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Pharmacology

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https://www.readbyqxmd.com/read/28219076/effect-of-n-benzylpiperazine-its-metabolite-n-benzylethylenediamine-and-its-disubstituted-analogue-n-n-dibenzylpiperazine-on-the-acquisition-formation-and-consolidation-of-memory-in-mice
#1
Juan Carlos Castillo-Hernández, Josué A Velázquez-Moyado, Adelfo Reyes-Ramírez, Elena G Ramírez-López, Martín González-Andrade, Andrés Navarrete
BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. These compounds increase the release of dopamine and serotonin. BZP mimics the psychoactive effects of 3,4-methylenedioxymethylamphetamine. BZP is metabolized to N-benzylethylenediamine (BEDA) and benzylamine. The compound N,N'-dibenzylpiperazine (DBZP) is obtained as a byproduct during the synthesis of BZP. Some PZDs have shown effects on memory; however, there are no previous reports on the activity of BZP, BEDA, and DBZP on memory or on a description of their neuropharmacological profile...
February 21, 2017: Pharmacology
https://www.readbyqxmd.com/read/28214870/the-inhibitory-effect-of-s-777469-a-cannabinoid-type-2-receptor-agonist-on-skin-inflammation-in-mice
#2
Takayo Haruna, Masahiko Soga, Yasuhide Morioka, Kinichi Imura, Yoko Furue, Mina Yamamoto, Jun Hayakawa, Masashi Deguchi, Akinori Arimura, Kiyoshi Yasui
We investigated the effects of S-777469 (1-[[6-Ethyl-1-[4-fluorobenzyl]-5-methyl-2-oxo-1, 2-dihydropyridine-3-carbonyl]amino]-cyclohexanecarboxylic acid), a novel cannabinoid type 2 receptor (CB2) agonist, on 1-fluoro-2,4-dinitrobenzene (DNFB)-induced ear inflammation and mite antigen-induced dermatitis in mice. The oral administration of S-777469 significantly suppressed DNFB-induced ear swelling in a dose-dependent manner. In addition, S-777469 significantly alleviated mite antigen-induced atopic dermatitis-like skin lesions in NC/Nga mice...
February 18, 2017: Pharmacology
https://www.readbyqxmd.com/read/28208135/abcb1-and-slco1b3-gene-polymorphisms-and-their-impact-on-digoxin-pharmacokinetics-in-atrial-fibrillation-patients-among-the-tunisian-population
#3
Nejia Tounsi, Imen Trabelsi, Emna Kerkeni, Mohamed Habib Grissa, Nizar Fredj, Adel Sekma, Malek Mzali, Ilhem Hellara, Kamel Monastiri, Wahiba Douki, Semir Nouira
BACKGROUND: Digoxin is a substrate of P-glycoprotein (P-gp) and organic anion transporting polypeptide transporters that are encoded by ABCB1 and SLCO1B3 genes. Genetic polymorphisms in both genes may explain inter-individual variability of serum digoxin concentration (SDC). This study evaluates the possible effect of the most common ABCB1 and SLCO1B3 polymorphisms on SDC after a single oral dose of digoxin in Tunisian atrial fibrillation (AF) patients. METHODS: ABCB1 and SLCO1B3 genotypes were analyzed in 102 patients with AF who received digoxin (0...
February 17, 2017: Pharmacology
https://www.readbyqxmd.com/read/28147362/hochuekkito-a-japanese-herbal-medicine-restores-metabolic-homeostasis-between-mitochondrial-and-glycolytic-pathways-impaired-by-influenza-a-virus-infection
#4
Keita Takanashi, Katsuaki Dan, Sho Kanzaki, Hideki Hasegawa, Kenji Watanabe, Kaoru Ogawa
BACKGROUND: Hochuekkito (HKT), a traditional Japanese herbal medicine (Kampo), has been used to treat symptoms of several diseases. In a recent clinical study, HKT was shown to be protective against the influenza virus infection. However, the underlying mechanism of the prophylactic effect is not clear. Mitochondrial and glycolytic pathways play important roles in cellular energy metabolism to maintain biological functions. These metabolic pathways are affected by the influenza virus infection...
February 2, 2017: Pharmacology
https://www.readbyqxmd.com/read/28147361/enantioselective-effect-of-flurbiprofen-on-lithium-disposition-in-rats
#5
Yuichi Uwai, Masashi Matsumoto, Tatsuya Kawasaki, Tomohiro Nabekura
AIMS: Lithium is administered for treating bipolar disorders and is mainly excreted into urine. Nonsteroidal anti-inflammatory drugs inhibit this process. In this study, we examined the enantioselective effect of flurbiprofen on the disposition of lithium in rats. METHODS: Pharmacokinetic experiments with lithium were performed. RESULTS: Until 60 min after the intravenous administration of lithium chloride at 30 mg/kg as a bolus, 17.8% of lithium injected was recovered into the urine...
February 2, 2017: Pharmacology
https://www.readbyqxmd.com/read/28132058/the-inhibitory-effects-of-ketamine-on-human-hyperpolarization-activated-cyclic-nucleotide-gated-channels-and-action-potential-in-rabbit-sinoatrial-node
#6
Junlian Xing, Chi Zhang, Wanzhen Jiang, Jie Hao, Zhipei Liu, Antao Luo, Peihua Zhang, Xinrong Fan, Jihua Ma
AIMS: To investigate the effects of ketamine on human hyperpolarization-activated cyclic nucleotide-gated (hHCN) 1, 2, 4 channel currents expressed in Xenopus oocytes and spontaneous action potentials (APs) of rabbit sinoatrial node (SAN). METHODS: The 2-electrode voltage clamp and standard microelectrode techniques were respectively applied to record hHCN channels currents expressed in Xenopus oocytes and APs of SAN separated from rabbit heart. RESULTS: Ketamine (1-625 µmol/L) blocked hHCN1, 2, and 4 currents with IC50 of 67...
January 28, 2017: Pharmacology
https://www.readbyqxmd.com/read/28125813/signal-transduction-underlying-the-inhibitory-mechanism-of-fluoxetine-on-electrical-field-stimulation-response-in-rat-ileal-smooth-muscle
#7
Phyu Phyu Khin, Tin Sandar Zaw, Uy Dong Sohn
Fluoxetine (FLX), a well-known antidepressant drug under the class of selective serotonin reuptake inhibitor, exerts its action by inhibiting the reuptake of serotonin selectively. In some studies, it has been demonstrated that FLX relaxes the intestinal smooth muscle. In this study, we aimed at studying the signal transduction pathway underlying the muscle relaxation effect of FLX on electrically stimulated rat ileal muscle contraction. To investigate the possible mechanism involved, various antagonists were used...
January 27, 2017: Pharmacology
https://www.readbyqxmd.com/read/28110334/muscone-induces-cyp1a2-and-cyp3a4-enzyme-expression-in-l02-human-liver-cells-and-cyp1a2-and-cyp3a11-enzyme-expression-in-kunming-mice
#8
Sha Liu, Yujie Cheng, Menglin Rao, Mi Tang, Zhi Dong
AIM: To examine the effect of synthetic muscone on the expression of CYP1A2 and CYP3A4 enzymes in human liver L02 cells and in the liver tissue of Kunming mice. METHODS: The L02 hepatic cell line was used to study the effect of low (10-4 μmol/L), middle (10-3 μmol/L), and high concentrations (10-2 μmol/L) of muscone on the expression of CYP1A2 and CYP3A4 enzymes. In addition, the cytochrome P450 (CYP) expression was investigated in Kunming mice after the administration of 10 mg/kg (low), 50 mg/kg (middle), and 100 mg/kg (high) dose of muscone for 6 days...
January 21, 2017: Pharmacology
https://www.readbyqxmd.com/read/28052289/the-pharmacokinetic-interaction-study-between-carvedilol-and-bupropion-in-rats
#9
Maria Bianca Abrudan, Dana Maria Muntean, Ana Maria Gheldiu, Maria Adriana Neag, Laurian Vlase
BACKGROUND/AIMS: The effects of multiple-dose bupropion on the pharmacokinetics of single-dose carvedilol were investigated in order to evaluate this possible drug-drug interaction. METHODS: A preclinical study was conducted among white male Wistar rats. Each rat was cannulated on the femoral vein prior to being connected to BASi Culex ABC®. During the reference period, each rat received an intravenous and an oral dose of 3.57 mg/kg body weight (b.w.) carvedilol, at 2 days distance...
January 5, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049212/enhanced-hyperthermic-responses-to-lipopolysaccharide-in-mice-exposed-to-repeated-cold-stress
#10
Tomoyoshi Miyamoto, Yoshinori Funakami, Erika Kawashita, Shiori Tomita, Ai Nomura, Nanako Sugimoto, Haruka Saeki, Takaya Miyazakia, Maho Tsubota, Seiji Ichida, Atsufumi Kawabata
Lipopolysaccharide (LPS) induces hyperthermia accompanied by various other systemic inflammatory symptoms. The rodents exposed to repeated cold (RC) stress according to a specific schedule are useful as experimental models for autonomic imbalance or fibromyalgia. It is now proven that RC-stressed mice exhibit tolerance to LPS, we examined thermal responses to LPS challenge in RC-stressed mice by monitoring core temperature using the telemetry system. Systemic administration of LPS caused bimodal hyperthermic responses in RC-stressed and unstressed mice...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049205/bufalin-inhibits-the-inflammatory-effects-in-asthmatic-mice-through-the-suppression-of-nuclear-factor-kappa-b-activity
#11
Zibierguli Zhakeer, Maierbati Hadeer, Zumulaiti Tuerxun, Kelibiena Tuerxun
Asthma is an inflammatory airway disease characterized by increased infiltration of inflammatory cells into the airways and poor respiratory function. Bufalin is one of the biological ingredients obtained from Chansu. Bufalin was found to possess various pharmacological properties including anti-inflammatory activities. However, the effect of bufalin treatment on asthma has not yet been reported. Therefore, this study aimed to investigate the inhibitory effect of bufalin on asthmatic response in a murine model...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049198/mechanism-of-2-3-4-5-tetrahydroxystilbene-2-o-%C3%AE-d-glucoside-induced-upregulation-of-glutamate-transporter-1-protein-expression-in-mouse-primary-astrocytes
#12
Xiangfan Chen, Wenfeng Hu, Xu Lu, Bo Jiang, Jili Wang, Wei Zhang, Chao Huang
Glutamate transporter-1 (GLT-1), a major glutamate transporter expressed in astrocytes, takes up excess glutamate from the micro-environment in order to prevent excitotoxicity. Drugs that increase GLT-1 expression may have therapeutic effects in disorders associated with neuronal excitotoxicity. 2,3,4',5-tetrahydroxystilbene 2-O-β-D-glucoside (TSG), a monomer of stilbene from polygonummultiflorum, exerts neuroprotection in a range of experimental models such as Alzheimer's disease and brain ischemia. In this study, we evaluated the effect of TSG on GLT-1 protein expression in mouse primary-cultured astrocytes...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049192/combined-memantine-and-donepezil-treatment-improves-behavioral-and-psychological-symptoms-of-dementia-like-behaviors-in-olfactory-bulbectomized-mice
#13
Yasushi Yabuki, Kazuya Matsuo, Koga Hirano, Yasuharu Shinoda, Shigeki Moriguchi, Kohji Fukunaga
Memantine, an uncompetitive N-methyl-D-aspartate receptor antagonist, and the cholinesterase inhibitor, donepezil, are approved in most countries for treating moderate-to-severe Alzheimer's disease (AD). These drugs have different molecular targets; thus, it is expected that the effects of combined treatment would be synergistic. Some reports do show memantine/donepezil synergy in ameliorating cognition in AD model animals, but their combined effects on behavioral and psychological symptoms of dementia (BPSD)-like behaviors have not been addressed...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28049190/the-efficacy-of-rituximab-combined-with-131i-for-ophthalmic-outcomes-of-graves-ophthalmopathy-patients
#14
Jiagen Li, Zhangsheng Xiao, Xianjie Hu, Yun Li, Xing Zhang, Songze Zhang, Weikun Gong, Jianqiang Zhao, Xuemei Ye
PURPOSE: The purpose of this study is to examine the effectiveness of introducing both rituximab (RTX) and 131I for active Graves' ophthalmopathy (GO) with hyperthyroidism. METHODS: In total, 217 patients suffering from active GO with hyperthyroidism were included in this research. All subjects were randomly assigned to 3 groups. Patients in group A solely received 131I treatment; group B1 underwent a methylprednisolone treatment in combination with 131I treatment; and group B2 received an RTX in combination with 131I treatment...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/27992867/dronedarone-modulates-m1-and-m3-muscarinic-receptors-with-subtype-selectivity-functional-selectivity-and-probe-dependence
#15
Gihan M Jayasuriya, Gwendolynne Elmslie, Ethan S Burstein, John Ellis
We have previously reported that amiodarone interacts with a novel allosteric site on muscarinic receptors. Amiodarone's most striking effect is to enhance the maximal response elicited by muscarinic agonists at the M1, M3, and M5 receptors. Furthermore, the quaternary analog N-ethylamiodarone (NEA) is inhibitory at these receptors and appears to compete with amiodarone at that allosteric site. In the present studies, we show that dronedarone also modulates Gq-mediated responses at M1 and M3, although in a more discriminating manner...
December 20, 2016: Pharmacology
https://www.readbyqxmd.com/read/27988509/rivaroxaban-induced-gastrointestinal-bleeding-presenting-as-acute-colon-obstruction
#16
Merav Cohen, Hadar Nevo, Dan Hershko, Alexander Becker
Rivaroxaban is a member of the novel target-specific oral anticoagulants (TSOACs) family of drugs recently approved for the prevention and treatment of venous thromboembolism events. A major drawback of the drug is its potential for causing severe hemorrhagic events, which may be difficult to treat in an emergency setting due to lack of effective antidote. Here, we describe a case of acute gastrointestinal (GI) hemorrhage leading to complete colon obstruction in a patient treated with rivaroxaban. Summary and Key Messages: The case presented here demonstrates a chain of events originating from an unprovoked intramural bleeding in a patient using rivaroxaban, leading to an organized giant clot formation, and to complete colon obstruction...
December 15, 2016: Pharmacology
https://www.readbyqxmd.com/read/27931022/hydrogen-sulfide-and-t-type-ca2-channels-in-pain-processing-neuronal-differentiation-and-neuroendocrine-secretion
#17
Kazuki Fukami, Fumiko Sekiguchi, Atsufumi Kawabata
BACKGROUND: Hydrogen sulfide (H2S), a gasotransmitter, is generated from L-cysteine by mainly 3 enzymes, cystathionine-γ-lyase (CSE), cystathionine-β-synthase, and 3-mercaptopyruvate sulfurtransferase in cooperation with cysteine aminotransferase. The H2S-forming enzymes, particularly CSE, are overexpressed under the pathological conditions such as inflammation, neuronal or neuroendocrine differentiation and cancer development. Given that Cav3.2 T-type Ca2+ channels mediate some of the biological activity of H2S, we focus on the role of the H2S/Cav3...
December 9, 2016: Pharmacology
https://www.readbyqxmd.com/read/27816979/evaluation-of-the-potential-pharmacokinetic-interaction-between-atomoxetine-and-fluvoxamine-in-healthy-volunteers
#18
Ioana Todor, Adina Popa, Maria Neag, Dana Muntean, Corina Bocsan, Anca Buzoianu, Laurian Vlase, Ana-Maria Gheldiu, Corina Briciu
BACKGROUND/AIMS: Attention deficit hyperactivity disorder (ADHD) is frequently associated with other psychiatric pathologies. Therefore, the present study investigated a possible pharmacokinetic interaction between atomoxetine (ATX), a treatment option for ADHD, and an antidepressant, namely, fluvoxamine (FVX). METHODS: Designed as an open-label, non-randomized clinical trial, the study included 2 periods. In period 1 (reference), each subject received ATX 25 mg (single-dose), whereas in period 2 (test), all subjects were given a combination of ATX 25 mg + FVX 100 mg, following a 6-day pretreatment regimen with the enzymatic inhibitor...
2017: Pharmacology
https://www.readbyqxmd.com/read/27771722/inhibitory-effects-of-antidepressants-on-acetylcholine-induced-contractions-in-isolated-guinea-pig-urinary-bladder-smooth-muscle
#19
Junji Uno, Keisuke Obara, Hiroko Suzuki, Satomi Miyatani, Daisuke Chino, Takashi Yoshio, Yoshio Tanaka
BACKGROUND/AIMS: To investigate the potential inhibitory effects of 18 clinically available antidepressants on acetylcholine (ACh)-induced contractions in guinea pig urinary bladder smooth muscle (UBSM) in order to predict whether they may induce voiding impairment. METHODS: Concentration-response curves for ACh-induced contractions in guinea pig UBSM strips were obtained in the absence or presence of selected antidepressants. When inhibitory effects indicated competitive antagonism, pA2 values against ACh were calculated and compared to plausible antidepressant blood concentrations...
2017: Pharmacology
https://www.readbyqxmd.com/read/27756073/cardiovascular-profile-of-propranolol-after-multiple-dosing-in-infantile-hemangioma
#20
Patrizia Salice, Mario Giovanni Bianchetti, Alessandra Giavarini, Erica Gondoni, Riccardo Cavalli, Anna Maria Colli, Federico Lombardi
Propranolol is becoming the treatment of choice for complicated infantile hemangioma. We report here data on peripheral blood flow, O2-saturation, electrocardiographic PR-interval, left ventricular function, blood pressure and heart rate that were assessed before and during treatment for ≥4 weeks with propranolol 2 mg/kg of body weight daily in 67 infants <12 months of age in normal sinus rhythm and with structurally normal hearts. Management with propranolol was well tolerated in all and did not modify peripheral blood flow, O2-saturation, electrocardiographic PR-interval and left ventricular fractional shortening or ejection fraction...
2017: Pharmacology
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