Detail of "94497-51-5"

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New type inducers of differentiation of human HL-60 promyelocytic leukemia cells

New type inducers of differentiation of human HL-60 promyelocytic leukemia cells. Terephthalic anilides. Kagechika, Hiroyuki; Kawachi, Emiko; Hashimoto, Yuichi; Shudo, Koichi (Fac. Pharm. Sci., Univ. Tokyo, Tokyo, Japan). Chem. Pharm. Bull., 32(10), 4209-12 (English) 1984.There are some reagents like 94497-51-5 is used in this study. CODEN: CPBTAL. ISSN: 0009-2363. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 18 Several synthetic compds., which were designed from structure-activity considerations of retinoids, teleocidins, and indolactams, were tested for their inducing activity of differentiation of human myelogenous leukemic cells (HL-60). Terephthalic acid mono-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-2-naphthylamide (I) [94497-51-5] or its Me ester (II) [94497-53-7] induced differentiation of these cells to cells which morphol. and functionally resembled granulocytes. I and II had a higher inducing activity than retinoic acid [302-79-4]. Alkyl substitution on the aniline ring was necessary for inducing activity, whereas an alkyl group on the N atom seemed to abolish the inducing activity. .

Studies on the metabolism and disposition of the new retinoid 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)carbamoyl] benzoic acid

Studies on the metabolism and disposition of the new retinoid 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)carbamoyl] benzoic acid. 3rd communication. Placental transfer and excretion into milk in rats. Mizojiri, Kenji; Okabe, Hiroshi; Sugeno, Koichi; Esumi, Yoshio; Takaichi, Matsuo; Harada, Tomoko; Seki, Hideaki; Inaba, Atsuhiro ( New Drug Research Laboratories, Shionogi and Co. Ltd., Osaka 561, Japan). Arzneimittel-Forschung, 47(2), 201-208 (English) 1997 Cantor. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) 4-[(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)carbamoyl]benzoi c acid (CAS 94497-51-5, Am-80) is a new synthetic retinoid which has been shown to have a potent topical antipsoriatic activity. Placental transfer and excretion into milk after administration of 14C-Am-80 to pregnant or nursing rats were investigated in view of reproductive and developmental toxicity studies. When 14C-Am-80 was administered topically at a dose of 10 mg/kg to normal-skin pregnant rats on the 12th day of pregnancy, plasma radioactivity in the dam and fetus was detected only at low levels. However, at a dose of 1 mg/kg to the stripped-skin pregnant rats, radioactivity levels peaked at 6 h in the maternal plasma (188.7 ng eq./g) and fetus (64.6 ng eq./g) and at a dose of 10 mg/kg, the peak maternal plasma level of radioactivity and the concn. of radioactivity in the fetus up to 24 h after dosing rose about 10-fold in proportion to the increased dose. At both doses, the radioactivity level in the fetus at the peak corresponded to approx. one-third of the maternal plasma level. When 14C-Am-80 was administered s.c. at a dose of l mg/kg to pregnant rats on the 12th day of pregnancy, radioactivity in the fetus peaked at 4 h after dosing, being about one-fourth of the maternal plasma level at the same time point. Radioactivity in the fetus after s.c. administration of 14C-Am-80 at a dose of 1 mg/kg to pregnant rats on the 19th day of pregnancy peaked (156.4 ng eq./g) at 4 h after dosing, corresponding to approx. one-half the maternal plasma level at the same time point, and then decreased gradually. Among the fetal tissues, relatively high radioactivity was found in the liver. Whole-body autoradiog. showed that in most tissues in the dam, the distribution pattern of radioactivity was similar to that in the non-pregnant rat. The concn. of radioactivity in the milk after s.c. administration of 14C-Am-80 at a dose of 1 mg/kg to lactating rats on the 9th day after delivery peaked at 8 h after dosing, being 94 times greater than that in the plasma. Unchanged Am-80 in the milk was largely recovered after hydrolysis of hexane exts. of the intact milk with lipase, suggesting extensive incorporation of Am-80 into the triglyceride in the milk because of its benzoic acid structure and high lipophilicity. As for radioactive metabolites which have hitherto been identified in rats, only M-6 (taurine conjugate of Am-80) and tetrahydro-tetra-methyl-naphthylamine (TTNA) were detectable in small amts. in the milk.