Nitrile-promoted Rh-catalyzed intermolecular hydroacylation of olefins with salicylaldehyde.

Rh-catalyzed intermolecular hydroacylation between salicylaldehyde and alkenylnitriles proceeded at room temperature to preferentially give normal-hydroacylated products. Addition of CH3CN and NaOAc accelerated the Rh-catalyzed hydroacylation of monoolefins to exclusively produce the normal-hydroacylated products under mild reaction conditions. Plausible mechanisms for the regioselections are also described.

Alteration of 5-HIAA levels in frontal cortex and dorsal raphe nucleus in rats treated with combined administration of tryptophan and ethanol.

The present studies sought to investigate the effect of tryptophan alone or coadministration of tryptophan and ethanol on the interaction of central frontal cortex and dorsal raphe nucleus serotonergic functional activities by utilizing in vivo microdialysis. Tryptophan (50 mg/kg, i.p.

[Analysis by structural equation modeling of the questionnaire about the risk and its preventive measures in a pharmacy].

Pharmacists are now facing a problem of developing measures for dispensing mistakes, because there recently is increasing social awareness on medical accidents and a tendency to increase medical accidents in pharmacies due to popularizing separation of dispensing and prescribing functions. In this study, questionnaire survey was conducted to investigate pharmacist's views on human error measures and the relationship between mistakes and the preventive measures. To clarify relationship between human error measures and preventive measures for avoiding mistakes, questionnaire result was analyzed based on structural equation modeling (SEM).

NO-1886 (ibrolipim), a lipoprotein lipase-promoting agent, accelerates the expression of UCP3 messenger RNA and ameliorates obesity in ovariectomized rats.

The synthetic compound NO-1886 (ibrolipim, [4-(4-bromo-2-cyano-phenylcarbamoyl)-benzyl]-phosphonic acid diethyl ester, CAS 133208-93-2) is a lipoprotein lipase (LPL)-promoting agent that decreases plasma triglycerides, increases high-density lipoprotein cholesterol levels, and prevents fat accumulation in high fat-fed rats. However, the effect of NO-1886 on body weight, fat accumulation, and energy expenditure in ovariectomized (OVX) rats is not clear. The primary aim of this study was to ascertain whether NO-1886 ameliorated obesity in OVX rats and to examine the effects on fatty acid oxidation-related enzymes.

Simultaneous analysis of human plasma catecholamines by high-performance liquid chromatography with a reversed-phase triacontylsilyl silica column.

The clinical importance of simultaneous analysis of 3,4-dihydroxyphenylglycol with other human plasma catecholamines has been investigated to better understand the sympathetic nervous system. However, previous reports have had analytical difficulties with both resolution and extraction. The current study uses a reversed-phase triacontylsilyl silica (C30) column under the mobile phase condition without ion-pair reagents to separate catecholamines and their metabolites, with above 91% recoveries for intra-assay, above 85% for inter-assay, and less than 10% (n=5) coefficient of variation.

Effects of acute and short-term administration of tryptophan plus ethanol on noradrenaline and serotonin metabolites in the locus coeruleus.

The effects of acute and short-term administration of tryptophan or tryptophan plus ethanol on serotonin [5-hydroxytryptamine (5-HT)] and two of its metabolites, 5-hydroxyindoleacetic acid (5-HIAA) and 5-hydroxytryptophol (5-HTPL), in the locus coeruleus were investigated in rats by using the microdialysis method. In addition, the acute effects of these drugs on noradrenaline and its metabolite 4-hydroxy-3-methoxymandelic acid (HMMA) were addressed. A single co-administration of tryptophan (50 mg/kg, i.

[Establishment of pharmaceutical management for patient care during lung cancer chemotherapy and its quantitative evaluation].

Pharmacists should play an important role in controlling the pharmaceutical management of the patients. Although the quantitative evaluations of pharmaceutical management are required systematically, no guideline is presented for patient care during lung cancer chemotherapy. We established a complete pharmaceutical management system and evaluated the performance of the system.

[Pharmacological properties of Gyokuheifusan, a traditional Kampo medicinal formula].

Gyokuheifusan (GHS, Jade Windscreen Powder in English, Yupingfengsan in Chinese) is an herbal formula in traditional Kampo medicine which consolidates superficial resistance to protect against invasion by external pathogens. This review describes the immunopharmacologic properties of GHS as a holistic Kampo medicine, which can affect human homeostasis and constitution of human beings. Oral treatment with GHS has preventive and curative effects in allergic rhinitis induced by Japanese cedar pollen in guinea pigs.

Effect of aminated gelatin on the nasal absorption of insulin in rats.

Absorption enhancers, which increase the permeability of drugs through epithelial membranes without damaging them, are especially useful for intranasal administration of peptide drugs. In this study, aminated gelatins, candidate enhancers, having different numbers of amino groups were prepared from gelatin (H-gelatin, isoelectric point = 9.0, MW 100 kDa) and a partial gelatin hydrolysate (L-gelatin, isoelectric point = 8.

Salicylic acid-induced inactivation of creatine kinase in the presence of lactoperoxidase and H2O2.

To clarify one mechanism of aspirin-induced gastric mucosal damage, inactivation of creatine kinase (CK) by salicylic acid that is easily produced from aspirin in vivo was examined in the presence of lactoperoxidase (LPO) and H2O2 (LPO-H2O2). Salicylic acid inactivated CK (rabbit muscle) during its interaction with LPO-H2O2. CK activity in gastric mucosal homogenate decreased dependent on the concentration of salicylic acid in the presence of LPO-H2O2.

[Preparing oral dosage form of ketamine in the hospital for simplicity and patient compliance--preparations using agar].

Ketamine has been widely used in the operation as intravenous and intramuscular injections, since ketamine has dissociative anesthetic properties. When it is given in sub-anesthetic dose, ketamine is known to have an analgesic effect. The analgesic effect is observed for patients with neuropathic pain when administrated not only by injection but also orally.

[Relationship between dose of mycophenolate mofetil and the occurrence of cytomegalovirus infection and diarrhea in renal transplant recipients].

To establish guidelines for avoiding the side effects of mycophenolate mofetil (MMF) in renal transplant recipients with tacrolimus (TAC)-based immunosuppression, the relationship between the daily dose of MMF and the occurrence of side effects was analyzed in this study. The frequency of side effects was investigated retrospectively in 28 renal transplant recipients treated with immunosuppression (men 14 : women 14, age: 33.0+/-12.

Pharmacokinetic interactions between Japanese traditional Kampo medicine and modern medicine (IV). Effect of Kamisyoyosan and Tokisyakuyakusan on the pharmacokinetics of etizolam in rats.

Kamisyoyosan (KSS) and Tokisyakuyakusan (TSS) are widely used herbal formulas in Japanese traditional kampo medicine to relieve the symptoms occurred in climacteric disturbance. Since Japanese physicians frequently prescribe these formulas combined with etizolam, one of benzodiazepine anxiolytics, we evaluated the pharmacokinetic interaction between KSS or TSS and etizolam, and in vitro inhibitory effect of KSS and TSS on rat cytochrome P450 (CYP) 3A activity in rat microsomes, to obtain drug information to prevent from disadvantage or adverse effects by their combined therapy. In in vitro experiment, KSS and TSS inhibited CYP3A activity comparable to grapefruit juice.

Pharmacological properties of traditional medicine (XXX): effects of Gyokuheifusan ([Symbol: see text]) on murine antigen-specific antibody production.

In the theory of traditional Chinese medicine (TCM), eqi ([Symbol: see text]) circulates at the superficial portion of the body to guard against exopathogen. Gyokuheifusan (GHS; [Symbol: see text]), containing Astragalus Root, Atractylodes Rhizome, and Saposhnikovia Root, is a TCM formula to treat the insufficiency of eqi by invigorating qi and consolidating the superficial resistance. In this study, we evaluated the effect of GHS on murine antibody production against ovalbumin (OVA) used as exopathogen.

Thiol oxidation induced by oxidative action of adriamycin.

To clarify the mechanism of the cardiotoxic action of adriamycin (ADM), the participation of free radicals from ADM in cardiotoxicity was investigated through the protective action of glutathione (GSH) or by using electron spin resonance (ESR). Oxidation of ADM by horseradish peroxidase and H2O2 (HRP-H2O2) was blocked by GSH concentration dependently. Inactivation of creatine kinase (CK) induced during interaction of ADM with HRP-H2O2 was also protected by GSH.

Distribution characteristics of grepafloxacin, a fluoroquinolone antibiotic, in lung epithelial lining fluid and alveolar macrophage.

The purpose of this study was to investigate the distribution of Grepafloxacin (GPFX), a new quinolone antimicrobial agent, in the lung epithelial lining fluid (ELF) and the alveolar macrophage (AM) in rats, which are potential infection sites in respiratory tract infections. We also aimed to clarify the mechanism governing the transferability of GPFX into the alveolus compartment from a kinetic point of view. The AUC ratios of ELF/plasma and AM/plasma after the oral administration of GPFX were 5.

Acute effect of milnacipran on the relationship between the locus coeruleus noradrenergic and dorsal raphe serotonergic neuronal transmitters.

The present studies sought to investigate the effect of milnacipran called the serotonin (5-HT) and noradrenaline (NA) reuptake inhibitor (SNRI) on the interaction of central locus coeruleus noradrenergic and dorsal raphe nucleus serotonergic functional activity by utilizing in vivo microdialysis. A single administration of milnacipran (60 mg/kg, s.c.

Determination of diffusion coefficients of peptides and prediction of permeability through a porous membrane.

The diffusion coefficient (D) of peptide and protein drugs needs to be determined to examine the permeability through biological barriers and to optimize delivery systems. In this study, the D values of fluorescein isothiocyanate (FITC)-labelled dextrans (FDs) and peptides were determined and the permeability through a porous membrane was discussed. The observed D values of FDs and peptides, except in the case of insulin, were similar to those calculated based on a relationship previously reported between the molecular weight and D of lower-molecular-weight compounds, although the molecular weight range was completely different.

Excised porcine skin experimental systems to validate quantitative microdialysis methods for determination of drugs in skin after topical application.

Microdialysis is useful as a method to evaluate the disposition of drugs in the skin to design improved transdermal delivery systems (TDDSs). In this study, quantitative microdialysis methods were validated in excised porcine skin experimental systems in vitro. Flurbiprofen (FP), used as a model drug, showed high affinity for the skin tissues in equilibrium states between the medium and skin.

Pharmacological properties of traditional medicine (XXIX): effect of Hange-shashin-to and the combinations of its herbal constituents on rat experimental colitis.

Hange-shashin-to (HST) has been used as an herbal formula to treat inflammatory ulcerative gut diseases complicated with psychoneurosis in Japanese traditional Kampo medicine. The aim of the present study is to clarify anti-colitic effect of HST using a model of colitis induced by intracolonic instillation of 2,4,6-trinitrobenzene sulfonic acid (TNBS) in rats, and to evaluate the pharmaceutical properties of its herbal components. The colonic damage was elucidated by macroscopic damage scores, colon wet weight and area of mucosal necrosis.

Effect of camellia oil on the permeation of flurbiprofen and diclofenac sodium through rat and pig skin.

The effect of camellia oil on the permeation of flurbiprofen (FP) and diclofenac sodium (DFS), used as model drugs, through rat and pig skin was examined. Two different types of camellia oil were used: one of them was purified by distillation and the other was purified by filtration without heating. The distilled camellia oil (DCO) and the filtered camellia oil (FCO) were applied to the skin as a pretreatment.

Anti-stress effects of 3,4,5-trimethoxycinnamic acid, an active constituent of roots of Polygala tenuifolia (Onji).

3,4,5-trimethoxycinnamic acid (TMCA) is one of the constituents in Onji (roots of Polygala tenuifolia WILLD), an herbal medicine used for sedative in Japanese traditional Kampo medicine. Our previous study revealed that oral administration of this compound prolongs sleeping time induced by hexobarbital in mice to exhibit sedative action. In the present study, we investigate the effects of TMCA on the stress induced with repeated cold exposure or intracerebroventricular injection of corticotrophin-releasing hormone (CRH).

Pharmacokinetic interactions between Japanese traditional medicine (kampo) and modern medicine (III). Effect of Sho-seiryu-to on the pharmacokinetics of azelastine hydrochloride in rats.

Sho-seiryu-to (SST) is widely used herbal formula in Japanese traditional medicine (kampo) to treat allergic diseases. Since Japanese physicians frequently prescribe this formula combined with azelastine hydrochloride, one of anti-histamine and anti-allergic medicines, we evaluated the pharmacokinetic interactions between SST and azelastine hydrochloride in rats to obtain the drug information for the prevention from disadvantage or adverse effects by their combined therapy. Oral administration of SST did not influence the plasma concentration profile of azelastine after its intravaneous injection, suggesting that SST would not change the activities of metabolic enzymes such as cytochrome P450s.

Inactivation of alcohol dehydrogenase by piroxicam-derived radicals.

Alcohol dehydrogenase (ADH) was used as a marker molecule to clarify the mechanism of gastric mucosal damage as a side effect of using piroxicam. Piroxicam inactivated ADH during interaction of ADH with horseradish peroxidase and H2O2 (HRP-H2O2). The ADH was more easily inactivated under aerobic than anaerobic conditions, indicating participation by oxygen.

A rabbit ear flap perfusion experiment to evaluate the percutaneous absorption of drugs.

A rabbit ear flap single-pass perfusion system was examined as an experimental method for studying the relationship between the physiological conditions of tissues and drug disposition after topical applications. Tyrode solutions containing bovine serum albumin (BSA) and sucrose or flurbiprofen (FP), used as a model drug, were perfused through the vessel in the ear flap to evaluate the physiological conditions prior to the application of FP to the skin surface. The extracellular volume and distribution properties of FP in the perfused ear were similar to those in an in vivo experimental system.