ayele, Begashaw Melaku Gebresillassie, Daniel Asfaw Erku, Eyob Alemayehu Gebreyohannes, Dessalegn Getnet Demssie, Amanual Getnet Mersha, Henok Getachew Tegegn
Ceftriaxone is among the most commonly utilized antibiotics owing to its high potency, wide spectrum of activity, and low risk of toxicity. It is used to treat different types of bacterial infections including pneumonia, bone infections, abdominal infections, Skin and soft tissue infections, urinary tract infections. However, evidence around the globe shows the misuse of Ceftriaxone. This study aimed at evaluating the appropriateness of ceftriaxone use in medical and emergency wards of Gondar university referral hospital (GURH), Northwest Ethiopia...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417763/combined-treatment-with-a-selective-pde10a-inhibitor-tak-063-and-either-haloperidol-or-olanzapine-at-subeffective-doses-produces-potent-antipsychotic-like-effects-without-affecting-plasma-prolactin-levels-and-cataleptic-responses-in-rodents
#15
Kazunori Suzuki, Akina Harada, Hirobumi Suzuki, Clizia Capuani, Annarosa Ugolini, Mauro Corsi, Haruhide Kimura
Activation of indirect pathway medium spiny neurons (MSNs) via promotion of cAMP production is the principal mechanism of action of current antipsychotics with dopamine D2 receptor antagonism. TAK-063 [1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one] is a novel phosphodiesterase 10A inhibitor that activates both direct and indirect pathway MSNs through increasing both cAMP and cGMP levels by inhibition of their degradation. The activation of indirect pathway MSNs through the distinct mechanism of action of these drugs raises the possibility of augmented pharmacological effects by combination therapy...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417762/improving-the-assessment-of-adverse-drug-reactions-using-the-naranjo-algorithm-in-daily-practice-the-japan-adverse-drug-events-study
#16
Hiroki Murayama, Mio Sakuma, Yuri Takahashi, Takeshi Morimoto
It is difficult to determine adverse drug reactions (ADRs) in daily complicated clinical practice in which many kinds of drugs are prescribed. We evaluated how well the Naranjo Algorithm (NA) categorized ADRs among suspected ADRs. The Japan Adverse Drug Events (JADE) study was a prospective cohort study of 3459 inpatients. After all suspected ADRs were reported from research assistants, a single physician reviewer independently assigned an NA score to each. After all NA score of suspected ADRs were scored, two physician reviewers discussed and determined ADRs based on the literature...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417761/pharmacokinetic-equivalence-comparable-safety-and-immunogenicity-of-an-adalimumab-biosimilar-product-m923-to-humira-in-healthy-subjects
#17
Jan Hillson, Tim Mant, Molly Rosano, Carolyn Huntenburg, Mehrshid Alai-Safar, Siddhesh Darne, Donna Palmer, Borislava G Pavlova, Jennifer Doralt, Russell Reeve, Niti Goel, Doris Weilert, Paul W Rhyne, Kamali Chance, John Caminis, James Roach, Tanmoy Ganguly
The aims of this randomized, double-blind, three-arm, single-dose study were to demonstrate pharmacokinetic (PK) equivalence of the adalimumab biosimilar M923 (hereafter referred to as "M923") to each of 2 reference products, and to assess M923's safety and immunogenicity. Primary PK endpoints were maximum observed concentration (Cmax ), area under the curve (AUC) from time 0 extrapolated to infinity (AUC0-inf ), and AUC from time 0 to 336 hours (AUC0-336 ). Secondary endpoints included safety and immunogenicity assessments...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417760/fosfomycin-as-a-potential-therapy-for-the-treatment-of-systemic-infections-a-population-pharmacokinetic-model-to-simulate-multiple-dosing-regimens
#18
Natalia V Ortiz Zacarías, Anneke C Dijkmans, Jacobus Burggraaf, Johan W Mouton, Erik B Wilms, Cees van Nieuwkoop, Daan J Touw, Ingrid M C Kamerling, Jasper Stevens
Fosfomycin has emerged as a potential therapy for multidrug-resistant bacterial infections. In most European countries, the oral formulation is only approved as a 3 g single dose for treatment of uncomplicated cystitis. However, for the treatment of complicated systemic infections, this dose regimen is unlikely to reach efficacious serum and tissue concentrations. This study aims to investigate different fosfomycin-dosing regimens to evaluate its rationale for treatment of systemic infections. Serum concentration-time profiles of fosfomycin were simulated using a population pharmacokinetic model based on published pharmacokinetic parameter values, their uncertainty, inter-individual variability and covariates...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417759/anxiety-and-activity-related-effects-of-paracetamol-on-healthy-and-neuropathic-rats
#19
Zuyue Chen, Hong Wei, Antti Pertovaara, Jianhong Wang, Synnöve Carlson
Paracetamol has recently been suggested to affect emotion processing in addition to alleviating pain in humans. We investigated in adult male Hannover-Wistar rats whether acute intraperitoneally administrated paracetamol affects behavior in tests measuring anxiety, mood, motor activity, and memory. Unoperated rats received saline or a low (50 mg/kg) or high (300 mg/kg) dose of paracetamol, while rats with a spared nerve injury (SNI) model of neuropathy and sham-operated rats received saline or the low dose of paracetamol...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29417758/protective-effect-of-carvedilol-alone-and-coadministered-with-diltiazem-and-prednisolone-on-doxorubicin-and-5-fluorouracil-induced-hepatotoxicity-and-nephrotoxicity-in-rats
#20
Abidemi J Akindele, Gabriel O Oludadepo, Kennedy I Amagon, Dhirendra Singh, Daniel D Osiagwu
This study investigated the protective effects of carvedilol alone and coadministered with prednisolone and diltiazem on doxorubicin (DOX) and 5-fluorouracil (5-FU)-induced toxicity. Each of 2 pools of 70 female rats were randomly allotted into 10 groups of 7 animals each and treated as follows: Group 1: normal saline (10 mL/kg); Group 2: normal saline and DOX (40 mg/kg)/5-FU (20 mg/kg) alone; Group 3: gallic acid (200 mg/kg) and DOX/5-FU; Group 4: carvedilol (0.075 mg/kg) and DOX/5-FU; Group 5: carvedilol (0...
February 2018: Pharmacology Research & Perspectives
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