Discovery of a Novel Class of State-Dependent NaV1.7 Inhibitors for the Treatment of Neuropathic Pain.

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

authors： Watanabe Y,Matsumoto Y,Seki M,Takase M,Matsumoto M

更新日期：1992-11-01 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

authors： Giammona G,Giannola LI,Carlisi B,Bajardi ML

更新日期：1989-08-01 00:00:00

abstract：:Alkylidenemalonates were readily dimerized in the presence of SmI2 to give 2,3-disubstituted 1,1,4,4-butanetetracarboxylates as mixtures of meso and racemic isomers in moderate to good yields. The structure of the less polar isomer of tetraethyl 2,3-diphenyl-1,1,4,4-butanetetracarboxylate was determined by X-ray cryst...

journal_title：Chemical & pharmaceutical bulletin

authors： Yamashita M,Okuyama K,Kawasaki I,Nakamura S,Nagamine R,Tsujita T,Ohta S

更新日期：2000-11-01 00:00:00

abstract：:A new polyhydroxy sterol ester, (25S)-5alpha-cholestane-3beta,6alpha,7alpha,8,15alpha,16beta-hexahydroxyl-26-O-14'Z-eicosenoate (1), together with seven known steroid derivatives (2-8), were isolated from the EtOH extract of the whole body of China Sea starfish Asterina pectinifera. The structure of 1 was determined b...

journal_title：Chemical & pharmaceutical bulletin

authors： Peng Y,Zheng J,Huang R,Wang Y,Xu T,Zhou X,Liu Q,Zeng F,Ju H,Yang X,Liu Y

更新日期：2010-06-01 00:00:00

abstract：:Indoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest because in vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically active analogs of these compounds, we developed a synthesis based on the photocyclization of tertiary ...

journal_title：Chemical & pharmaceutical bulletin

authors： Aragon PJ,Yapi AD,Pinguet F,Chezal JM,Teulade JC,Blache Y

更新日期：2007-09-01 00:00:00

abstract：:A new flavonol triglycoside, isorhamnetin 3-O-beta-D-xylopyranosyl-(1"-->3)-alpha-L-rhamnopyranosyl-(1'''-->6")-beta-D-galactopyranoside, has been isolated from the leaves of Hammada scoparia together with two known compounds, isorhamnetin 3-O-beta-D-apiofuranosyl-(1'''-->2")[alpha-L-rhamnopyranosyl-(1"-->6")]-beta-D-...

journal_title：Chemical & pharmaceutical bulletin

authors： Ben Salah H,Jarraya R,Martin MT,Veitch NC,Grayer RJ,Simmonds MS,Damak M

更新日期：2002-09-01 00:00:00

abstract：:Possible utility of hydroxyalkylated beta-cyclodextrin (beta-CyD) derivatives as parenteral drug carriers was investigated, using nimodipine, a dihydropyridine derivative with calcium antagonistic action, as a model drug. The aqueous solubility of nimodipine increased linearly with increase in the concentration of hyd...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida A,Yamamoto M,Itoh T,Irie T,Hirayama F,Uekama K

更新日期：1990-01-01 00:00:00

abstract：:The admixture of a steroid ointment and a moisturizing cream is frequently prescribed to patients suffering from atopic dermatitis. For the mixing operation, a revolution/rotation-type hybrid mixer is widely used in pharmacy. The purpose of this study was to monitor the mixed state of the admixtures during the mixing ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yokokawa M,Setoyama H,Okada K,Hayashi Y,Machida Y,Onuki Y,Obata Y

更新日期：2018-01-01 00:00:00

abstract：:A new isoflavone, 4'-gamma,gamma-dimethylallyloxy-5,7,2',5'-tetramethoxyisoflavone, brandisianin A (1), was isolated from the leaves of Millettia brandisiana, along with one synthetically known isoflavone, 7,4'-di-O-prenylgenistein (2) and twelve known compounds. The structures were elucidated on the basis of extensiv...

journal_title：Chemical & pharmaceutical bulletin

authors： Pancharoen O,Athipornchai A,Panthong A,Taylor WC

更新日期：2008-06-01 00:00:00

abstract：:Bioassay-directed fractionation of the extract of the cyanobacterium P. tenue led to the isolation of the three classes of glycolipids, viz., monogalactosyl diacylglycerol (MGDG), digalactosyl diacylglycerol (DGDG), and sulfoquinovosyl diacylglycerol (SQDG) as anti-tumor-promoters. In comparing the anti-tumor-promotin...

journal_title：Chemical & pharmaceutical bulletin

authors： Shirahashi H,Murakami N,Watanabe M,Nagatsu A,Sakakibara J,Tokuda H,Nishino H,Iwashima A

更新日期：1993-09-01 00:00:00

abstract：:A prevention method of the sorption of bromhexine HCl to plastic materials used in packaging was investigated. Four kinds of plastic packaging materials were used: Polyethylene (PE), polyethylene terephthalate (PET), polypropylene (PP) and polyacrylonitrile (PAN). Three polyethylenes having different densities were us...

journal_title：Chemical & pharmaceutical bulletin

authors： Kukita T,Furuuchi S,Nemoto M,Yoshida T

更新日期：1992-11-01 00:00:00

abstract：:N-9-Fluorenylmethoxycarbonyl-Se-4-methoxybenzylselenocysteine++ + [Fmoc-Sec(MBzl)-OH] was synthesized from selenocystine and successfully applied to Fmoc-based solid-phase peptide synthesis. The stability and the deprotection conditions of the Se-MBzl group were examined. The diselenide bond of a peptide was directly ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koide T,Itoh H,Otaka A,Yasui H,Kuroda M,Esaki N,Soda K,Fujii N

更新日期：1993-03-01 00:00:00

abstract：:Different crystal packing of hydrates from anhydrate crystals leads to different physical properties, such as solubility and stability. Investigation of the potential of varied hydrate formation, and understanding the stability in an anhydrous/hydrate system, are crucial to prevent an undesired transition during the m...

journal_title：Chemical & pharmaceutical bulletin

authors： Takeuchi S,Kojima T,Hashimoto K,Saito B,Sumi H,Ishikawa T,Ikeda Y

更新日期：2015-01-01 00:00:00

abstract：:To understand more fully the effect of polyunsaturated fatty acids (PUFAs) on lipid bilayers, we investigated the effects of treatment with fatty acids on the properties of a model membrane. Three kinds of liposomes comprising dipalmitoylphosphatidylcholine (DPPC), dioleylphosphatidylcholine (DOPC), and cholesterol (C...

journal_title：Chemical & pharmaceutical bulletin

authors： Onuki Y,Hagiwara C,Sugibayashi K,Takayama K

更新日期：2008-08-01 00:00:00

abstract：:Bis[2-[(E)-2-octenoylamino]ethyl] disulfide (compd. I-3) inhibited collagen- and arachidonic acid-induced rat platelet aggregation, although not adenosine 5'-diphosphate (ADP)-induced rat platelet aggregation. Based on these results, we then investigated the inhibitory effect of compd. I-3 on thromboxane B2 formation ...

journal_title：Chemical & pharmaceutical bulletin

authors： Mimura T,Nakajima H,Tsujikawa K,Yasuda N,Haruyama M,Okabe M,Iwai M,Yokoyama K

更新日期：1989-03-01 00:00:00

abstract：:The Pictet-Spengler reaction of tryptamine type 1,2-dihydropyridine 5c derived from the cycloaddition of the sec-nitrodienamine 3c with acetaldehyde afforded the indoloquinolizine derivatives 6 and 7. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Koike T,Shinohara Y,Tobinaga S,Takeuchi N

更新日期：2000-12-01 00:00:00

abstract：:The abnormal aggregation of amyloid β-peptide (Aβ) is central to the pathogenesis of Alzheimer's disease, the major form of dementia. Aromatic π-π interactions have been suggested to play a crucial role in the aggregation of not only Aβ, but also other amyloidogenic proteins. In this study, each or all phenylalanine (...

journal_title：Chemical & pharmaceutical bulletin

authors： Genji M,Yano Y,Hoshino M,Matsuzaki K

更新日期：2017-01-01 00:00:00

abstract：:To experimentally clarify a possible stereostructure-activity relationship proposed for H2-receptor antagonists, three 5-aminophenylimidazoles (1, 2 and 3), in which respective amino groups are located on the ortho, meta and para positions of the benzene ring, were synthesized and examined for their conformational cha...

journal_title：Chemical & pharmaceutical bulletin

authors： Ishida T,In Y,Inoue M,Kurihara T,Moriomoto K,Morisaka K,Shibata K

更新日期：1990-07-01 00:00:00

abstract：:The objective of this study was to synthesize several new pregnane derivatives and evaluate them as antiandrogens. From the commercially available 16-dehydropregnenolone acetate (7), two new steroidal compounds were synthesized: 17alpha-hydroxy-17beta-methyl-16beta-phenyl-D-homoandrosta-1,4,6-triene-3,20-dione (18) an...

journal_title：Chemical & pharmaceutical bulletin

authors： Cabeza M,Heuze I,Bratoeff E,Ramírez E,Martínez R

更新日期：2001-05-01 00:00:00

abstract：:Hydrophobically modified hydroxypropyl methylcellulose (HM-HPMC), a polymer in which a small amount of HPMC is stearoxyl substituted, was used as an emulsifier of emulsion-type lotion. A high-pressure homogenizer (microfluidizer) was used. The viscosity of the 1% HM-HPMC aqueous gel decreased after passing through the...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujii M,Wada F,Honda N,Miura K,Hashizaki K,Taguchi H,Koizumi N,Watanabe Y

更新日期：2020-01-01 00:00:00

abstract：:Panaxacol (1) and dihydropanaxacol (2), cytotoxic polyacetylenes isolated from the callus of Panax ginseng, were synthesized starting from D-(-)-diethyl tartrate. The absolute configuration of 1 was determined to be 9R, 10R and the absolute configuration at C-3 of 2 was tentatively assigned as 3S by the application of...

journal_title：Chemical & pharmaceutical bulletin

authors： Fujimoto Y,Satoh M,Takeuchi N,Kirisawa M

更新日期：1990-06-01 00:00:00

abstract：:The purpose of this study was to predict the stability of imipenem in a mixed infusion. The hydrolysis of imipenem 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 (k(obs)) of pH, ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshida M,Takasu Y,Shimizu K,Asahara K,Uchida T

更新日期：2013-01-01 00:00:00

abstract：:Colon-specific drug delivery systems (CDDS) can improve the bioavailability of drug through the oral route. A novel formulation for oral administration using pH-enzyme Di-dependent chitosan mcirospheres (MS) and 5-Fu as a model drug has been investigated for colon-specific drug delivery by the emulsification/chemical ...

journal_title：Chemical & pharmaceutical bulletin

authors： Zhao XL,Li KX,Zhao XF,Pang DH,Chen DW

更新日期：2008-07-01 00:00:00

abstract：:A high-performance liquid chromatographic method and a UV derivative spectrophotometric method for the determination of famciclovir, a highly active antiviral agent, in tablets were developed in the present work. The various parameters, such as linearity, precision, accuracy, specificity, robustness, limit of detectio...

journal_title：Chemical & pharmaceutical bulletin

authors： Srinubabu G,Sudharani B,Sridhar L,Rao JS

更新日期：2006-06-01 00:00:00

abstract：:Fifteen triterpenoid saponins were isolated from the berries of Hedera colchica and their structures established on the basis of chemical and spectroscopic evidence. Among them, two are new compounds: coichiside A (3) and colchiside B (15) and four are described for the first time in the berries of Hedera colchica (co...

journal_title：Chemical & pharmaceutical bulletin

authors： Mshvildadze V,Elias R,Faure R,Debrauwer L,Dekanosidze G,Kemertelidze E,Balansard G

更新日期：2001-06-01 00:00:00

abstract：:Four new lignans, 3',4'-O,O-demethylenehinokinin (1), chamalignolide (2), 8'beta-hydroxyhinokinin (3) and 7beta,8beta-epoxyzuonin A (4), as well as (-)-hinokinin (5), and (-)-zuonin A (6), were isolated from the heartwood of Chamaecyparis obtusa var. formosana. The structures of these lignans were unambiguously determ...

journal_title：Chemical & pharmaceutical bulletin

authors： Kuo YH,Chen CH,Lin YL

更新日期：2002-07-01 00:00:00

abstract：:Stereocontrolled syntheses of model compounds related to a major antigenic epitope against antibupleurum 2IIc/PG-1-IgG from antiulcer pectic polysaccharide are described. A trisaccharide derivative (13) was prepared as a precursor and a novel and simple approach for the rational design of a glycocluster and glycodendr...

journal_title：Chemical & pharmaceutical bulletin

authors： Jin Y,Hada N,Oka J,Kanie O,Daikoku S,Kanie Y,Yamada H,Takeda T

更新日期：2006-04-01 00:00:00

abstract：:Cornusiin A (1), cornusiin B (2) and cornusiin C (3), new dimeric, monomeric and trimeric hydrolyzable tannins, were isolated from the fruits of Cornus officinalis (Cornaceae). Their structures, including the orientation of the valoneoyl group in 1 and 3, were established on the basis of chemical and spectroscopic dat...

journal_title：Chemical & pharmaceutical bulletin

authors： Hatano T,Ogawa N,Kira R,Yasuhara T,Okuda T

更新日期：1989-08-01 00:00:00

abstract：:From the bark of Cryptomeria japonica were isolated sugikurojins I (1) and J (2), and an abietane derivative (3) was obtained for the first time as a natural product. These structures were elucidated primarily through extensive NMR experiments. Sugikurojin I (1) has a unique skeleton incorporating an abietane diterpen...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshikawa K,Suzuki K,Umeyama A,Arihara S

更新日期：2006-04-01 00:00:00

abstract：:Alpha-trifluoromethyl allenol ethers 9a-e were prepared in moderate to good yields by the Julia-Lythgoe process using beta-ethoxy-beta-trifluoromethyl vinylic sulfone 3. Several reactions of 9c were examined to give alpha,beta-unsaturated trifluoromethyl ketone derivatives 11 and 12. ...

journal_title：Chemical & pharmaceutical bulletin

authors： Yoshimatsu M,Hibino M

更新日期：2000-09-01 00:00:00