All issues
Predecessor
Volume 112, Issue 2
Displaying 1-8 of 8 articles from this issue
- |<
- <
- 1
- >
- >|
-
Masatoshi YAMATO1992 Volume 112 Issue 2 Pages 81-99
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn reviewing my lifework, I wish to summarize the results of studies on the development of new biological-active compounds. The following subjects are discussed : 1) syntheses and biological activities of benzoxazole derivatives, 2) structure-activity relationships of phyllodulcin, a natural sweetner, and 3, 4-dihydroisocoumarins for sweetness, 3) syntheses and structure-activity relationships of spiro [isocoumarin-piperidine] analogs for antiallergic activity, 4) design, structure-activity relationships, and a mechanism of antitumor action of bistropolone derivatives, 5) design, structure-activity relationships of fused tetracyclic quinolines for antitumor activity.View full abstractDownload PDF (1475K) -
Tatsuo NAGASAKA, Kenichi MOMOSE, Fumiko HAMAGUCHI, Kenji YAMADA, Hiroa ...1992 Volume 112 Issue 2 Pages 100-107
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSVarious 1-trans-cinnamoyl-2-pyrrolidinones (6a-k) and 1-[trans-3-(pyridyl)acryloyl]-2-pyrrolidinones (9a-c) were prepared as analogues of the nootropic agent, aniracetam (2), and their effects on hemicholinium-induced impairment of water maze learning in mice were examined. 1-(trans-3-Methoxycinnamoyl)-, 1-(trans-4-methoxycinnamoyl)- and 1-(trans-4-chlorocinnamoyl)-2-pyrrolidinones (6c, d, h) and 1-[trans-3-(3-pyridyl)acryloyl]-2-pyrrolidinone (9c) were found to be more active than aniracetam in these tests. In addition, these 2-pyrrolidinones (6a-k, 9a-c) were apparently observed to lengthen mouse survival time following hemicholinium injection into the brain.View full abstractDownload PDF (770K) -
Chiaki TASHIRO, Syuji YUASA, Kenichi DEMIZU1992 Volume 112 Issue 2 Pages 108-114
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFour alcholic metabolities of (±)-3-chloro-5-[3-(2-oxo-1, 2, 3, 5, 6, 7, 8, 8a-octahydroimidazo [1, 2-a] pyridine-3-spiro-4'-peperidino) propyl]-10, 11-dihydro-5H-dibenz [b, f] azepine (mosapramine), a new antipsychotic drug, were synthesized in order to determine their chemical structures. A mixture of 10-ethoxy-3-chloro-10, 11-dihydro-5H-dibenz [b, f] azepine and 11-ethoxy isomer was used as a starting material. Isomeric intermediates, i. e. 10-oxo-3-chloro-5-(3-chloropropyl)-10, 11-dihydro-5H-dibenz [b, f] azepine and 11-oxo isomer, were separated by chromatography with silica gel. The metabolites were obtained by NaBH4 reduction of the corresponding 10-oxo or 11-oxo compounds followed by introduction of spiro-piperidine moieties into propyl side chain.View full abstractDownload PDF (701K) -
Hiroshi NAKAMURA, Noriko KUMAZAWA, Setsuko OHTA, Takashi FUJITA, Taisu ...1992 Volume 112 Issue 2 Pages 115-123
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIt has been reported that the methanol extract from the bark of Acer nikoense MAXIM. (AN) and the fractions separated from this extract showed the protection for liver injuries induced by carbontetrachloride (CCl4) in rat. On the other hand, the evidence manifested that the fractions of the callus of young branches from AN were recognized to have protective effects on the CCl4-induced liver injuries in rat. In this study, the protective activities of the fractions extracted from the callus of AN were investigated on the α-naphthylisothiocyanate (ANIT)-induced liver injuries in rat. The protectively active principles on the ANIT-induced liver injuries were found in the ether soluble fraction. The components of the protective effect were purified by repeated silica gel chromatographies. One of the protective substances in this fraction was identified to be β-sitosterol. The protective fractions on the ANIT-induced liver injuries showed the protective effects on ANIT-induced cholestasis, but did not show cholagogic effects.View full abstractDownload PDF (817K) -
Tamotsu NIKAIDO, Setsuko IIZUKA, Noriko OKADA, Takashi KUGE, Taichi OH ...1992 Volume 112 Issue 2 Pages 124-128
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA Chinese herbal medicinal prescription, Makyo-kanseki-to, was studied for the inhibitory activity of adenosine 3', 5'-cyclic monophosphate (cAMP) phosphodiesterase. The effect for the inhibitory activity of cAMP phosphodiesterase by combination with constituent crude drugs of the prescription was studied. Gypsum acted as a mitigatory component for Ephedra herb and Glycyrrhiza in cAMP phosphodiesterase inhibition test.View full abstractDownload PDF (526K) -
Takafumi ITAMI, Makoto EMA, Jun SAKAMOTO, Katsuko HOSODA, Mamoru NOGUC ...1992 Volume 112 Issue 2 Pages 129-134
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe antipyretic effects of oral administration of eight traditional Chinese medicines (dried extracts) were tested in febrile rabbits injected with bacterial pyrogen, lipopolysaccharide (LPS) 0.05 μg/kg (i.v.). The traditional Chinese medicines were given 0.6-2 g/10 ml/kg (p.o.) simultaneously with LPS. The most potent antipyretic effect was observed in Dai-jyoki-to (Tachen-chi-tang). The moderate antipyretic effects were observed in Tokisyakuyaku-san (Tang-kuei-shao-yao-san) and Syo-saiko-to (Hssiao-chai-hutang). Koso-san (Hsiang-su-san), Oren-gedoku-to (Huang-lien-chieh-tu-tan), Gorei-san (Wu-ling-san), Kakkon-to (Ko-ken-tang) and Byakkoka-ninjin-to (Pai-hu-chia-jen-sheng-tang) showed no effects.View full abstractDownload PDF (657K) -
Kenroh SASAKI, Masaaki ISHIKAWA, Yoshio TAKAYANAGI, Kenichi SASAKI1992 Volume 112 Issue 2 Pages 135-140
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe variation of hepatic drug-metabolism was investigated in male Wistar rats bearing hind paw edema induced by carrageenan (1%, 0.1 ml, s. c.). The content of cytochrome P-450 and the biotransformation of aminopyrine in the hepatic 9000×g supernatant (S-9) decreased after the subcutaneous injection of carrageenan to rat hind paw. In carrageenan-treated rats the plasma concentration of antipyrine after the administration of antipyrine (20 mg/kg, i. v.) was higher than that of control rats. In comparison with the control groups, the pharmacokinetic parameters of antipyrine in carrageenan-treated rats was altered. AUC0-200 and t1/2 significantly increased and CLtot and ke significantly decreased. On the other hand, no change of the volume of distribution (Vd) was observed. The results indicate that the hepatic drug metabolism under the carrageenan-induced inflammation is inhibited both in vitro and in vivo.View full abstractDownload PDF (726K) -
Determination and Stability Studies of Urea in Urea Creams by High-Performance Liquid ChromatographyTsutomu YASUDA, Toshihiro AKAMA, Hiroshi IKAWA1992 Volume 112 Issue 2 Pages 141-145
Published: February 25, 1992
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA method was developed for determining urea in urea creams by high-performance liquid chromatography using strong acidic cation exchange gel. Elution was carried out with 0.05 M phosphate buffer (pH 3.4) at 40°C, and detection was made with a UV-spectrometer at 200 nm. This method was used for studying and comparing the stability of urea creams produced by ourselves and by other manufactures. The assay showed that there were differences in the stability of the tested creams.View full abstractDownload PDF (433K)
- |<
- <
- 1
- >
- >|