Kouzi Yamada
Eisai
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Featured researches published by Kouzi Yamada.
Inflammation Research | 1990
S. Kumakura; Mannen Mishima; Seiichi Kobayashi; Hiroshi Shirota; Shinya Abe; Kouzi Yamada; Susumu Tsurufuji
Antiinflammatory effects of indomethacin farnesil (IMF), a novel prodrug of indomethacin, was examined after both oral and local administration. In the air pouch carrageenin-induced inflammation, an oral dose of IMF exerted dose dependent inhibitory effects on the accumulation of inflammatory exudate fluid and the migration of leukocytes into the exudate. Both the increased vascular permeability and the prostaglandin E2 levels in the exudate fluid were reduced by IMF. Significant levels of free indomethacin were detected in the pouch fluid. In spite of the inability of IMF to inhibit prostaglandin synthesis in a cell free cyclooxygenase system, IMF injected locally inhibited carrageenin paw edema, and the inhibitory effect was comparable to that of indomethacin itself. When injected locally into the paw together with carrageenin,14C-IMF was effectively converted to its active metabolite, indomethacin. The indomethacin concentration in the paw tissue was comparable to that of indomethacin injected paws with the same molar dose of free indomethacin.
Xenobiotica | 1987
Yukio Nishizawa; Shinya Abe; Kouzi Yamada; Toshihiko Nakamura; Isao Yamatsu; Kensaku Kinoshita
The metabolic disposition of the anti-ulcer agent geranylgeranylacetone (GGA) was examined in rats. Urinary metabolites were isolated and identified by mass spectrometry and 1H n.m.r. studies. Three metabolites were dicarboxylic acids with chain lengths of C7, C9 and C11 and accounted for 31.6%, 14.8% and 5.3%, respectively, of the radioactivity excreted in the urine 24 h after oral administration of 14C-GGA. The metabolites produced by the incubation of GGA with liver microsomes in the presence of an NADPH-generating system were identified as an omega-hydroxylated derivative of GGA and its ketone-reduced form. The characterization of GGA metabolites indicates that the metabolic pathway of GGA in rats involves omega-oxidation (possibly via the corresponding carboxylic acid) and successive beta-oxidation processes.
Xenobiotica | 1991
Tsutomu Yoshimura; Satoru Tanaka; H. Sakurai; Y. Nagai; Kouzi Yamada; S. Katayama; Shinya Abe; Isao Yamatsu
1. The 5-lipoxygenase inhibitor (I), a substituted benzothiazole is metabolized mainly by glucuronide and/or sulphate conjugation in rat, guinea-pig, beagle and rhesus monkey. Glucuronidation is the major pathway, and sulphation is more extensive in rat and beagle than in guinea-pig and rhesus monkey. 2. After a single oral dosing of 14C-I (10 mg/kg), more than 96% of the dose was excreted in 7 days in all four species, however there is species difference in urinary excretion, which was 2.8 +/- 0.3% in rat, 46.9 +/- 1.6% in guinea-pig, 2.6% in beagle and 68.2% in rhesus monkey. 3. After a single i.v. dose of 14C-I to bile duct-cannulated rats and guinea pigs, bile was a major route of elimination, and in rats the ratio of glucuronide to sulphate in excreta increased from 0.71 +/- 0.01 to 0.93 +/- 0.05 as the dose was increased from 0.2 to 20 mg/kg.
Archive | 1982
Akio Sato; Kenji Nakajima; Yoshimasa Takahara; Shizumasa Kijima; Noriaki Kuwana; Shinya Abe; Kouzi Yamada
Archive | 1986
Isao Yamatsu; Shinya Abe; Yuichi Inai; Takeshi Suzuki; Kensaku Kinoshita; Mannen Mishima; Yoshinori Katoh; Seiichi Kobayashi; Manabu Murakami; Kouzi Yamada
Archive | 1983
Akio Sato; Kenji Nakajima; Yoshimasa Takahara; Shizumasa Kijima; Noriaki Kuwana; Shinya Abe; Kouzi Yamada
Archive | 1982
Akio Sato; Kenji Nakajima; Yoshimasa Takahara; Shizumasa Kijima; Noriaki Kuwana; Shinya Abe; Kouzi Yamada
Archive | 1984
Isao Yamatsu; Shinya Abe; Yuichi Inai; Takeshi Suzuki; Kensaku Kinoshita; Mannen Mishima; Yoshinori Katoh; Seiichi Kobayashi; Manabu Murakami; Kouzi Yamada
Archive | 1982
Isao Yamatsu; Shinya Abe; Yuichi Inai; Takeshi Suzuki; Kensaku Kinoshita; Mannen Mishima; Yoshinori Katoh; Seiichi Kobayashi; Manabu Murakami; Kouzi Yamada
Archive | 1982
Isao Yamatsu; Shinya Abe; Yuichi Inai; Takeshi Suzuki; Kensaku Kinoshita; Mannen Mishima; Yoshinori Katoh; Seiichi Kobayashi; Manabu Murakami; Kouzi Yamada