Publication


Featured researches published by Kazuya Takenouchi.


Steroids | 2012

TEI-A00114: A new vitamin D3 analogue that inhibits neutrophil recruitment in an acute lung injury hamster model while showing reduced hypercalcemic activity

Yasuhiro Takano; Hiroaki Mitsuhashi; Seiichi Ishizuka; Katsushi Takahashi; Manabu Chokki; Kazuya Takenouchi; Qingzhi Gao; Hiroko Tanaka; Atsushi Hazato; Masayasu Tabe; Minoru Furuya; Kenji Manabe; Koichi Ueno

While searching for vitamin D(3) analogues which inhibit neutrophil recruitment in the lung without elevating plasma calcium level, we found that (5Z,7E)-(1S,3R)-20(R)-[(5E)-(2S)-2-hydroxy-2-methyl-cyclopentanone-5-ylidene]methyl-9,10-secopregna-5,7,10(19)-triene-1,3-diol (TEI-A00114) had the best efficacy and calcemic action. TEI-A00114 has a vitamin D receptor affinity 2.5-fold weaker and a vitamin D binding protein affinity 330.9-fold weaker than those of 1α,25(OH)(2)D(3). The estimated effective doses for 40% inhibition (ED(40)) via peroral and intratracheal administration are 7.6 and 0.4 μg/kg, respectively. TEI-A00114 was also tested by inhaled administration, and its ED(40) was calculated as 0.2 μg/kg. The estimated 40% inhibitory concentration (IC(40)) of TEI-A00114 on interleukin (IL)-8 production induced by lipopolysaccharide and on IL-1β in human whole blood cells in vitro were 9.8 × 10(-8) or 1.8 × 10(-9)M, respectively. These levels of TEI-A00114s activities are equal to those of 1α,25(OH)(2)D(3). On the other hand, the calcemic action of TEI-A00114, which was evaluated at day 14 after sequential peroral quaque die administration, was 89-fold weaker (molar ratio) than that of 1α,25(OH)(2)D(3). These results indicate that TEI-A00114 has a dissociated profile between inhibition of neutrophil recruitment in the lung and calcemic action, suggesting its suitability over 1α,25(OH)(2)D(3) as a candidate for the treatment of acute lung injury.


Inorganic Chemistry | 1993

A new cyclam with an NH2-pendant donor, 6-amino-1,4,8,11-tetraazacyclotetradecane, and its nickel(II) complexes

Eiichi Kimura; Makoto Haruta; Tohru Koike; Mitsuhiko Shionoya; Kazuya Takenouchi; Yoichi Iitaka


Journal of Organic Chemistry | 1993

Novel bifunctional macrocyclic chelating agents appended with a pendant-type carboxymethylamino ligand and nitrobenzyl group and stability of the 88YIII complexes

Kazuya Takenouchi; Kenzo Watanabe; Yoshinori Kato; Tohru Koike; Eiichi Kimura


Journal of Organic Chemistry | 1993

Novel pendant-type macrocyclic bifunctional chelating agents: (Carboxymethyl)amino derivatives of 2-(4-nitrobenzyl)-1,4,7,10-tetraazacyclo-dodecane-N,N{prime},N{double_prime},N{prime}{double_prime}-tetraacetic acid and their complex formation with yttrium(III)

Kazuya Takenouchi; Masayasu Tabe; Kenzo Watanabe; Atsuo Hazato; Yoshinori Kato; Mitsuhiko Shionoya; Tohru Koike; Eiichi Kimura


Archive | 1993

PYRROLO(2,3-D)PYRIMIDINE HAVING CYCLIC AMINO GROUP AT 4-POSITION

Minoru Furuya; Hideki Horiuchi; Takashi Kadota; Keiji Komoriya; Yasushi Sakuma; Kazuya Takenouchi; Takahiro Takeuchi; Yoshihiro Yamanaka; 安司 佐久間; 実 古屋; 秀樹 堀内; 恵司 小森谷; 義弘 山中; 一弥 竹之内; 隆博 竹内; 孝志 門田


Archive | 2001

Use of vitamin d derivatives as bone resorption inhibitors

Seiichi Ishizuka; Kazuya Takenouchi; Atsushi Imaizumi; Yasuhiro Oue; Noriyoshi Kurihara; Sakamuri V. Reddy; G. D. Roodman


Archive | 1994

Nitrogen-containing bicyclic heterocyclic derivative and medicinal preparation containing the same

Toshiaki Harada; Masakazu Hasegawa; Hitoshi Omori; Katsushi Takahashi; Kazuya Takenouchi; 俊明 原田; 斉 大森; 一弥 竹之内; 雅一 長谷川; 克史 高橋


Archive | 2004

Vitamin d3 lactone derivatives

Kazuya Takenouchi; Miyuki Anzai; Hiroshi Saito; Kazuhisa Okada; Seiichi Ishizuka; Daishiro Miura; Hiroaki Takayama; Atsushi Kittaka; Nozomi Saito; Toshie Fujishima


Archive | 1993

4-HETEROALICYCLIC-PYRROLO(2,3-D)PYRIMIDINE

Hideki Horiuchi; Takashi Kadota; Keiji Komoriya; Yasushi Sakuma; Kazuya Takenouchi; Takahiro Takeuchi; Yoshihiro Yamanaka; 安司 佐久間; 秀樹 堀内; 恵司 小森谷; 義弘 山中; 一弥 竹之内; 隆博 竹内; 孝志 門田


Archive | 2004

Crystal of (23s)-1alpha-hydroxy-27-nor-25-methylenevitamin d3-26,23-lactone and process for producing the same

Kazuya Takenouchi; Kenji Manabe

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