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Journal of Pharmacological Sciences

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https://www.readbyqxmd.com/read/28330759/amiodarone-reduces-depolarization-evoked-glutamate-release-from-hippocampual-synaptosomes
#1
Chia Yu Chang, Chi Feng Hung, Shu Kuei Huang, Jinn Rung Kuo, Su Jane Wang
Decreased brain glutamate level has emerged as a new therapeutic approach for epilepsy. This study investigated the effect and mechanism of amiodarone, an anti-arrhythmic drug with antiepileptic activity, on glutamate release in the rat hippocampus. In a synaptosomal preparation, amiodarone reduced 4-aminopyridine-evoked Ca(2+)-dependent glutamate release and cytosolic Ca(2+) concentration elevation. Amiodarone did not affect the 4-aminopyridine-evoked depolarization of the synaptosomal membrane potential or the Na(+) channel activator veratridine-evoked glutamate release, indicating that the amiodarone-mediated inhibition of glutamate release is not caused by a decrease in synaptosomal excitability...
March 8, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28325557/effects-of-new-antiarrhythmic-agent-ss-68-on-excitation-conduction-electrical-activity-in-purkinje-fibers-and-pulmonary-veins-assessment-of-safety-and-side-effects-risk
#2
Saida K Bogus, Vladislav S Kuzmin, Denis V Abramochkin, Konstantin F Suzdalev, Pavel A Galenko-Yaroshevsky
The compound SS-68 has been selected among numerous new derivatives of indole and demonstrated antiarrhythmic effects in animal models. The present study concerns several aspects of SS-68 safety and efficacy as a potential antiarrhythmic drug. The first estimation of atrioventricular conduction in mammalian heart under SS-68 has been carried out; effects of SS-68 in Purkinje fibers and myocardium of pulmonary veins have been investigated. The drug weakly affects cardiac atrioventricular conduction: only high concentrations of SS-68 (≥10 μmol/L) significantly decrease this parameter...
March 2, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28318829/toll-like-receptor-4-inhibitor-protects-against-retinal-ganglion-cell-damage-induced-by-optic-nerve-crush-in-mice
#3
Yukimichi Nakano, Masamitsu Shimazawa, Kazuki Ojino, Hiroshi Izawa, Hiroto Takeuchi, Yuki Inoue, Kazuhiro Tsuruma, Hideaki Hara
Toll-like receptor 4 (TLR4) plays key roles in innate immune responses and inflammatory reactions. TAK-242 (resatorvid) is a small-molecule cyclohexene derivative that selectively inhibits TLR4 signaling pathways and suppresses inflammatory reactions. Here we investigated the protective effects of TAK-242 against optic nerve crush (ONC) which induces axonal injury like glaucoma in mice. TAK-242 was injected intravitreally immediately after ONC. The effect of TAK-242 was evaluated by measuring the number of fluorogold-labeled retinal ganglion cells (RGCs) at 10 days after ONC...
March 2, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28302446/electrophysiological-evidence-of-increased-glycine-receptor-mediated-phasic-and-tonic-inhibition-by-blockade-of-glycine-transporters-in-spinal-superficial-dorsal-horn-neurons-of-adult-mice
#4
Misa Oyama, Seiya Kuraoka, Shun Watanabe, Takashi Iwai, Mitsuo Tanabe
To understand the synaptic and/or extrasynaptic mechanisms underlying pain relief by blockade of glycine transporter subtypes GlyT1 and GlyT2, whole-cell recordings were made from dorsal horn neurons in spinal slices from adult mice, and the effects of NFPS and ALX-1393, selective GlyT1 and GlyT2 inhibitors, respectively, on phasic evoked or miniature glycinergic inhibitory postsynaptic currents (eIPSCs or mIPSCs) were examined. NFPS and ALX-1393 prolonged the decay phase of eIPSCs without affecting their amplitude...
February 27, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28314697/demeanor-of-rivaroxaban-in-activated-inactivated-fxa
#5
Kaname Seki, Yosuke Mizuno, Toku Sakashita, Shintaro Nakano, Jun Tanno, Yasushi Okazaki, Toshihiro Muramatsu, Shigeyuki Nishimura, Takaaki Senbonmatsu
Activated factor X (FXa) plays an important role in thrombin generation and inflammation. Factor X is not converted constitutively to FXa, but only after intrinsic clotting factors are activated and/or cellular injury occurs. Although rivaroxaban is one of direct FXa inhibitors, its function in the inactivated coagulation cascade is unclear. In human umbilical vein endothelial cells that natively express protease-activated receptor-1 and -2, high dose rivaroxaban did not alter gene transcripts including pro-inflammatory genes in DNA microarray...
February 24, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28302448/aconitine-a-potential-novel-treatment-for-systemic-lupus-erythematosus
#6
Xiaodong Li, Liwei Gu, Lan Yang, Dong Zhang, Jianying Shen
BACKGROUND: Aconitum plants have been widely used in China for thousands of years. Recent evidences indicate that aconitine, the main active ingredient of Aconitum, has immunomodulatory properties that might be useful for treating autoimmune diseases, such as rheumatoid arthritis. In this study, we conducted a pilot study to explore the effect and mechanisms of aconitine on the treatment of systemic lupus erythematosus. METHODS: A pristane-induced murine model was used...
February 24, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28286019/methotrexate-causes-acute-hyperplasia-of-enterochromaffin-cells-containing-substance-p-in-the-intestinal-mucosa-of-rats
#7
Takuji Machida, Yuho Takano, Kenji Iizuka, Maiko Machida, Masahiko Hirafuji
This study aimed to investigate the acute and chronic effect of methotrexate on the intestinal substance P metabolism after a single administration to rats. Methotrexate caused a significant increase in the number of substance P-containing cells in the ileal mucosa both at 24 and 96 h. Most of enterochromaffin cells expressing l-tryptophan hydroxylase contained substance P. The expression of Tac1 mRNA was increased by methotrexate at 24 h, but not at 96 h. Thus, methotrexate causes acute hyperplasia of enterochromaffin cells in the intestinal mucosa of rats with a transient increase in the production of substance P...
February 22, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28325558/l-citrulline-ameliorates-cerebral-blood-flow-during-cortical-spreading-depression-in-rats-involvement-of-nitric-oxide-and-prostanoids-mediated-pathway
#8
Yuki Kurauchi, Koichi Mokudai, Asami Mori, Kenji Sakamoto, Tsutomu Nakahara, Masahiko Morita, Ayako Kamimura, Kunio Ishii
l-Citrulline is a potent precursor of l-arginine, and exerts beneficial effect on cardiovascular system via nitric oxide (NO) production. Migraine is one of the most popular neurovascular disorder, and imbalance of cerebral blood flow (CBF) observed in cortical spreading depression (CSD) contributes to the mechanism of migraine aura. Here, we investigated the effect of l-citrulline on cardiovascular changes to KCl-induced CSD. in rats. Intravenous injection of l-citrulline prevented the decrease in CBF, monitored by laser Doppler flowmetry, without affecting mean arterial pressure and heart rate during CSD...
February 17, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28302447/dcebio-facilitates-myogenic-differentiation-via-intermediate-conductance-ca-2-activated-k-channel-activation-in-c2c12-myoblasts
#9
Shoko Tanaka, Yuko Ono, Kazuho Sakamoto
Membrane hyperpolarization is suggested to be a trigger for skeletal muscle differentiation. We investigated whether DCEBIO, an opener of the small/intermediate conductance Ca(2+) activated K(+) (SKCa/IKCa) channels, increase myogenic differentiation in C2C12 skeletal myoblasts. DCEBIO significantly increased myotube formation, protein expression level of myosin heavy chain II, and mRNA expression level of myogenin in C2C12 myoblasts cultured in differentiation medium. DCEBIO induced myotube formation and hyperpolarization were reduced by the IKCa channel blocker TRAM-34, but not by the SKCa channel blocker apamin...
February 17, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28279595/effect-of-a-dosing-time-on-quetiapine-induced-acute-hyperglycemia-in-mice
#10
Snehal Kapse, Hitoshi Ando, Yuki Fujiwara, Chisato Suzuki, Kentaro Ushijima, Hiroko Kitamura, Keiko Hosohata, Kazuhiko Kotani, Shigeki Shimba, Akio Fujimura
Although rare, second-generation antipsychotic drugs cause severe hyperglycemia within several days after the initiation of therapy. Because glucose tolerance exhibits circadian rhythmicity, we evaluated an effect of a dosing-time on quetiapine-induced acute hyperglycemia in mice. A single intraperitoneal dose of quetiapine dosing-time-independently induced insulin resistance in fasted C57BL/6J mice. However, acute hyperglycemic effect was detected only after dosing of the drug at the beginning of an active phase...
February 17, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28259560/4-chlorophenylguanidine-is-an-asic3-agonist-and-positive-allosteric-modulator
#11
Amruta S Agharkar, Eric B Gonzales
Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems. The ASIC3 subtype is found primarily in the periphery where the channel mediates pain signals caused by ischemia and inflammation. Here, we provide identify 4-chlorophenylguanidine (4-CPG) as an ASIC3 positive allosteric modulator and newest member of the growing group of guanidine modulators of ASICs. Furthermore, the 4-CPG reversed the effects of ASIC3 desensitization...
February 17, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28258822/intra-articular-lentivirus-mediated-gene-therapy-targeting-cracm1-for-the-treatment-of-collagen-induced-arthritis
#12
Shuang Liu, Takeshi Kiyoi, Erika Takemasa, Kazutaka Maeyama
Abnormal store-operated calcium uptake has been observed in peripheral T lymphocytes of rheumatoid arthritis (RA) patients, and sustained intracellular calcium signalling is known to mediate the functions of many types of immune cells. Thus, it is hypothesized that regulating calcium entry through CRACM1 (the pore-forming subunit of calcium release-activated calcium (CRAC) channels; also known as ORAI1) may be beneficial for the management of RA. Localized CRACM1 knockdown in the joints and draining lymph nodes (DLNs) of mice with collagen-induced arthritis (CIA) was achieved via lentiviral-based delivery of shRNA targeting mouse CRACM1...
February 11, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28245963/characterization-of-microminipigs-as-an-in%C3%A2-vivo-experimental-model-for-cardiac-safety-pharmacology
#13
Suchitra Matsukura, Yuji Nakamura, Xin Cao, Takeshi Wada, Hiroko Izumi-Nakaseko, Kentaro Ando, Hiroshi Yamazaki, Atsushi Sugiyama
We pharmacologically characterized microminipigs as an in vivo experimental model by assessing cardiovascular effects of pilsicainide, verapamil and E-4031, which can preferentially inhibit cardiac Na(+), Ca(2+) and K(+) channels, respectively. Intravenous infusion of 1 mg/kg of pilsicainide (n = 4), 0.1 mg/kg of verapamil (n = 4) and 0.01 followed by 0.1 mg/kg of E-4031 (n = 5) over 10 min decreased the heart rate, mean blood pressure and ventricular contractility. Moreover, pilsicainide prolonged the PR interval, QRS width and QTc; verapamil prolonged the PR interval, but shortened the QRS width and QTc; and E-4031 prolonged the QTc, whereas no substantial change was detected in the PR interval or QRS width...
February 11, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28242177/structure-activity-relationship-of-a-novel-series-of-inhibitors-for-cancer-type-transporter-l-type-amino-acid-transporter-1-lat1
#14
Pornparn Kongpracha, Shushi Nagamori, Pattama Wiriyasermkul, Yoko Tanaka, Kazuko Kaneda, Suguru Okuda, Ryuichi Ohgaki, Yoshikatsu Kanai
L-type amino acid transporter 1 (LAT1) is known as a cancer-type amino acid transporter. In cancer cells, LAT1 is responsible for the cellular uptake of many essential amino acids including leucine that activates mechanistic/mammalian target of rapamycin (mTOR), regulating cancer cell growth. In this study, we designed a novel series of LAT1 inhibitors, SKN101-105, based on the structure of triiodothyronine (T3), a known LAT1 blocker. The compounds consist of core structure of 2-amino-3-[3,5-dichloro-4-(naphthalene-1-methoxy)-phenyl]-propanoic acid and different modifications on the naphthalene...
February 9, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28238645/periostin-antisense-oligonucleotide-prevents-adhesion-formation-after-surgery-in-mice
#15
Shinji Takai, Masafumi Yoshino, Kazumasa Takao, Kazunori Yoshikawa, Denan Jin
To study the role of periostin in adhesion formation, the effect of periostin antisense oligonucleotide (PAO) on adhesion formation was evaluated in mice. Under anesthesia, the serous membrane of the cecum was abraded, and the adhesion score and mRNA levels of periostin and its related factors were determined after surgery. Saline, 40 mg/kg of negative sense oligonucleotide (NSO), or 40 mg/kg of PAO were injected into the abdomen after surgery, and the adhesion score and mRNA levels were evaluated 14 days later...
February 9, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28215474/establishment-of-disseminated-intravascular-coagulation-dic-model-by-a-single-iv-administration-of-escherichia-coli-derived-lipopolysaccharide-lps-to-cynomolgus-monkeys-and-evaluation-of-its-pathophysiological-status
#16
Hirofumi Minomo, Kengo Inoue, Shuko Sakaki, Takanobu Okazaki, Kinji Kobayashi, Kazuhiko Inoue, Atsuro Miyata
We prepared a DIC model by administrating LPS to cynomolgus monkeys, and investigated its potential for evaluations of new medicines for DIC therapy. Peripheral blood mononuclear cells (PBMC) collected from cynomolgus monkeys were incubated with LPS (8 types), and TNF-α levels in the media were measured. LPS from Escherichia coli (K-235) was most appropriate in terms of larger increases and smaller variation in TNF-α levels. PBMC from rats, cynomolgus monkeys or humans were incubated with LPS (K-235), and the TNF-α response to LPS was investigated...
February 2, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28209485/effects-of-clozapine-on-adipokine-secretions-productions-and-lipid-droplets-in-3t3-l1-adipocytes
#17
Tomomi Tsubai, Akira Yoshimi, Yoji Hamada, Makoto Nakao, Hiroshi Arima, Yutaka Oiso, Yukihiro Noda
Clozapine, a second-generation antipsychotic (SGA), is a cause of side effects related to metabolic syndrome. The participation of serotonin 5-HT2C and histamine H1 receptors in the central nervous system has been reported as a mechanism of the weight gain caused by clozapine. In the present study, we investigated the direct pharmacological action of clozapine on the 3T3-L1 adipocytes and compared it to that of blonanserin, an SGA with low affinity for both receptors. Short-term exposure to clozapine decreased secretion and mRNA expression of leptin...
January 28, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28233634/serotonergic-and-dopaminergic-systems-are-implicated-in-antidepressant-like-effects-of-chotosan-a-kampo-formula-in-mice
#18
Sachie Sasaki-Hamada, Azusa Suzuki, Yudai Ueda, Kinzo Matsumoto, Jun-Ichiro Oka
We previously demonstrated that chotosan (CTS), a traditional herbal formula called Kampo medicine, improves diabetes-induced cognitive deficits. In the present study, we investigated the antidepressant-like effects of CTS in mice. The administration of CTS (1.0 g/kg, for 3 days) decreased the immobility time in the forced-swim test, and this decrease was prevented by the prior administration of sulpiride (an antagonist of D2/3 receptors) and WAY100635 (an antagonist of 5-HT1A receptors). None of the treatments tested altered the locomotor activity of mice...
January 26, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28237320/a-perspective-on-metabolic-surgery-from-a-gastroenterologist
#19
REVIEW
Yu-Fong Syu, Akio Inui, Chih-Yen Chen
Type 2 diabetes (T2D) and obesity are important public health problems. The global prevalence of diabetes mellitus is 8.8%. Interventional diabetology and obesitology have been recently advocated as treatment options for T2D and obesity. The roles of metabolic surgery such as Roux-en-Y gastric bypass, sleeve gastrectomy, gastric banding, and biliopancreatic diversion are focused. Different types of metabolic surgeries have different glucose-lowering and weight loss effects. Endoscopic treatments include the intra-gastric balloon (to restrict the gastric volume) and duodenal-jejunal bypass liner (DJBL, as a malabsorptive procedure)...
January 19, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28089228/intraplantar-injection-of-sialidase-reduces-mechanical-allodynia-during-inflammatory-pain
#20
Shun Watanabe, Takashi Iwai, Mitsuo Tanabe
Sialic acids are highly charged glycoresidues that are attached to glycoproteins or glycosphingolipids, and they are associated with various biological functions. Gangliosides, sialic acid-containing glycosphingolipids, are abundant in neural tissues and play important roles in the nervous system. Previous studies revealed that peripheral gangliosides are involved in nociceptive behavior and hyperalgesia. These observations prompted us to determine whether the sialic acid-cleaving enzyme sialidase affects pain signaling...
January 3, 2017: Journal of Pharmacological Sciences
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