نتایج جستجو برای: tak

تعداد نتایج: 2900  

2017
Lili Pan Juan Du Taotao Li Hua Liao

BACKGROUND Platelet-to-lymphocyte ratio (PLR) and neutrophil-to-lymphocyte ratio (NLR) have been reported to reflect the inflammatory response and disease activity in a variety of autoimmune diseases. OBJECTIVES This study aimed to evaluate the value of PLR and NLR as markers to monitor disease activity in Takayasu's arteritis (TAK). METHODS A retrospective case-control study involving 88 p...

2018
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 t...

Journal: :The Journal of pharmacology and experimental therapeutics 2016
Eri Shiraishi Kazunori Suzuki Akina Harada Noriko Suzuki Haruhide Kimura

Cognitive deficits in various domains, including recognition memory, attention, impulsivity, working memory, and executive function, substantially affect functional outcomes in patients with schizophrenia. 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 potent and selective phosphodiesterase 10A inhibitor that produces antipsychoti...

Journal: :Molecular pharmacology 2007
Trudy A Kohout Qiu Xie Shelby Reijmers Kenneth J Finn Zhiqiang Guo Yun-Fei Zhu R Scott Struthers

Drugs that exhibit insurmountable antagonism are proposed to provide improved clinical efficacy through extended receptor blockade. Long-term suppression of the gonadotropin-releasing hormone receptor (GnRHR) is an important therapeutic approach for a number of sex hormone-dependent diseases. In this study, we describe the mechanism and structural components required for insurmountable activity...

Journal: :The Journal of pharmacology and experimental therapeutics 1999
K Notoya H Nagai T Oda M Gotoh T Hoshino H Muranishi S Taketomi T Sohda H Makino

TAK-778 [(2R,4S)-(-)-N-(4-diethoxyphosphorylmethylphenyl)-1,2,4, 5-tetrahydro-4-methyl-7, 8-methylenedioxy-5-oxo-3-benzothiepin-2-carboxyamide; mw 505.53], a novel osteoblast differentiation promoting compound, was characterized in vitro and in vivo models. TAK-778 at doses of 10(-6) M and higher promoted potently bone-like nodule formation in the presence of dexamethasone in rat bone marrow st...

Journal: :Rheumatology 2013
Neslihan Yilmaz Meryem Can Fatma Alibaz Oner Melike Kalfa Hakan Emmungil Omer Karadag Fatih Yildiz Gezmis Kimyon Baris Yilmazer Vedat Gerdan Sule Yasar Bilge Birkan Ilhan Veli Cobankara Timucin Kasifoglu Ayse Cefle Bunyamin Kisacik Ahmet Mesut Onat Servet Akar Fatos Onen Eren Erken Sedat Kiraz Kenan Aksu Gokhan Keser Gonca Mumcu Haner Direskeneli

OBJECTIVE Patient-reported outcomes (PROs) are increasingly accepted to be among the major tools for outcome assessment in rheumatic disorders. In this study we aimed to assess quality of life (QoL), disability, anxiety and depression in patients with Takayasu's arteritis (TAK). METHODS Patients followed with the diagnosis of TAK (n = 165) and healthy controls (HCs) (n = 109) were enrolled to...

2015
Kazunori Suzuki Akina Harada Eri Shiraishi Haruhide Kimura

Phosphodiesterase 10A (PDE10A) is a cAMP/cGMP phosphodiesterase highly expressed in medium spiny neurons (MSNs) in the striatum. We evaluated the in vivo pharmacological profile of a potent and selective PDE10A inhibitor, TAK-063 (1-[2-fluoro-4(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one). TAK-063 at 0.3 and 1 mg/kg p.o., increased cAMP and cGMP levels in t...

Journal: :The Journal of pharmacology and experimental therapeutics 2002
Kalina Venkova D M Sutkowski-Markmann B Greenwood-Van Meerveld

Pathways controlling gastrointestinal function involve the activation of neurokinin NK1 receptors by substance P (SP) under normal and pathological conditions. Our aim was to pharmacologically characterize the effect of a nonpeptide NK1 receptor antagonist TAK-637 [(aR,9R)-7-[3,5-bis(trifluoromethyl)benzyl]-8,9,10,11-tetrahydro-9-methyl-5-(4-methylphenyl)-7H-[1,4]diazocino[2,1-g] [1,7]naphthyri...

2013
Tomomi TANAKA Satoshi OHKURA Yoshihiro WAKABAYASHI Takenobu KUROIWA Kiyosuke NAGAI Natsumi ENDO Akira TANAKA Hisanori MATSUI Masami KUSAKA Hiroaki OKAMURA

The aim of the present study was to determine if the estradiol-induced luteinizing hormone (LH) surge is influenced by the constant exposure to TAK-683, an investigational metastin/kisspeptin analog, that had been established to depress the pulsatile gonadotropin-releasing hormone (GnRH) and LH secretion in goats. Ovariectomized goats subcutaneously received TAK-683 (TAK-683 group, n=6) or vehi...

2015
Akina Harada Kazunori Suzuki Naomi Kamiguchi Maki Miyamoto Kimio Tohyama Kosuke Nakashima Takahiko Taniguchi Haruhide Kimura

Phosphodiesterase 10A (PDE10A) inhibition is a novel and promising approach for the treatment of central nervous system disorders such as schizophrenia and Huntington's disease. A novel PDE10A inhibitor, TAK-063 [1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)-pyridazin-4(1H)-one] has shown high inhibitory activity and selectivity for human recombinant PDE10A2 in v...

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