Abstract:
:The prostacyclin I1 (PGI1) analogue, SM-10906 and its methyl ester, SM-10902, have been compared with the PGI2 analogue, iloprost, with respect to binding to the PGI2 receptor, stimulation of adenylate cyclase activity and inhibition of thrombin-induced Ca2+ mobilization in mastocytoma P-815 cells. SM-10906 displaced [3H]iloprost binding to the membrane fraction, the IC50 value being 100 nM, but showed very low affinity for the prostaglandin E (PGE) receptor. SM-10906 dose-dependently stimulated GTP-dependent adenylate cyclase activity in the membrane fraction, the EC50 value being 35 nM. Furthermore, SM-10906 prevented a thrombin-induced increase in the intracellular Ca2+ concentration, the IC50 value being 300 nM. These IC50 and EC50 values are much lower than those of SM-10902. These results demonstrate that SM-10906, a stable PGI1 derivative, is an agonist for the [3H]iloprost-binding (PGI2) receptor, and that it prevents thrombin-induced Ca2+ mobilization through stimulation of the adenylate cyclase system in mastocytoma cells. On the other hand, a methyl ester derivative of PGI1, SM-10902, was inactive in the binding assay, but it seems to be a partial agonist for adenylate cyclase activity [corrected].
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Oka M,Negishi M,Yamamoto T,Satoh K,Hirohashi T,Ichikawa Adoi
10.1248/bpb.17.74subject
Has Abstractpub_date
1994-01-01 00:00:00pages
74-7issue
1eissn
0918-6158issn
1347-5215journal_volume
17pub_type
杂志文章abstract::Carvedilol, an alpha- and beta-adrenergic blocking drug, is mainly metabolized by CYP2D6, UGT1A1, UGT2B4 and UGT2B7. This drug is administered orally as a racemic mixture of R(+)- and S(-)-enantiomers. It has been reported that CYP2D6 prefers metabolizing S-carvedilol to R-carvedilol stereoselectively. On the other ha...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.30.2146
更新日期:2007-11-01 00:00:00
abstract::The extracellular signal-regulated kinase (ERK) pathway is a major determinant in the control of diverse cellular processes such as proliferation, survival, and motility. This pathway is often upregulated in human cancers and as such represents an attractive target for mechanism-based approaches to cancer treatment. H...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.34.1781
更新日期:2011-01-01 00:00:00
abstract::Nafamostat mesilate, an ester drug with extensive hydrolysis in vivo, exhibits species difference in the relative contribution for its hydrolysis in blood and tissues. For the rat, the main hydrolysis site may be blood and human may be tissue (mainly by liver). The paper gave in vivo evidence that human tissue may giv...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.1985
更新日期:2008-11-01 00:00:00
abstract::Escherichia coli BM2506 produced macrolide 2'-phosphotransferase II [MPH (2') II]. A gene for MPH (2') II, designated mphB, is located on plasmids pTZ3721 and pTZ3723 in E. coli BM2506. In the present study, we determined the nucleotide sequence of the 6.5-kb EcoRI-PstI fragment containing mphB on pTZ3721. The DNA reg...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.227
更新日期:1999-02-01 00:00:00
abstract::We have previously proposed a novel deconvolution method, which can estimate first-pass metabolism of orally administered drugs. In the present study, we examined whether this deconvolution method is useful for evaluating oral dosage forms. The absorption and first-pass metabolism of orally administered aspirin formul...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.1212
更新日期:1999-11-01 00:00:00
abstract::It is well established that vesicular nucleotide transporter (VNUT) is responsible for vesicular storage of nucleotides such as ATP, and that VNUT-expressing cells can secrete nucleotides upon exocytosis, playing an important role in purinergic chemical transmission. In the present study, we show that VNUT is expresse...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b14-00275
更新日期:2014-01-01 00:00:00
abstract::We earlier reported that collagen synthesis in false aged model rats was stimulated by the administration of a methanol extract from the leaves of Eucommia ulmoides OLIVER. When the methanol extract was fractionated to n-hexane, ethyl acetate, acetone and methanol fractions by silica gel chromatography, we discovered ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.582
更新日期:1999-06-01 00:00:00
abstract::It has been identified that skeletal muscle is an endocrine tissue. Since skeletal muscle aging affects not only to muscle strength and function but to systemic aging and lifespan, myokines secreted from skeletal muscle may be crucial factors for intertissue communication during aging. In the present study, we investi...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b17-00969
更新日期:2018-01-01 00:00:00
abstract::P2X7 receptor (P2X7R), a purinergic receptor, is involved in pathophysiological events such as inflammation and cell death, and thus is an attractive target for therapeutic approaches. It is reported that divalent metal cations (DMCs) inhibit P2X7R activation and that there are species differences in their inhibitory ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b16-00887
更新日期:2017-01-01 00:00:00
abstract::Microanalytical methods were developed for measuring galactosyl-beta-cyclodextrin (Gal-betaCD) and mannosyl (Man)-betaCD in biological matrices of the rat by HPLC with pulsed amperometric detection. Then, using these methods, the absorption, distribution and excretion of intravenously and orally administered Gal-betaC...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.23.472
更新日期:2000-04-01 00:00:00
abstract::This study aims to determine the potential renal protective effects of Opuntia ficus-indica (L.) Miller (OFI) fruits against cisplatin-induced nephrotoxicity in mice. The antioxidant activity of OFI methanol extract was calculated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulfo...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b19-01044
更新日期:2020-01-01 00:00:00
abstract::This study was conducted to determine the beneficial effects of treating digestive disorders of (6E,12E)-tetradecadiene-8,10-diyne-1,3-diol diacetate (TDEYA) detected in the plasma in hydrolyzed form: (6E,12E)-tetradecadiene-8,10-diyne-1,3-diol (TDEY), following the oral administration of a decoction of Atractylodes r...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1364
更新日期:1994-10-01 00:00:00
abstract::Propiverine hydrochloride, oxybutynin hydrochloride and terodiline hydrochloride have both anticholinergic and antispasmodic effects, and are used for the management of urinary frequency and incontinence. The average standard therapeutic doses of these drugs differ greatly. We retrospectively analyzed their pharmacolo...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.30.1297
更新日期:2007-07-01 00:00:00
abstract::The anti-inflammatory effects of 1,6-anhydro-3,4-dideoxy-2-furfuryl-beta-D-threo-3-enopyranose (MT2221) were investigated using animal models and compared with the effects of dexamethasone (DEX) and cyclosporin A (CYA). MT2221 inhibited carrageenan-induced acute inflammation and adjuvant arthritis in rats, as well as ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1070
更新日期:1994-08-01 00:00:00
abstract::Coffee is a popular beverage worldwide with various nutritional benefits. Diterpene cafestol, one of the major components of coffee, contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects. In thi...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.128
更新日期:2010-01-01 00:00:00
abstract::As an attempt to find bioactive medicinal herbs exerting anti-asthmatic activity, the effects of an ethanol extract from the parts of Saururus chinensis were evaluated in both in vitro and in vivo. The ethanol extract of S. chinensis (ESC) inhibited generation of the cyclooxygenase-2 (COX-2) dependent phases of prosta...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.211
更新日期:2006-02-01 00:00:00
abstract::The present study was performed to investigate the effects of histamine H(1)-antagonists on the sleep-awake state in rats placed on a grid suspended over water in comparison with rats placed on sawdust. When rats were placed on the grid suspended over water, significant increases in the awake time and decreases in non...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.51
更新日期:2009-01-01 00:00:00
abstract::This study was designed to evaluate the protective effect of kolaviron (KV), a biflavonoid from Garcinia kola seeds, against gamma-radiation (5 Gy)-induced oxidative stress in brain of Wistar rats. Vitamin C (VC) served as standard antioxidant. Forty-four rats were divided into 4 groups of 11 animals each. One group w...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.260
更新日期:2010-01-01 00:00:00
abstract::Plasma hyaluronan biding protein (PHBP) is a novel serine protease, which has an amino acid sequence homology to that of hepatocyte growth factor activator (HGFA), and has a similar domain structure to that of urinary plasminogen activator (u-PA), found in human plasma. We searched the PHBP substrate in human plasma b...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.24.140
更新日期:2001-02-01 00:00:00
abstract::Radiation induces an important inflammatory response in the irradiated organs, characterized by leukocyte infiltration and vascular changes. Since adhesion molecules play an important role in facilitating the immune response at the inflammation sites, interfering with the expression of these molecules may be an import...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.752
更新日期:2010-01-01 00:00:00
abstract::Doxorubicin (DOX) is a potent antitumor agent, but the cardiotoxicity mediated by the formation of reactive oxygen species limit its clinical use. The present study aims to explore electrocardiographic and biochemical evidence for the cardioprotective effect of two antioxidants, Lycium barbarum polysaccharides (LBP, t...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.1523
更新日期:2011-01-01 00:00:00
abstract::Cancer is one of the leading causes of death in the world. The triterpenoid compound asiatic acid derived from the tropical medicinal plant Centella asiatica displays cytotoxic activity on fibroblast cells and several other kinds of cells. The present work studies asiatic acid-mediated growth inhibition of cancer cell...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.1399
更新日期:2009-08-01 00:00:00
abstract::Apocynum venetum LINN. is an important Chinese crude drug, and its sibling species A. pictum SCHRENK is a confusable herb which is similar to it. The purpose of this study is to develop DNA molecular markers to distinguish A. venetum from A. pictum through the combinative technologies of bulked segregate analysis (BSA...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.522
更新日期:2010-01-01 00:00:00
abstract::We investigated the effects of restraint and footshock stress and norepinephrine treatment on gastric emptying. The gastric emptying was significantly inhibited by restraint stress. beta(3)-adrenergic antagonist canceled the inhibition of gastric emptying caused by restraint stress, while beta(1)-, beta(2)-, alpha(1)-...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.26.368
更新日期:2003-03-01 00:00:00
abstract::Antioxidant property and hematopoietic repair capacity are important characteristics of radioprotective agents. Some studies have demonstrated that 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG), a molecule isolated from the waterlily, has antioxidant, hematopoietic repair, and anti-inflammatory activities. In this st...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.1122
更新日期:2010-01-01 00:00:00
abstract::In a previous study we found that 50% ethanol extracts of immature fruits of Citrus unshiu (satsuma mandarin) have anti-allergic effects against the Type I, II and IV allergic reactions. However, many adverse interactions between citrus fruit, especially grapefruit juice, and drugs have been reported due to the inhibi...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.31.925
更新日期:2008-05-01 00:00:00
abstract::In order to prepare fine granules of sparfloxacin (SPFX), a new quinolone anti-bacterial drug that shows masking of the bitter taste of SPFX and dissolutes at a rapid rate, various film-coated fine granules containing 20% SPFX and 0-52% low-substituted hydroxypropylcellulose(L-HPC) in the cores, were prepared by a spr...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.16.172
更新日期:1993-02-01 00:00:00
abstract::Telekin, a eudesmane-type sesquiterpene lactone compound isolated from Chinese folk medicine Carpesium divaricatum, has been reported to strongly inhibit the proliferation of cancer cells. In this study, the involvement of a mitochondria-mediated pathway in the pro-apoptotic action of telekin was investigated in human...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b13-00058
更新日期:2013-01-01 00:00:00
abstract::The roles of OmpC and OmpF in acidic resistance (AR) were examined. When ompC and ompF were deleted, AR was decreased. The decreased level of AR seen in the mutant that was deficient in ompC and ompF was elevated by the addition of glutamate, but not by the addition of arginine or lysine. The expression levels of adiA...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.330
更新日期:2011-01-01 00:00:00
abstract::Effects of epidermal growth factor (EGF) on the expression of alpha(2)-adrenergic responses were examined in primary cultures of adult rat hepatocytes. The alpha(2)-responses were assessed by the inhibition of the rate of forskolin-stimulated cAMP formation by the selective alpha(2)-adrenergic agonists, oxymetazoline ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.19.518
更新日期:1996-04-01 00:00:00