Abstract:
:Each testosterone [125I]iodinated histamine derivative where [125I]iodinated histamines were linked to respective 15 alpha- and 15 beta-carboxymethyltestosterone (15 alpha- and 15 beta-CMT), testosterone-3-(O-carboxymethyl)oxime (T-3-CMO) and testosterone-17 beta-hemisuccinate (T-17-HS) were tested for their usefulness as radiotracers in testosterone immunoassay. In the use of anti-15 alpha- and 15 beta-CMT antisera produced in rabbits against 15 alpha- and 15 beta-CMT-bovine serum albumin (BSA) conjugates, the antisera with 15 alpha- and 15 beta-CMT-[125I]iodinated tracers showed low sensitivity and somewhat low specificity in comparison with those of the antisera with tritiated testosterone (T-3H). On the other hand, the antisera with T-3-CMO-[125I]iodinated tracer showed high sensitivity but low specificity for 5 alpha-dihydrotestosterone (5 alpha-DHT) in comparison with T-3H. The T-17-HS-[125I]iodinated tracer was not bound to the antisera. In the use of anti-15 alpha- and 15 beta-CMT antisera produced in rabbits by pretreatment with 15 alpha-carboxymethyl-5 alpha-DHT linked to a copolymer of D-glutamic acid and D-lysine followed by immunization with 15 alpha- and 15 beta-CMT-BSA, the antisera with homologous [125I]iodinated tracer showed high sensitivity and specificity.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Miyake Y,Shigetoshi M,Kojima Mdoi
10.1248/cpb.38.951subject
Has Abstractpub_date
1990-04-01 00:00:00pages
951-5issue
4eissn
0009-2363issn
1347-5223journal_volume
38pub_type
杂志文章abstract::A novel series of furan-2-one and pyrrolin-2-one derivatives having PAI-1 (plasminogen activator inhibitor-1) inhibitory activity were synthesized and evaluated for their antithrombotic activity in a rat arterial thrombosis model. Among the synthesized compounds, 5f (T-1776Na) was found to have good selectivity for PA...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.57.979
更新日期:2009-09-01 00:00:00
abstract::A series of substituted 6,7-dihydro-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acids was synthesized and tested for antibacterial activities. Among them, 9-fluoro-6,7-dihydro-5-methyl-8-(4-methyl-1-piperazinyl)-1-oxo-1H,5H- benzo[i,j]quinolizine-2-carboxylic acid (OPC-7241) exhibited potent antibacterial activity ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.37.2103
更新日期:1989-08-01 00:00:00
abstract::Two coumarins and one polyacetylene, 5-0-(3-chloro-2-hydroxy-3-methylbutyl)-8-methoxypsoralen (1), 2',3'-dihydro-jatamansin (2), and 10-chloro-1-heptadecene-4,6-diyne-3,8,9-triol (3), along with 15 known compounds (4-18), were isolated from the methanol extract of Niphogeton ternata. Their structures were elucidated b...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.50.115
更新日期:2002-01-01 00:00:00
abstract::The attachment of various drugs bearing -NH2 groups to poly-alpha,beta-aspartic acid as a biodegradable carrier afforded in good yields macromolecular prodrugs which were characterized with respect to composition and drug load by spectroscopic and analytical methods. N-Ethyl-N'-(3-dimethylaminopropyl)carbodiimide hydr...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.37.2245
更新日期:1989-08-01 00:00:00
abstract::Rapid and precise compositional analysis of copoly (DL-lactic/glycolic acid) (PLGA) was performed by pyrolysis-gas chromatography/mass spectrometry (Py-GC/MS) combined with one-step hydrolysis and methylation in the presence of tetramethylammonium hydroxide (TMAH). Pyrolysis of PLGA with TMAH gave two characteristic p...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.49.203
更新日期:2001-02-01 00:00:00
abstract::The purpose of this study was to predict the stability of meropenem in a mixed infusion. The hydrolysis of meropenem in aqueous solution was found to be accelerated by pH, and by increasing concentrations of sodium bisulfite (SBS) and L-cysteine. Equations were derived for the degradation rate constants (kobs) of pH, ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c14-00516
更新日期:2015-01-01 00:00:00
abstract::Of 4-amino-5-chloro-2-methoxy-N-(1-ethyl-2-hydroxymethyl-4- pyrrolidinyl)benzamide, four optical isomers, (2S,4S)-1 (TKS159), (2S,4R)-25, (2R,4S)-26 and (2R,4R)-27, were prepared from optically active 4-amino-1-ethyl-2-hydroxymethylpyrrolidine di-p-toluenesulfonate [(2S,4S)-14, (2S,4R)-17, (2R,4S)-20 and (2R,4R)-23, r...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.47.1650
更新日期:1999-11-01 00:00:00
abstract::A new cycloartane bisdesmoside and two new trinorcycloartane glycosides, along with four known cycloartane compounds, were isolated from the rhizomes of Cimicifuga dahurica (Ranunculaceae). The structures of the new compounds were elucidated as 3-O-alpha-L-arabinopyranosyl cimigenol 15-O-beta-D-glucopyranoside, 24-hyd...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.49.1468
更新日期:2001-11-01 00:00:00
abstract::In the course of our research on spiro-compounds as neurokinin receptor antagonists, N-[2-aryl-4-(spiro-substituted piperidin-1'-yl)butyl]carboxamides were designed, based on YM-35375 (3) as a lead compound, and evaluated for NK2 receptor-antagonistic activities. Some derivatives inhibited the binding of radio-labeled...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.46.242
更新日期:1998-02-01 00:00:00
abstract::To find novel PPAR ligands, we prepared several 3-{3 or 4-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives which were designed based on the structure of our previous PPARgamma ligand 1. In PPAR binding affinity assays, compound 4, which had an ethoxy group at the C-2 position of the propanoic acid o...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.55.1053
更新日期:2007-07-01 00:00:00
abstract::Six new cyclic peptides, gypsophin A-F (1-6), were isolated from Gypsophila oldhamiana. Their structures were elucidated by extensive NMR and chemical degradation. Compound 3 exhibited moderate activity of antiplatelet aggregation in vitro. ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c12-01094
更新日期:2013-01-01 00:00:00
abstract::Hyosgerin, a new optically active coumarinolignan, has been isolated and characterized along with three other coumarinolignans, venkatasin, cleomiscosin A and cleomiscosin B, from the seeds of Hyoscyamus niger L. The structure was determined on the basis of spectroscopic analysis and chemical conversion. The optical p...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.54.538
更新日期:2006-04-01 00:00:00
abstract::Three new spirostanol glycosides (1-3) and a new furostanol glycoside (4), together with two known spirostanol glycosides (5 and 6) were isolated from the whole plants of Agave utahensis (Agavaceae). The structures of the new compounds were determined by spectroscopic analysis and the results of hydrolytic cleavage. ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.55.145
更新日期:2007-01-01 00:00:00
abstract::An efficient synthesis of the antiviral and antioxidative chromene (1) was achieved. A small amount of chromene 1 could be derived from plastoquinones 2 and 3, the major constituents of the brown alga, Sargassum micracanthum. By the following synthetic scheme involving its application, many kinds of analogs can be syn...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.54.391
更新日期:2006-03-01 00:00:00
abstract::A new ent-kaurane diterpene glycoside, beta-D-glucopyranosyl 17-hydroxy-ent-kauran-19-oate-16-O-beta-D-glucopyranoside (4) was isolated from the dried leaves of Cussonia bojeri SEEM., together with four known compounds identified as 16beta,17-dihydroxy-kauran-19-oic acid (1), beta-D-glucopyranosyl 16beta,17-dihydroxy-...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.50.1122
更新日期:2002-08-01 00:00:00
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
abstract::First, Raddeanin A, a cytotoxic oleanane-type triterpenoid saponin isolated from Anemone raddeana REGEL, was synthesized. Stepwise glycosylation was adopted in the synthesis from oleanolic acid, employing arabinosyl, glucosyl and rhamnosyl trichloroacetimidate as donors. The chemical structure of Raddeanin A was confi...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c14-00138
更新日期:2014-01-01 00:00:00
abstract::A new cytotoxic substance, designated russuphelin A (1), has been isolated from the mushroom Russula subnigricans Hongo (Basidiomycetes). The structure was elucidated as 2,6-bis(2,6-dichloro-4-hydroxyphenyloxy)-1,4-dimethoxy-benzene on the basis of spectroscopic data and confirmed by total synthesis. ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.40.3185
更新日期:1992-12-01 00:00:00
abstract::A series of 1,2,3,4-tetrahydroisoquinoline derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton were prepared and evaluated for their in vitro binding affinities to muscarinic receptors and for antagonism of bradycardia in vivo. Among them, compound 3f had the highest affinity for ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.47.672
更新日期:1999-05-01 00:00:00
abstract::A novel series of 2-acyl-3-carboxyl-tetrahydroisoquinoline derivatives were synthesized and biologically evaluated. Among them, (S)-2-{(E)-3-furan-2-ylacryloyl}-7-[(2E,4E)-5-(2,4,6-trifluorophenyl)penta-2,4-dienyloxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (compound 17u) was identified as a potent protein ty...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c18-00571
更新日期:2018-01-01 00:00:00
abstract::The sugar-inositol portion of the novel glycosylinositol-phosphoceramides, ZGL1 and ZGL2, from the filamentus fungi, Acremonium sp., were elucidated by a combination of NMR techniques including (1)H-(1)H (COSY and HOHAHA) and (1)H-(13)C (HMQC and HMBC) spectroscopy. Further, examination of the (1)H-(31)P HMQC spectrum...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.52.473
更新日期:2004-04-01 00:00:00
abstract::A new stilbene, 4-[(2"E)-7"-hydroxy-3",7"-dimethyloct-2"-enyl]-2',3,4',5-tetrahydroxy-trans-stilbene (1), and the known compound chlorophorin (2) were isolated from the heartwood of Chlorophora excelsa. Both 1 and 2 showed tyrosinase inhibitory activity with IC(50) values of 96 and 1.3 microM, respectively. ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.51.318
更新日期:2003-03-01 00:00:00
abstract::The metabolites of clentiazem in the urine or bile of rats and dogs were investigated. Fifteen basic, 6 acidic, 2 neutral and 4 conjugated metabolites were isolated. In the present paper, fourteen reference compounds as shown in Charts 1, 2 and 3 were synthesized to identify the structures of the metabolites in proced...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.42.167
更新日期:1994-01-01 00:00:00
abstract::The rates of release of nicotinamide (NAA) from fatty acid (FA)-NAA complexes, FA-NAA, were determined at various temperatures, and the thermodynamic quantities for the release of NAA were estimated. The results were compared with the previous results obtained for FA-thiamine disulfide (TDS) complexes, (FA)6(TDS). The...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.39.3114
更新日期:1991-12-01 00:00:00
abstract::We investigated the kinetics of in vitro transformation of a dichlorinated propyl paraben (2-propyl 3,5-dichloro-4-hydroxybenzoate; Cl2PP) by the rat liver S9 fraction and assessed the aryl hydrocarbon receptor (AhR) agonist activity of the metabolite products identified in HPLC and GC/MS analysis and by metabolite sy...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c15-00977
更新日期:2016-01-01 00:00:00
abstract::A highly sensitive spectrophotometric determination of human serum albumin (HSA) with 3',4',5',6'-tetrachlorogallein (T.Cl.Gall)-Mo(VI) complex in a Triton X-100 + polyvinyl alcohol micellar medium is proposed. This method can be used to determine up to ca. 150 micrograms/10 ml of HSA from the optical absorbance at 64...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.37.2452
更新日期:1989-09-01 00:00:00
abstract::We describe here a Tf₂NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes signi...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.59.1190
更新日期:2011-01-01 00:00:00
abstract::The effect of chromomycin A3 binding on the geometry of DNA duplex (plasmid pBR322) has been examined using topoisomerase I relaxation followed by gel electrophoresis. To determine the equilibrium constant of this drug-DNA binding-dissociation reaction in the same concentration range (ca. 10(-5) M) in the same buffer ...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.46.1667
更新日期:1998-11-01 00:00:00
abstract::We report a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis of CDK2 inhibitors using fragment molecular orbital (FMO) calculations and partial least squares (PLS) regression. In our analysis, fragment binding energies of individual amino acids and fragment binding energy of a single l...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.c18-00990
更新日期:2019-01-01 00:00:00
abstract::A new 9,19-cyclolanostane-type triterpene xyloside (1), from the rhizomes of Cimicifuga racemosa, has been isolated together with four known saponins; cimiaceroside A, 25-O-methylcimigenol-3-O-beta-D-xylopyranoside, 27-deoxyactein and 23-O-acetylshengmanol-3-O-beta-D-xylopyranoside. The structure of the new compound w...
journal_title:Chemical & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/cpb.48.425
更新日期:2000-03-01 00:00:00