5,125 results match your criteria Nippon Yakurigaku Zasshi Folia Pharmacologica Japonica[Journal]


[Drug properties of fosravuconazole L-lysine ethanolate (NAILIN Capsules 100 mg), a new oral azole therapeutic for onychomycosis: an analysis based on non-clinical and clinical trial data].

Nihon Yakurigaku Zasshi 2019 ;153(2):79-87

Teikyo University Institute of Medical Mycology.

Ravuconazole is a fourth generation azole exerting strong antifungal activity, with low drug-drug interaction and hepatic dysfunction risks. Fosravuconazole l-lysine ethanolate (fosravuconazole; NAILIN Capsules 100 mg) was developed as a ravuconazole prodrug. Ravuconazole exerts strong antifungal activity against various pathogenic fungi including dermatophytes and Candida. Read More

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http://dx.doi.org/10.1254/fpj.153.79DOI Listing
January 2019

[Personalized medicine for oral molecular-targeted anticancer drugs].

Authors:
Masatomo Miura

Nihon Yakurigaku Zasshi 2019 ;153(2):73-78

Department of Pharmacy, Akita University Hospital.

Therapeutic drug monitoring (TDM) is carried out by evaluating drug plasma (or serum) concentrations in response to individual optimal treatments by dose adjustment to improve efficacy or avoid side effects. Many molecular-targeted anticancer drugs show exposure-efficacy and exposure-toxicity relationships. Therefore, plasma concentrations of anticancer drugs can be used as biomarkers. Read More

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http://dx.doi.org/10.1254/fpj.153.73DOI Listing
January 2019
1 Read

[Molecular understanding of hierarchy and lineage of mesenchymal stem cells in vivo].

Nihon Yakurigaku Zasshi 2019 ;153(2):67-72

Department of Regenerative Science, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences.

Mesenchymal stem cell (MSC) is a type of tissue stem cell. In clinical studies, cultured MSCs have shown important therapeutic effects on diseases via the reduction of neurological defects and regulation of immune responses. However, in vivo MSC localization, function, and properties are poorly understood; therefore, the molecular understanding of MSCs hierarchy is less advanced compared to hematopoietic stem cell hierarchy. Read More

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http://dx.doi.org/10.1254/fpj.153.67DOI Listing
January 2019
1 Read

[Dissecting early development of the kidney by single cell transcriptomics].

Nihon Yakurigaku Zasshi 2019 ;153(2):61-66

Department of Life Science Frontiers, Center for iPS Cell Research and Application, Kyoto University.

Each of the billions of the cells in our body exhibits their identity with unique gene expression profile. Recent advances in single cell transcriptomics enable to conduct cell taxonomy identifying new cell types and to re-arrange cells in order of pseudo-time course describing differentiation status of each cell. Even though the cost is still high, the single cell transcriptomics now becomes one of the conventional assays. Read More

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http://dx.doi.org/10.1254/fpj.153.61DOI Listing
January 2019

[Hypoxia epigenetically bestows astrocytic differentiation potential on human pluripotent cell-derived neural stem/precursor cells].

Nihon Yakurigaku Zasshi 2019 ;153(2):54-60

Department of Stem Cell Biology and Medicine, Graduate School of Medical Sciences, Kyushu University.

The central nervous system (CNS) is composed of three major cell types, neurons, astrocytes, and oligodendrocytes, which differentiate from common multipotent neural stem/precursor cells (NS/PCs). However, NS/PCs do not have this multipotentiality from the beginning: neurons are generated first and astrocytes are later during CNS development. This developmental progression is observed in vitro by using human (h) NS/PCs derived from pluripotent cells, such as embryonic- and induced pluripotent-stem cells (ES/iPSCs), however, in contrast to rodent's pluripotent cells, they require quite long time to obtain astrocytic differentiation potential. Read More

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http://dx.doi.org/10.1254/fpj.153.54DOI Listing
January 2019
1 Read

[MPMBP, a novel bisphosphonate with an antioxidant side chain, stimulates bone formation through inhibition of NF-κB nuclear translocation].

Nihon Yakurigaku Zasshi 2019 ;153(1):4-10

Center for Environmental Dentistry, Graduate School of Dentistry, Tohoku University.

Bisphosphonates (BPs) are chemically characterized by a P-C-P bond with two lateral side chains on the carbon atom, and have been widely used as anti-resorptive agents in various metabolic bone diseases. 4-[(methylthio) phenylthio] methanebisphosphonate (MPMBP) is a novel non-nitrogen-containing BP with an antioxidant side chain that possesses anti-inflammatory properties. Since inflammation is known to be a cause of the pathological bone resorption, we investigated the effects of MPMBP on bone metabolism both in vitro and in vivo. Read More

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http://dx.doi.org/10.1254/fpj.153.4DOI Listing
January 2019

[Pharmacological profiles and clinical effects of amenamevir tablet as treatments for herpes zoster].

Nihon Yakurigaku Zasshi 2019 ;153(1):35-43

Medical Affairs Department, Maruho Co., Ltd.

Herpes zoster is a viral infectious disease caused by reactivation of varicella zoster virus (VZV) in a latently infected ganglion, and is characterized by blistering and pain developing in a zonal region innervated from the ganglion. Amenamevir is an antiherpes agent that does not have a nucleic acid-like structure, and exerts antiviral action by inhibiting the enzymatic activity of a virus-derived helicase-primase complex, which is considered essential for viral DNA replication. Amenamevir is mainly metabolized by CYP3A, and excreted into feces. Read More

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http://dx.doi.org/10.1254/fpj.153.35DOI Listing
January 2019
1 Read

[Translational behavioral research using common marmosets in the psychiatric field].

Nihon Yakurigaku Zasshi 2019 ;153(1):28-34

Higher Brain Function Research, Drug Research Division, Sumitomo Dainippon Pharma Co., Ltd.

The drug discovery activities for novel compounds with the superior efficacies to current drugs have been largely unsuccessful in the psychiatric field. One of the main reasons is the lack of appropriate behavioral assays and animal models for psychiatric disorders. Since the prefrontal cortex has great roles in their pathophysiology, non-human primate common marmosets with the well-developed prefrontal cortex would be useful as experimental animals in the future translational research. Read More

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http://dx.doi.org/10.1254/fpj.153.28DOI Listing
January 2019
3 Reads

[Current situation and future issues of antiresorptive agent-related osteonecrosis of the jaw].

Nihon Yakurigaku Zasshi 2019 ;153(1):22-27

Department of Dentistry and Oral Surgery, Hyogo College of Medicine.

Bisphosphonate-related osteonecrosis of the jaw (BRONJ), which is characterized by refractory bone exposure, has recently emerged as a serious side effect of bisphosphonate (BP) treatment. BRONJ was first thought to be due to administration of high doses of intravenous BP to treat metastatic bone lesions or multiple myeloma. However, more recent studies have indicated that BRONJ also frequently occurs in patients receiving low doses of BP for the treatment of osteoporosis. Read More

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http://dx.doi.org/10.1254/fpj.153.22DOI Listing
January 2019
1 Read

[Anabolic action of teriparatide to osteoporotic patients].

Nihon Yakurigaku Zasshi 2019 ;153(1):16-21

Developmental Biology of Hard Tissue, Faculty of Dental Medicine, Hokkaido University.

Intermittent administration of human parathyroid hormone (PTH) [1-34], or teriparatide, has been used for osteoporotic treatment, which is available for daily and weekly administration for the osteoporotic patients in Japan, increasing bone mass and reduce bone fracture risk. In general, continuous PTH infusion shows catabolic effects in bone, while the intermittent administration of PTH results in anabolic action in osteoporotic patients. Intermittent PTH administration promotes preosteoblastic proliferation, as well as stimulates osteoblastic bone formation dependent on cell coupling with osteoclasts. Read More

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http://dx.doi.org/10.1254/fpj.153.16DOI Listing
January 2019

[The mechanism of anti-RANKL antibody in the treatment of metabolic bone diseases including osteoporosis - possible applications of anti-RANKL antibody to the treatment of cancer patients].

Authors:
Hisataka Yasuda

Nihon Yakurigaku Zasshi 2019 ;153(1):11-15

Nagahama Institute for Biochemical Science, Oriental Yeast Co., Ltd.

Discovery of RANKL (receptor activator of NF-κB ligand) gave a great impact on identification of the mechanisms regulating osteoclast differentiation and function, establishment of research field bridging bone and mineral research and immunology (osteoimmunology), and development of a fully human anti-RANKL monoclonal neutralizing antibody (denosumab). Denosumab has been clinically available for treatment of osteoporosis and cancer-induced bone diseases in the US, Europe and many countries including Japan. Denosumab is a so-called blockbuster of which sales amount was 3. Read More

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http://dx.doi.org/10.1254/fpj.153.11DOI Listing
January 2019

[The 139th Regional Meeting (Kanto Area)].

Authors:

Nihon Yakurigaku Zasshi 2019 ;153(Supplement):S56-S88

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http://dx.doi.org/10.1254/fpj.153.S56DOI Listing
January 2019

[The 69th Regional Meeting (Kita Area)].

Authors:

Nihon Yakurigaku Zasshi 2019 ;153(Supplement):S1-S55

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http://dx.doi.org/10.1254/fpj.153.S1DOI Listing
January 2019

[Pharmacological profile and clinical findings of palbociclib (IBRANCE capsule 25 mg/125 mg)].

Nihon Yakurigaku Zasshi 2018;152(6):306-318

Medical Affairs Oncology, Pfizer Japan Inc.

Palbociclib is the world's first cyclin dependent kinase (CDK) 4 and 6 inhibitor. It's believed that palbociclib stops the cell cycle progression by inhibiting the activity of the complex consisting of CDK 4/6 and cyclin D, and suppresses tumor growth. In preclinical study using nonclinical model, it was confirmed that most of the cell lines sensitive to palbociclib are estrogen receptor (ER) positive. Read More

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http://dx.doi.org/10.1254/fpj.152.306DOI Listing
January 2018
1 Read

[Dysfunction of Na/Ca exchangers is associated with cognitive decline in Alzheimer's disease].

Nihon Yakurigaku Zasshi 2018;152(6):299-305

Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Tohoku University.

Na/Ca exchanger (NCX) is mainly expressed in the plasma membrane and mediates electrogenical exchange of one Ca for three Na, depending on the electrochemical gradients across the plasma membrane. NCX has three different isoforms (NCX1, NCX2, NCX3) encoded by distinct genes in mammals. Here, we report that NCX2 and NCX3 protein levels are relatively reduced in hippocampal CA1 of Alzheimer's disease model mice. Read More

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http://dx.doi.org/10.1254/fpj.152.299DOI Listing
January 2018
6 Reads

[Homeostatic regulation of basal ganglia circuit for flexible behavior].

Authors:
Takatoshi Hikida

Nihon Yakurigaku Zasshi 2018;152(6):295-298

Laboratory for Advanced Brain Functions, Institute for Protein Research, Osaka University.

Behavioral inflexibility has been reported in various psychiatric disorders including drug addiction and schizophrenia. Considerable evidence has demonstrated a critical role for the basal ganglia in the flexibility of behavioral strategies. These processes are guided by the activity of two discrete neuron types, dopamine D1- or D2-receptor expressing medium spiny neurons (D1-/D2-MSNs) in the basal ganglia circuit. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/6/152_295/_arti
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http://dx.doi.org/10.1254/fpj.152.295DOI Listing
January 2018
8 Reads

[Consideration for future in vitro BBB models - technical development to investigate the drug delivery to the CNS].

Authors:
Kaoru Sato

Nihon Yakurigaku Zasshi 2018;152(6):287-294

National Institute of Health Sciences.

Blood vessels in the central nervous system (CNS) limit the material exchange between blood and parenchyma by blood brain barrier (BBB). At present, no appropriate in vitro BBB models are available for the investigation whether or not the candidate compounds for new drugs could be delivered to the CNS. This causes huge difficulties of the development of CNS drugs and prediction of CNS adverse effects. Read More

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http://dx.doi.org/10.1254/fpj.152.287DOI Listing
January 2018

[DEPDC5, a new key to understand various epilepsies].

Authors:
Saeko Ishida

Nihon Yakurigaku Zasshi 2018;152(6):281-285

Laboratory of Molecular Neuroscience, Medical Research Institute (MRI), Tokyo Medical and Dental University (TMDU).

Epilepsy is one of the most frequent neurological disorders characterized by spontaneous and recurrent seizures. Most seizures last for the lifetime and the patients require long term therapies. However, about 30% of the patients are refractory to antiepileptic drugs. Read More

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http://dx.doi.org/10.1254/fpj.152.281DOI Listing
January 2018

[Function of synaptic vesicle protein 2A (SV2A) as a novel therapeutic target for epilepsy].

Nihon Yakurigaku Zasshi 2018;152(6):275-280

Department of Pharmacology, Osaka University of Pharmaceutical Sciences.

Epilepsy is a chronic neurologic disease characterized by recurrent seizures, affecting nearly 1% of the population. Synaptic vesicle protein 2A (SV2A) is a membrane protein specifically expressed in synaptic vesicles and is now implicated in the pathogenesis of epileptic disorders. This is because 1) Sv2a-knockout mice exhibit severe seizures, 2) SV2A serves as a specific binding site for certain antiepileptics (e. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/6/152_275/_arti
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http://dx.doi.org/10.1254/fpj.152.275DOI Listing
January 2018
2 Reads

[Epileptogenesis mediated by glial cells].

Nihon Yakurigaku Zasshi 2018;152(6):268-274

Department of Pediatrics, Interdisciplinary Graduate School of Medicine, University of Yamanashi.

Epilepsy is one of the most common diseases of the central nervous system. Many epilepsies are controllable because of the existence of different antiepileptic drugs with multiple mechanisms of action. However, about 30% of epilepsy is so-called refractory epilepsy in which existing drugs do not show enough therapeutic effects. Read More

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http://dx.doi.org/10.1254/fpj.152.268DOI Listing
January 2018

[Regulation of adventitial fibroblast functions in pulmonary hypertension].

Authors:
Muneyoshi Okada

Nihon Yakurigaku Zasshi 2018 ;152(5):258

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http://dx.doi.org/10.1254/fpj.152.258DOI Listing
January 2018

[Current situation of diagnosis for food allergy].

Nihon Yakurigaku Zasshi 2018 ;152(5):256-257

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http://dx.doi.org/10.1254/fpj.152.256DOI Listing
January 2018

[Pharmacological profile and clinical efficacy of transdermal patch containing emedastine difumarate (ALLESAGA TAPE)].

Nihon Yakurigaku Zasshi 2018 ;152(5):246-255

Research and Development Division, Hisamitsu Pharmaceutical Co., Inc.

ALLESAGA TAPE is the first transdermal drug delivery system of emedastine difumarate, as a second-generation antihistamine, for allergic rhinitis. It has been suggested that the efficacy of emedastine difumarate in allergic rhinitis is mediated through a combination of chemical mediator release inhibitory effects and eosinophil chemotaxis inhibitory effects, in addition to a strong anti-histaminic effect. In the pharmacological evaluation on histamine-induced vascular hyperpermeability in rats, ALLESAGA TAPE showed an anti-histaminic effect in a dose-dependent manner and exhibited a long-lasting anti-histaminic effect until 24 hours after administration. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/5/152_246/_arti
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http://dx.doi.org/10.1254/fpj.152.246DOI Listing
January 2018
9 Reads

[Establishment of a novel evaluation system for dopaminergic axonal outgrowth and its regulatory factor].

Authors:
Yasuhiko Izumi

Nihon Yakurigaku Zasshi 2018 ;152(5):240-245

Laboratory of Pharmacology, Kobe Pharmaceutical University.

The nigrostriatal dopaminergic pathway is implicated with Parkinson's disease. Elucidation of this projection mechanism is not only important for considering developmental brain formation, but also contributes to the development of a therapy for regenerating the lost neural circuit. Although several axon guidance cues have been reported to induce dopaminergic axons from the substantia nigra to the striatum, the mechanisms by which the dopaminergic axons extend in the striatum remain unclear. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/5/152_240/_arti
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http://dx.doi.org/10.1254/fpj.152.240DOI Listing
January 2018
9 Reads

[Pathophysiological functions of gas mediators in neurodegeneration].

Authors:
Yoshinori Mikami

Nihon Yakurigaku Zasshi 2018 ;152(5):233-239

Department of Physiology, Faculty of Medicine, Toho University.

Since the discovery of nitric oxide (NO) as gaseous signaling molecule, two other gaseous mediators, carbon monoxide (CO) and hydrogen sulfide (HS) have been found to be also involved in many physiological and pathophysiological functions. This review will briefly summarize our recent progress in the pathophysiology of NO and HS. In the photoreceptor cells, the level of intracellular Ca is kept relatively low by HS. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/5/152_233/_arti
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http://dx.doi.org/10.1254/fpj.152.233DOI Listing
January 2018
9 Reads

[Physiological roles of redox signals in relation to synaptic plasticity and brain functions].

Authors:
Sho Kakizawa

Nihon Yakurigaku Zasshi 2018 ;152(5):227-232

Department of Biological Chemistry, Graduate School of Pharmaceutical Sciences, Kyoto University.

In our classical knowledge, redox molecules, including reactive oxygen species (ROS), nitric oxide (NO) and hydrogen sulfide, are considered to be generated as byproducts of aerobic metabolism and act as harmful oxidants of macromolecules, such as proteins and lipids. On the other hands, recently, expressions of enzymes producing redox molecules are identified and reported to be expressed in wide range of tissues, including brain. Moreover, activities of some of these enzymes are revealed to be regulated by physiological signals (e. Read More

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http://dx.doi.org/10.1254/fpj.152.227DOI Listing
January 2018

[Development and application of a novel thiol labeling reagent for protein thiol analysis].

Authors:
Yuki Tatenaka

Nihon Yakurigaku Zasshi 2018 ;152(5):223-226

Dojindo Laboratories.

Modification of protein thiol is one of the most important post-translational modifications and it occurs depending on the redox state in cells. Protein S-nitrosylation is NO (nitric oxide)-dependent modification of protein thiols and is crucial for regulation of cellular functions such as transcription, protein expression, and signal transduction. Maleimide reagents are generally used to assess the redox status of the thiols in a protein of interest. Read More

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http://dx.doi.org/10.1254/fpj.152.223DOI Listing
January 2018

[Production of HS, HS, and persulfide species (CysSSH and GSSH) by 3-mercaptopyruvate sulfurtransferase].

Authors:
Norihiro Shibuya

Nihon Yakurigaku Zasshi 2018 ;152(5):216-222

National Institute of Neuroscience, National Center of Neurology and Psychiatry.

Accumulating evidence shows that hydrogen sulfide (HS) has physiological roles in various tissues and organs, including the regulation of neuronal activity, vascular tension, a release of insulin, and protection of the heart, kidney, and brain from ischemic insult. HS is produced from l-cysteine by pyridoxal 5'-phosphate (PLP)-dependent enzymes, cystathionine β-synthase (CBS) and cystathionine γ-lyase (CSE). 3-Mercaptopyruvate sulfurtransferase (3MST) is the third HS-producing enzyme, and its substrate 3-mercaptopyruvate (3MP) is provided from l-cysteine and α-ketoglutarate (α-KG) by a PLP-dependent cysteine aminotransferase (CAT). Read More

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https://www.jstage.jst.go.jp/article/fpj/152/5/152_216/_arti
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http://dx.doi.org/10.1254/fpj.152.216DOI Listing
January 2018
6 Reads

[Anti-inflammatory action of the transcription factor Nrf2].

Authors:
Yasuhiko Izumi

Nihon Yakurigaku Zasshi 2018 ;152(4):209

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http://dx.doi.org/10.1254/fpj.152.209DOI Listing
January 2018

[Extracellular matrix biomarkers for cardiac diseases].

Authors:
Muneyoshi Okada

Nihon Yakurigaku Zasshi 2018 ;152(4):208

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http://dx.doi.org/10.1254/fpj.152.208DOI Listing
January 2018

[Current progress of research and use of microminipigs in drug development].

Nihon Yakurigaku Zasshi 2018 ;152(4):202-207

Swine and Poultry Department, Shizuoka Prefectural Research Institute of Animal Industry, Swine and Poultry Research Center.

The use of minipigs has been increasing in the areas of pharmacology researches and drug development. The microminipig developed by Fuji Micra Inc. (Shizuoka, Japan) inherits characteristics of other pig strains showing several similarities to humans in anatomy, physiology, omnivorousness and diurnal, but at the same time has several advantages over other pig strains because of its small size which allows easy keeping, handling and dosing, and saving of test substances. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/4/152_202/_arti
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http://dx.doi.org/10.1254/fpj.152.202DOI Listing
January 2018
1 Read

[Neurological mechanism and therapeutic strategy for posttraumatic stress disorders].

Nihon Yakurigaku Zasshi 2018 ;152(4):194-201

Department of Pharmacology, Tohoku University Graduate School of Pharmaceutical Sciences.

Posttraumatic stress disorder (PTSD) is most often induced by traumatic events and serious public health problems. PTSD is characterized by excessive response to contextual memory and impaired fear extinction and also associated with mild cognitive impairment, attention and learning deficits. Clinical and animal studies suggest that increased susceptibility of emotion- and fear-related neuronal circuits, including those in the amygdala, prefrontal cortex and hippocampus, contributes to development and retention of PTSD symptoms. Read More

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http://dx.doi.org/10.1254/fpj.152.194DOI Listing
January 2018
3 Reads

[Gut microbiota and nonalcoholic steatohepatitis].

Nihon Yakurigaku Zasshi 2018 ;152(4):187-193

Department of Gastroenterology and Hepatology, Yokohama City University School of Medicine.

Nonalcoholic fatty liver disease (NAFLD), especially nonalcoholic steatohepatitis (NASH), is a disease that may lead to liver cirrhosis or hepatocellular carcinoma. The number of patients is increasing steadily and the pathology is diverse. Effective treatment is still mainly focused on diet and exercise therapy. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/4/152_187/_arti
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http://dx.doi.org/10.1254/fpj.152.187DOI Listing
January 2018
11 Reads

[The involvement of NOX1/NADPH oxidase in the development of non-alcoholic steatohepatitis].

Authors:
Misaki Matsumoto

Nihon Yakurigaku Zasshi 2018 ;152(4):181-186

Department of Pharmacology, Kyoto Prefectural University of Medicine.

Reactive oxygen species (ROS) are known to play a critical role in the development of non-alcoholic steatohepatitis (NASH). To clarify the source of ROS, we examined the expression of superoxide-generating NADPH oxidase isoforms in the liver of high-fat and high-cholesterol (HFC) diet-fed mice. The mRNA expression of NOX1 was significantly elevated in mice on HFC diet for 8 weeks. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/4/152_181/_arti
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http://dx.doi.org/10.1254/fpj.152.181DOI Listing
January 2018
2 Reads

[Recent progress in the research of Eosinophilic GastroIntestinal Diseases (EGIDs)].

Nihon Yakurigaku Zasshi 2018 ;152(4):175-180

Department of Gastroenterology and Hepatology, Shimane University, Faculty of Medicine.

Eosinophilic esophagitis (EoE) and eosinophilic gastroenteritis (EGE), which are included in eosinophilic gastrointestinal disorders (EGIDs), are allergic gastrointestinal diseases mainly caused by food allergens, which features dense infiltration of eosinophiles in the gastrointestinal mucosa. A possible mechanism of these diseases are Th2 type allergic reactions, including IL-5, IL-13, and IL-15, thymic stromal protein (TSLP), and eotaxin 3, which are considered to have important roles. The number of patients with EoE is rapidly increasing in both Western and Asian countries. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/4/152_175/_arti
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http://dx.doi.org/10.1254/fpj.152.175DOI Listing
January 2018
3 Reads

[TRPV4 regulates vascular endothelial permeability during colonic inflammation in dextran sulphate sodium-induced murine colitis].

Nihon Yakurigaku Zasshi 2018 ;152(4):170-174

Division of Pathological Sciences, Department of Pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University.

The transient receptor potential vanilloid 4 (TRPV4) is a nonselective cation channel involved in physical sensing in various tissue types. The present study aimed to elucidate the function and expression of TRPV4 in colonic vascular endothelial cells during dextran sulphate sodium (DSS)-induced colitis. The role of TRPV4 in the progression of colonic inflammation was examined in the 2% DSS-induced murine colitis model using immunohistochemical analysis, Western blotting, and Evans blue dye extrusion assay. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/4/152_170/_arti
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http://dx.doi.org/10.1254/fpj.152.170DOI Listing
January 2018
1 Read

[The 133th Regional Meeting (Kinki Area)].

Authors:

Nihon Yakurigaku Zasshi 2018 ;152(Supplement):S109-S142

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http://dx.doi.org/10.1254/fpj.152.S109DOI Listing
January 2018

[Pharmacological and clinical profile of spinal muscular atrophy (SMA) therapeutic drug nusinersen (Spinraza)].

Nihon Yakurigaku Zasshi 2018 ;152(3):147-159

President and representative director, Biogen Japan Ltd.

Nusinersen (Spinraza) was approved as Japan's first antisense oligonucleotide (ASO) drug for treatment of SMA (spinal muscular atrophy) patients with a deletion or mutation of the survival motor neuron (SMN) 1 gene and ≥1 copy of the SMN2 gene. Nuseinersen is a fully modified 2'-O-(2-methoxyethyl) (2'-MOE) ASO designed to bind the SMN2 pre-mRNA and alter splicing, such that a mature mRNA is produced and is translated as full-length SMN protein. In 4 types of mouse SMA disease models, treatment with nusinersen improved the form of the neuromuscular junction, increased myofiber size, improved righting reflex and grip, and prolonged survival. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/3/152_147/_arti
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http://dx.doi.org/10.1254/fpj.152.147DOI Listing
January 2018
15 Reads

[Establishment of retinal disease models using non-human primates and its strategy for drug discovery].

Nihon Yakurigaku Zasshi 2018 ;152(3):139-146

Molecular Pharmacology, Department of Biofunctional Evaluation, Gifu Pharmaceutical University.

Retinal diseases such as glaucoma, diabetic retinopathy, age-related macular degeneration and retinitis pigmentosa are the major causes of blindness. However, these pathological mechanisms remain to be elucidated, and development of new therapeutic agents has been desired. A large number of experimental animal models using rodents (rats and mice) have been used for the evaluations of the pathogenesis and novel therapeutic candidates in retinal diseases. Read More

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http://dx.doi.org/10.1254/fpj.152.139DOI Listing
January 2018
1 Read

[Pharmacological profile of a novel nonhuman primate model of knee osteoarthritis].

Nihon Yakurigaku Zasshi 2018 ;152(3):132-138

Pharmacology Group, Hamamatsu Pharma Research, Inc.

A number of promising compounds developed in rodent arthritis models lack efficacy in clinical osteoarthritis (OA) pain. To enhance successful translation of preclinical findings, a nonhuman primate (NHP) model of knee OA was developed and characterized using behavioral assessments designed for use in the NHP. A unilateral medial meniscectomy (MMx) was performed and animals underwent an exercise regimen. Read More

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http://dx.doi.org/10.1254/fpj.152.132DOI Listing
January 2018
3 Reads

[Muscle mass measurement by DXA and MRI in non-human primates].

Nihon Yakurigaku Zasshi 2018 ;152(3):126-131

Shin Nippon Biomedical Laboratories, Ltd. Drug Safety Research Laboratories (SNBL DSR).

The global population is aging rapidly and, in Japan, the number of elderly has been steadily rising. It is important to shrink the gap between the average lifespan and the number of years people can expect to remain healthy. This links with improving the quality of life for the elderly and reducing social welfare spending. Read More

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http://dx.doi.org/10.1254/fpj.152.126DOI Listing
January 2018

[The role of pharmacology to produce firuglipel (DS-8500a), an orally available GPR119 agonist for type 2 diabetes mellitus].

Nihon Yakurigaku Zasshi 2018 ;152(3):119-124

Daiichi Sankyo RD Novare, Co., Ltd.

GPR119 (G-protein coupled receptor 119) has been shown to be highly expressed in the lower small intestinal and colorectal L-cells and pancreatic β-cells, and mediates intracellular cAMP concentration, glucagon like peptide (GLP-1) secretion, and glucose stimulated insulin secretion (GSIS). As the next generation for the treatment of type 2 diabetes mellitus (T2DM), GPR119 agonist has been intensively studied by pharmaceutical companies and a lot of patents have been applied by them. In such highly competitive condition, biological differentiation and to find an advantage among GPR119 agonists were necessary to proceed the candidate compound in further clinical investigation. Read More

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http://dx.doi.org/10.1254/fpj.152.119DOI Listing
January 2018
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[Contribution of pharmacological research to the discovery of a first-in-class drug, mirabegron, for the treatment of overactive bladder].

Nihon Yakurigaku Zasshi 2018 ;152(3):111-118

Research Program Management, Drug Discovery Research, Astellas Pharma Inc.

Overactive bladder (OAB) is defined as urgency, with or without urge incontinence, usually with frequency and nocturia. Antimuscarinic drugs are often prescribed as a standard care; however, the treatment discontinuation due to the adverse events including dry mouth and constipation has been an issue. Taking these situations into account, we considered that a novel OAB drug having a different mechanism from antimuscarinics fills the unmet medical need. Read More

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http://dx.doi.org/10.1254/fpj.152.111DOI Listing
January 2018
9 Reads

[Pharmacological characteristics and clinical efficacies of a novel potassium-competitive acid blocker, vonoprazan fumarate].

Nihon Yakurigaku Zasshi 2018 ;152(3):104-110

Gastroenterology Drug Discovery Unit, Research, Takeda Pharmaceutical Company Limited.

Proton pump inhibitors (PPIs) inhibit H, K-ATPase, an enzyme which is the final step of gastric acid secretion and is selectively located in the gastric parietal cells. PPIs block the enzyme in a covalent and irreversible binding manner, thus providing better efficacy than previous pharmacological agents such as antacids and histamine H receptor antagonists. Although PPIs have been the first-line therapeutic option for acid related diseases (ARDs), there are several limitations to their efficacy, i. Read More

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http://dx.doi.org/10.1254/fpj.152.104DOI Listing
January 2018
1 Read

[Usage of common marmoset to drug discovery research].

Authors:
Erika Sasaki

Nihon Yakurigaku Zasshi 2018 ;152(2):94-99

Central Institute for Experimental Animals.

Rodent laboratory animals, such as mice and rats have been greatly contributing to biomedical research. Although its usefulness would not change in the future, nonhuman primates (NHPs) also offer excellent models for preclinical research to assess safety and efficacy of developing novel therapeutic approaches because of their similarities of genetics, metabolism and physiological characteristics to humans. Recent years, the gene modification technology in nonhuman primates has been developed. Read More

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https://www.jstage.jst.go.jp/article/fpj/152/2/152_94/_artic
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http://dx.doi.org/10.1254/fpj.152.94DOI Listing
January 2018
10 Reads

[Importance of diacylglycerol signaling in cerebellar motor coordination].

Nihon Yakurigaku Zasshi 2018 ;152(2):90-93

Applied Chemistry in Bioscience Division, Agrobioscience, Graduate School of Agricultural Science.

Brain can be roughly divided into two parts, cerebrum and cerebellum. Cerebrum controls higher brain functions including memory, emotion and cognition, while cerebellum is important for motor coordination. The only output neuron in cerebellum, Purkinje cell, regulates long term depression (LTD). Read More

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http://dx.doi.org/10.1254/fpj.152.90DOI Listing
January 2018
13 Reads

[Functional roles of phosphotyrosine adaptor Shc in the brain].

Authors:
Sho Kakizawa

Nihon Yakurigaku Zasshi 2018 ;152(2):84-89

Department of Biological Chemistry, Graduate School of Pharmaceutical Sciences, Kyoto University.

Adaptor molecules (adaptor proteins) have indispensable roles in cellular signaling, essential for cellular proliferation, development and metabolism. Shc (Src homology and collagen homology)-family molecule is a group of adaptor molecules, and indicated to be involved in intracellular phosphotyrosine signaling. Shc family has 4 subtypes, ShcA-ShcD, and there are long and short isoforms in ShcA and ShcC whereas ShcB and ShcD have short isoform only. Read More

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http://dx.doi.org/10.1254/fpj.152.84DOI Listing
January 2018