Search Results 1-20 of 156

  • Design, Synthesis, and Structure–Activity Relationships Study of <i>N</i>-Pyrimidyl/Pyridyl-2-thiazolamine Analogues as Novel Positive Allosteric Modulators of M<sub>3</sub> Muscarinic Acetylcholine Receptor

    Tanaka Hiroaki , Takahashi Taisuke , Akaiwa Michinori , Negoro Kenji , Kawaminami Eiji , Mihara Hisashi , Fuji Hideyoshi , Okimoto Risa , Ino Katsutoshi , Ishizu Kenichiro

    … mAChR with excellent subtype selectivity. … also showed a distinct pharmacological effect on isolated smooth muscle tissue from rat bladder and favorable pharmacokinetics profiles, suggesting its potential as a chemical tool for probing the M<sub>3</sub> …

    Chemical and Pharmaceutical Bulletin 69(4), 360-373, 2021

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  • Development of Porphyrin Derivatives for Theranostics  [in Japanese]

    Hirohara Shiho

    <p>高齢化社会が進む中,がんによる死亡数は年々増加傾向にある.そのため,完治可能な期間でのがん(早期がん)の発見と,高齢の患者に対応した非常に低侵襲性で非観血的ながん治療,またがん診断とがん治療を同時に行うことができるセラノスティクスの確立が求められている.本論文ではセラノスティクス薬剤の開発として,高いPDT効果と速い腫瘍集積性を有するP(Glc)<sub>2</ …

    Nippon Laser Igakkaishi 41(4), 394-401, 2021

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  • Development of Tumor-targeting Antitumor Agents Based on Polymer Effect  [in Japanese]

    Nakamura Hideaki

    … The P-ZnPP suppressed tumor growth by local generation of cytotoxic singlet oxygen, and the tumor tissue was visualized by fluorescence upon light irradiation. … Subsequently, a two-step mechanism for tumor selectivity was observed for the cytotoxic anthracycline, pirarubicin (THP), which conjugated the HPMA-based copolymer <i>via</i> …

    YAKUGAKU ZASSHI 140(10), 1243-1249, 2020

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  • Pharmacological profile, clinical efficacy, and safety of esaxerenone (Minnebro<sup>®</sup> tablets 1.25 mg, 2.5 mg, 5 mg)  [in Japanese]

    Yamakawa Satoru , Homma Tsuyoshi , Yamada Makiko , Igawa Yoshiyuki , Yoshimura Motonobu

    <p>エサキセレノンは,非ステロイド型の新規選択的ミネラルコルチコイド受容体拮抗薬(MRブロッカー)であり,従来のステロイド構造のMR拮抗薬とは異なるMR複合体を形成し,より強いMR拮抗作用と高いMR選択性を発揮する.In vivoでは,尿細管MRの活性化の指標である尿中ナトリウム/カリウム比を低下させ,食塩感受性高血圧モデルでは食塩負荷に伴う血圧上昇,尿中蛋白排泄の上昇及び腎臓の組織 …

    Folia Pharmacologica Japonica 155(5), 340-350, 2020

    J-STAGE  Ichushi Web 

  • Overview of recent GPCR research  [in Japanese]

    Kurose Hitoshi

    … GPCR research starts from analysis of the tissue responses by agonist stimulation. … Although crystallization of GPCR has resolved many important issues of GPCRs, there are many unresolved issues such as structural basis of G protein selectivity and drug design based on structural information. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society 93(0), 3-S28-1, 2020

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  • Development of a novel chemical tag tool for calcium imaging by near-infrared fluorescence  [in Japanese]

    Yuki Isono , Asanuma Daisuke , Okubo Yohei , Namiki Shigeyuki , Hirose Kenzo

    … imaging because of its high tissue penetration, low light scattering, and minimal autofluorescence. … Many types of NIR chemical probes have been developed but they lack selectivity for labeling of particular cell types upon multi-cell bolus loading. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society 93(0), 1-SS-60, 2020

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  • Development of a novel chemical tag tool for calcium imaging by near-infrared fluorescence  [in Japanese]

    Yuki Isono , Asanuma Daisuke , Okubo Yohei , Namiki Shigeyuki , Hirose Kenzo

    … imaging because of its high tissue penetration, low light scattering, and minimal autofluorescence. … Many types of NIR chemical probes have been developed but they lack selectivity for labeling of particular cell types upon multi-cell bolus loading. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society 93(0), 1-P-134, 2020

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  • Debridement Using the Hydrosurgery System and Negative Pressure Wound Therapy that Allowed Immediate Skin Grafting in a Patient withSevere Fournier's Gangrene  [in Japanese]

    Machida Taku , Suda Ryuichiro , Nishimura Masaki , Yanagisawa Shinji

    <p>【緒言】フルニエ壊疽に対する電気メスによるデブリードマンは迅速性に欠け,組織選択性は低い.Hydrosurgery System(以下HS)は高圧水流を利用したデブリードマンを行う技術である.また,局所陰圧閉鎖療法(Negative pressure wound therapy:以下NPWT)は,解剖学的理由から本症に対して施行されることは少ない.</p><p& …

    Nippon Daicho Komonbyo Gakkai Zasshi 73(1), 19-24, 2020

    J-STAGE  Ichushi Web 

  • A Novel TNF-α Converting Enzyme (TACE) Selective Inhibitor JTP-96193 Prevents Insulin Resistance in KK-A<sup>y</sup> Type 2 Diabetic Mice and Diabetic Peripheral Neuropathy in Type 1 Diabetic Mice

    Maekawa Mariko , Ohta Takeshi , Sasase Tomohiko , Tadaki Hironobu , Tomimoto Daisuke , Okuma Chihiro , Sano Ryuhei , Ishii Yukihito , Katsuda Yoshiaki , Yoshiuchi Hiromi , Kakefuda Reina

    … value of 5.4 nM and showed more than 1800-fold selectivity against other matrix metalloproteinases. … In mouse models of obesity and diabetes, JTP-96193 reduced the TNF-α release from the fat tissue and prevented development of diabetes and improved insulin resistance, respectively. …

    Biological and Pharmaceutical Bulletin 42(11), 1906-1912, 2019

    J-STAGE  Ichushi Web 

  • Genetic and tissue-specific RNA-sequencing analysis of self-compatible mutant TSC28 in <i>Brassica rapa</i> L. toward identification of a novel self-incompatibility factor

    Osaka Masaaki , Nakazono Mikio , Fujii Sota , Murase Kohji , Takayama Seiji , Suzuki Go , Suwabe Keita , Watanabe Masao , Nabemoto Moe , Maeda Shunsuke , Sakazono Satomi , Masuko-Suzuki Hiromi , Ito Kana , Takada Yoshinobu , Kobayashi Issei , Lim Yong Pyo

    … <p>Self-incompatibility (SI) is a sophisticated system for pollen selectivity to prevent pollination by genetically identical pollen. …

    Genes & Genetic Systems 94(4), 167-176, 2019

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  • An emerging role of angiotensin receptor binding protein ATRAP as a possible novel player in pathophysiology of visceral obesity and metabolic disorders

    Tamura Kouichi , Wakui Hiromichi , Ohki Kohji , Azushima Kengo , Uneda Kazushi , Kobayashi Ryu , Kinguchi Sho , Haruhara Kotaro , Yamaji Takahiro , Yamada Takayuki

    … GPCRs are now known to support a diversity of pharmacological profiles, a concept broadly referred to as functional selectivity. … In the course of an investigational search for a fine means to regulate AT1R signaling at the local tissue sites, we have focused our analysis on the AT1R-associated protein (ATRAP), which is a molecule that directly binds to the carboxyl-terminal domain of AT1R. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society WCP2018(0), SY73-2, 2018

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  • Analgesic effects of a novel monoclonal antibody against Nav1.7 sodium channel

    Yoneda Sosuke , Hasegawa Minoru , Kasai Erika , Takahashi Tatsuya , Yoshikawa Mai , Onoda Junji , Izumi Takaya , Yamane Shoji , Maekawa Kazuhiko , Asaki Toshiyuki

    … However the search of Nav1.7-specific inhibitor has not been successfully progressed because small molecules are limited to have high selectivity in high sequence similarity among Nav channel subtypes. … Prepared antibodies were evaluated by binding affinity to immunogen peptide and Nav1.7 expressed on cell membrane and rat DRG tissue. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society WCP2018(0), PO3-2-25, 2018

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  • Inhibitory effects of an orally active small molecule alpha4beta1/alpha4beta7 integrin antagonist, TR-728, on TNBS-induced colitis in rats

    Sasaki Rie , Koga Yoko , Hirokawa Hiroe , Itaba Shoichi , Meguro Hiroyuki , Kainoh Mie

    … TR-728 is a novel orally active small molecule alpha4beta1/alpha4beta7 integrin antagonist and has different properties from the antibody, such as gut-dominant distribution and selectivity for the active form of alpha4beta1. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society WCP2018(0), PO2-5-36, 2018

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  • Inhibitory effects of an orally active small molecule alpha4beta1/alpha4beta7 integrin antagonist, TR-728, on DSS-induced experimental colitis in mice and spontaneous colitis in HLA-B27 transgenic rats

    Koga Yoko , Sasaki Rie , Hirokawa Hiroe , Hara Sunao , Hayashi Kenichi , Meguro Hiroyuki , Kainoh Mie

    … TR-728 is a novel orally active small molecule alpha4beta1/alpha4beta7 integrin antagonist and has different properties from the antibody, such as gut-dominant distribution and selectivity for the acive form of alpha4beta1. … Histological analysis demonstrated that TR-728 also suppressed colonic tissue damage.</p><p><b>Conclusion</b>: These results suggest that TR-728 can be expected to useful in the treatment of UC. …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society WCP2018(0), PO2-5-35, 2018

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  • Linking real-time activity with detailed anatomy at cellular resolution across the vertebrate brain

    Deisseroth Karl

    … we have been able to discover principles of function by solving the key high-resolution channelrhodopsin crystal structures and by structure-guided redesign for altered ion selectivity, kinetics, and spectral properties<sup>1,2</sup>. … And we will present in detail a new general method for identifying the cellular manifestation of internal states by integrating brain-wide single-cell activity imaging and control with hydrogel-tissue chemistry<sup>10</sup> …

    Proceedings for Annual Meeting of The Japanese Pharmacological Society WCP2018(0), PL-2, 2018

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  • Development of a Bubble Type Pulsed Laser-induced Liquid Jet Applicator by Air Entrainment  [in Japanese]

    SO Keisuke , KANZAWA Yusuke , WASHIO Toshikatsu , YANO Tomoyuki , ARAFUNE Tatsuhiko

    … Here, we improved the LILJ for another surgical application while maintaining its key advantage of tissue selectivity. … Next, the bubble jet was injected into gelatin, which simulated living tissue, and the crushing effect and depth were measured using a high-speed camera. … The bubble jet did not damage the brain parenchyma, and the blood vessels and pia matter on the surface of the brain tissue were preserved. …

    Transactions of Japanese Society for Medical and Biological Engineering 56(6), 237-242, 2018

    J-STAGE  Ichushi Web 

  • P-67 Synthesis of novel LXR agonists based on naphthoquinone derivatives  [in Japanese]

    Nishioka Tatsuma , Umeda Kaori , Yoshida Yuma , Makishima Makoto , Suhara Yoshitomo

    … Liver X receptors (LXRs) are members of the nuclear receptor superfamily.LXRs include two subtypes, LXRα and LXRβ, which have different tissue distributions.LXRα is highly expressed in liver, intestine, adipose tissue, and macrophages, on the otherhand, LXRβ is ubiquitously existed in organs and tissues. … Manysynthetic LXR agonists have been reported including T0901317 and GW3965, however,most of them do not show subtype selectivity. …

    Symposium on the Chemistry of Natural Products, symposium papers 59(0), 477-482, 2017

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  • Puled Laser-Induced Liquid Jet Surgery System: From Bench to Bedside  [in Japanese]

    NAKAGAWA Atsuhiro , TOMINAGA Teiji , KAWAGUCHI Tomohiro , ENDO Toshiki , OGAWA Yoshikazu , YAMASHITA Shinichi , ARAFUNE Tatsuhiko , KATO Takashi , WASHIO Toshikatsu , ARAI Yoichi

    … This technology discriminates from other in terms of no heat damage, tissue selectivity, andhigh affi nity to be incorporated into minimally invasive medical device, such as catheter and endoscopy.The device is now in the phase of clinical study for microsurgery, but had three major barriers duringthis translational research process. …

    The Review of Laser Engineering 44(3), 165, 2016

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  • OH-Radical Specific Addition to Glutathione S-Atom at the Air-Water Interface: Relevance to the Redox Balance of the Lung Epithelial Lining Fluid.

    Enami Shinichi , Hoffmann Michael R , Colussi Agustín J

    … Antioxidants in epithelial lining fluids (ELF) prevent inhaled air pollutants from reaching lung tissue. … The remarkable specificity of ·OH on water versus its lack of selectivity in bulk water implicates an unprecedented steering process during [OH···GSH] interfacial encounters. …

    The journal of physical chemistry letters 6(19), 3935-3943, 2015-09-14

    IR 

  • Discovery of Novel Selective ERα/ERβ Ligands by Multi-pharmacophore Modeling and Virtual Screening

    Huang Wenhai , Wei Wenhua , Yang Yewei , Zhang Tao , Shen Zhengrong

    … Estrogen receptor α (ERα) and estrogen receptor β (ERβ) regulate different sets of gene expression, and have different ligand responses, which make the estrogen tissue-specific. … Thus, the estrogen receptor (ER) subtype-selective ligands can improve the target-site selectivity and decrease the off-target effect. …

    Chemical and Pharmaceutical Bulletin 63(10), 780-791, 2015

    J-STAGE  Ichushi Web 

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