Abstract:
:The pharmacokinetic profiles of the hypoglycemic agent, acetohexamide (AH) and its major active metabolite, hydroxyhexamide (HH) were studied in three species of laboratory animals after intraperitoneal (ipl) administration in comparison with those after intravenous (iv) administration of AH and of the preformed metabolite HH. Reductive biotransformation of AH to HH was reversible in rats and guinea pigs, while it was irreversible in rabbits. The parameters of reversible drug-metabolite pharmacokinetics were calculated, including essential clearances of reversible and irreversible elimination, volumes of distribution at the steady state and sojourn times or turnover rates of the metabolite pair. An interconversion model, which incorporated a first-pass metabolism, was applied to the disposition kinetics of AH and HH, and the available fractions of AH and generated metabolite HH in each species were elucidated.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Asada S,Nagamine S,Nakae Hdoi
10.1248/cpb.37.760subject
Has Abstractpub_date
1989-03-01 00:00:00pages
760-5issue
3eissn
0009-2363issn
1347-5223journal_volume
37pub_type
杂志文章abstract::Virulence (vir) gene expression of Agrobacterium tumefaciens is activated by plant phenolic compounds such as alpha-hydroxyacetosyringone (HOAS), acetosyringone (AS), methyl syringate, coniferyl alcohol and sinapyl alcohol. Inositol was found to be a potentiating factor of vir-inducing activity, which enhanced the vir...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.39.2613
更新日期:1991-10-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2015-01-01 00:00:00
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pub_type: 杂志文章
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更新日期:2002-05-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.37.1647
更新日期:1989-06-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.38.3147
更新日期:1990-11-01 00:00:00
abstract::A novel cytolytic factor, dolabellanin P, was purified to apparent homogeneity from the purple fluid of the sea hare, Dolabella auricularia. Purified dolabellanin P is a single polypeptide of 60 kDa. The amino acid composition and the N-terminus of the factor were also determined. This factor nonspecifically lysed all...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1989-08-01 00:00:00
abstract::We used near infrared (NIR) spectroscopy to evaluate the degree of mixing of blended dry syrup (DS) products whose particle sizes are not specified in the Revised 16th Edition of the Japanese Pharmacopoeia, and also evaluated the degree of mixing when powder products or fine granule products were added to DS products....
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2012-01-01 00:00:00
abstract::ZCVI₄-2 is a newly developed furoxan-based nitric oxide-releasing derivative of oleanolic acid. It exhibited strong cytotoxicity against human hepatocellular carcinoma (HCC) in vitro and significantly inhibited the growth of HCC tumors in vivo. However, its low aqueous solubility and toxicity due to the fast release o...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2011-01-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2004-10-01 00:00:00
abstract::A mechanism for the relatively high permeability of vitamin C in relation to the change in the protein domain of the stratum corneum has been proposed. Firstly, the skin permeation characteristics of vitamin C (l-[1-14C]-ascorbic acid) using whole skin and stripped skin of the hairless mouse were investigated. By empl...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:1998-01-01 00:00:00
abstract::The absorption of insulin (from porcine pancreas) from the rectum of rabbits after the administration of hollow-type suppositories containing insulin and five kinds of cyclodextrins (CyDs) was investigated. Three types of suppositories were employed: suppository I containing insulin (approximately 26 IU/mg) and variou...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.40.3042
更新日期:1992-11-01 00:00:00
abstract::A series of 4-alkoxy-2-(1-piperazinyl)quinazoline derivatives was synthesized and evaluated for its ability to reverse a scopolamine-induced learned impairment in a one-trial passive avoidance task (antiamnestic activity). 2-(4-Allyl-1-piperazinyl)-4-pentyloxyquinazoline (4) showed more potent antiamnestic activity th...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.39.367
更新日期:1991-02-01 00:00:00
abstract::Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/cpb.c17-00413
更新日期:2018-01-01 00:00:00
abstract::To improve the oral bioavailability of a dermorphin tetrapeptide analog, N(alpha)-1-iminoethyl-Tyr-D-MetO-Phe-MebetaAla-OH (III), which has a potent analgesic activity after oral administration, various derivatives were synthesized to increase lipophilicity by esterification of the C-terminal carboxyl group and/or acy...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.51.759
更新日期:2003-07-01 00:00:00
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journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.49.373
更新日期:2001-04-01 00:00:00
abstract::The CHCl3 extract of the root of Angelica japonica showed high inhibitory activity against human gastric adenocarcinoma (MK-1) cell growth. From this extract, a new furanocoumarin named japoangelone and four furanocoumarin ethers of falcarindiol, named japoangelols A-D, were isolated together with caffeic acid methyl ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.47.96
更新日期:1999-01-01 00:00:00
abstract::A new series of novel (2S)-2-({2-[1,4-dihydro-3,5-bis(methoxycarbonyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridin-1-yl]-2-oxoethyl}amino)-3-(4-hydroxyphenyl) propanoic acid (3a) and its analogues 3b-j has been synthesized. These compounds were evaluated for their in vitro antioxidant activity, anti-inflammatory activity an...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.59.1153
更新日期:2011-01-01 00:00:00
abstract::We investigated the distribution and fate of liposomes after their intravenous injection into a mouse. Liposomes were composed of dimyristoylphosphatidylcholine, cholesterol and dicetylphosphate (7:2:1, molar ratio) with or without lactosylceramide. They were characterized as small unilamellar vesicles, approximately ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.40.1016
更新日期:1992-04-01 00:00:00
abstract::Enzymatic functions are often altered during disease onset and progression, and therefore chemical-biological studies, which utilize chemical knowledge to discover novel protein functions, are often employed to find proteins with functions closely related to disease phenotypes. Such studies are known as forward chemic...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章,评审
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更新日期:2017-01-01 00:00:00
abstract::Using CPG support linked with 5-deazaflavin, the 5-deazaflavin modified oligodeoxynucleotides at 3'-end(ODN-dF1) were synthesized. The thermal stability of the duplex of ODN-dF1 with its complement was higher than that of oligonucleotide linked to 5-deazaflavin at 5'-end internucleotide linkage. ...
journal_title:Chemical & pharmaceutical bulletin
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更新日期:1993-07-01 00:00:00
abstract::Five glycyrrhetinic acid (Ib) derivatives have been synthesized to try to improve the antioxidant activity. Their in vitro antioxidant activities were studied using a cytochrome P450/NADPH reductase system from rat liver microsomes. The generation of microsomal free radicals was followed by oxidation of the DCFH-DA pr...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2004-12-01 00:00:00
abstract::The developmental change of uridine diphosphate-glucuronyltransferase (UDPGT) was studied using hepatic microsomes of rat fetuses on days 18 and 21 of gestation. Total phospholipid content was higher on day 21 than on day 18, although no significant difference in the composition between the two stages was observed. Li...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.39.2454
更新日期:1991-09-01 00:00:00
abstract::All-methylated isorugosin B was synthesized via two-step esterification between optically active valoneic acid and glucose derivatives. ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2010-03-01 00:00:00
abstract::A series of 5-(pyridin-4-yl)-N-substituted-1,3,4-oxadiazol-2-amines (3a-d), 5-(pyridin-4-yl)-N-substituted-1,3,4-thiadiazol-2-amines (4a-d) and 5-(pyridin-4-yl)-4-substituted-1,2,4-triazole-3-thiones (5a-d) were obtained by the cyclization of hydrazinecarbothioamide derivatives 2a-d derived from isonicotinic acid hydr...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c15-00059
更新日期:2015-01-01 00:00:00
abstract::To obtain optically active threo-2-amino-3-hydroxy-3-phenylpropanoic acid (1), (2RS,3SR)-2-benzoylamino-3-hydroxy-3-phenylpropanoic acid [(2RS,3SR)-2] was first optically resolved using (1S,2S)- and (1R,2R)-2-amino-1-(4-nitrophenyl)-1,3-propanediol as the resolving agents to afford (2R,3S)- and (2S,3R)-2 in yields of ...
journal_title:Chemical & pharmaceutical bulletin
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更新日期:2003-12-01 00:00:00
abstract::To estimate membrane potential in synaptosomes with the use of tetraphenylphosphonium (TPP+), an equation relating the amount of TPP+ accumulated in synaptosomes with membrane potential was derived from the following two assumptions. (1) TPP+ molecules were distributed into plasma membranes, mitochondria and cytosol o...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.37.3333
更新日期:1989-12-01 00:00:00
abstract::Hot aqueous extracts of 134 Chinese crude drugs were subjected to screening for inhibitory activity on K+ contracture of guinea pig taenia coli, and significant activity was observed in 17 crude drugs. Chemical investigations of two crude drugs, Kakko and Ubai, which originate from Pogostemon cablin and Prunus mume, r...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.37.345
更新日期:1989-02-01 00:00:00
abstract::The aim of the present study was to mask the bitterness of propiverine hydrochloride (P-4) by converting it to propiverine free base. Fine granules comprising the free base, which was converted from P-4 by desalination, were prepared. By using Fourier transform infrared spectroscopy, thermogravimetry-differential ther...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c12-00206
更新日期:2012-01-01 00:00:00
abstract::Asymmetric epoxidation reactions of chalcone derivatives catalyzed by chiral calcium complexes using hydrogen peroxide were developed. The epoxidation reactions proceeded smoothly to afford the desired products in good yields with good enantioselectivities. This is the first example of chiral calcium-catalyzed asymmet...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
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更新日期:2018-01-01 00:00:00
abstract::In our search for novel anti-human immunodeficiency virus (HIV)-1 agents, 14 delavirdine analogues were synthesized and evaluated as potential anti-HIV-1 agents in cell-based assays. Compound 1Aa exhibited potent and selective anti-HIV-1 activity in acutely infected MT4 cells, with effective concentration (EC50) value...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.49.1406
更新日期:2001-11-01 00:00:00