Detail of "27724-96-5"

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Metabolism of 4-(2-carboxyethyl)phenyl trans-4-aminomethylcyclohexane carboxylate hydrochloride (DV-1006), a new antiulcer drug

Metabolism of 4-(2-carboxyethyl)phenyl trans-4-aminomethylcyclohexane carboxylate hydrochloride (DV-1006), a new antiulcer drug. 1. Absorption, distribution, excretion and metabolism in rats. Ono, Kenji; Okazaki, Osamu; Saito, Tadashi; Sano, Mitsuji; Akimoto, Takeshi (Res. Inst., Daiichi Seiyaku Co., Ltd., Tokyo, Japan). Oyo Yakuri, 12(2), 269-77 (English) 1976. CODEN: OYYAA2. ISSN: 0369-8033. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The metabolic fate of 14C-labeled DV-1006 (I) [27724-96-5] was investigated in rats after a single oral or i.v. administration. The blood levels of radioactivity reached a peak 8 h after oral administration and thereafter declined rapidly. The blood levels of I after an i.v. injection fell off biphasically and the whole blood half life was 1.19 h up to 4 h after injection and 3.0 h thereafter. The radioactivity in the tissues tested reached a max. 8 h after oral administration. The highest radioactivity was in the gastric wall, followed in order by the kidney, liver, lung, adrenal, heart, and skeletal muscle at 8 h. Approx. 61% and 32% of the administered radioactivity was recovered in the feces and urine resp., 48 h after oral administration. When it was injected i.v., about 92% of the administered radioactivity was excreted in the urine within 24 h after administration, and a few % in the feces. Four radioactive compds. were detected in rat urine. These were identified by an isotopic diln. method as tranexamic acid [1197-18-8], trans-hexahydrotelephthalic acid [619-82-9], trans-p-hydroxymethylcyclohexane carboxylic acid [66185-74-8], and I. The major metabolite in plasma and urine was tranexamic acid regardless of the administration route.

Acute toxicity of 4-(2-carboxyethyl) phenyl trans-4-aminomethylcyclohexane carboxylate hydrochloride (DV-1006), a new antiulcer drug, and its several metabolites

Acute toxicity of 4-(2-carboxyethyl) phenyl trans-4-aminomethylcyclohexane carboxylate hydrochloride (DV-1006), a new antiulcer drug, and its several metabolites. Onodera, Takeshi; Ohno, Hiroshi; Akiyama, Yoshihiro; Hoshina, Takashi; Akimoto, Takeshi (Res. Inst., Daiichi Seiyaku Co., Ltd., Tokyo, Japan). Oyo Yakuri, 12(2), 265-7 (English) 1976. CODEN: OYYAA2. ISSN: 0369-8033. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The acute toxicity of DV-1006 (I) [27724-96-5], a new antiulcer drug, and its metabolites was studied in mice and rats. LD50 values (g/kg) of I were as follows: orally, >5 in mice and rats; s.c., 4.57in mice and 1.50 in rats; i.p., 1.53 in mice and 0.75 in rats; i.v., 0.69 in mice and 0.35 in rats. Toxic signs in mice included sedation, lacrimation, piloerection, tonic convulsion, and those in rats were lacrimation, bloody discharge from the eye, reddening of the skin, hematuria, diarrhea, prostration, tonic convulsion and tremor. Most deaths occured within 24 h after treatment following dyspnea. Three metabolites of I were considerably less toxic than the parent compd., though toxic symptoms caused by the metabolites were similar to those caused by I.