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We have demonstrated an ultrafast high-contrast surface-reflection all-optical switch using a spin-polarization scheme. The device is made with low-temperature-grown Be-doped strained InGaAs/InAlAs multiple quantum wells. It has a photoresponse of 300 fs due to ultrafast electron trapping. The on/off ratios have been drastically improved by more than 20 dB, and reached over 30 and 40 dB at pump pulse energies of 4 and 14 pJ, respectively. Furthermore, we have obtained polarization insensitive operation by handling the two orthogonal components of the signal pulse at two different points.

Chromatic dispersion properties of the Ti:LiNbO(3) optical waveguide have been investigated. Dispersion values of the waveguide fabricated in Z-cut LiNbO(3) were sigma(TE) = -2.0 fsec cm(-1) nm(-l) at a wavelength of 1.3 microm and sigma(TE) = -1.3 fsec cm(-1) nm(-1) at a wavelength of 1.5 microm. Measurement results were compared with theoretical values that take into account the bulk dispersion data and the waveguide dispersion characteristics.

The electrocatalytic hydrogenation of the title compound was examined over Raney Ni, Raney Co, Pt-carbon and Pd-carbon as hydrogen-active powder electrodes. A high conversion of ketone to alcohol was observed on the Raney catalysts when the pKa values of the proton sources employed were around 5. The metal-on-carbon catalysts showed a relatively low conversion of ketone regardless of the proton sources. The stereochemistry of the reaction was examined.

On irradiation with (E)-anethole in benzene 10-hydroxymethyl-9-phenanthrenecarboxylic lactone (STL) gave an intermolecular [2+2] cycloadduct, a cyclobutane derivative, while 8-hydroxymethyl-9-phenanthrenecarboxylic lactone (SCL) afforded both of a cyclobutane with the same conformation and an olefinic product derived from an oxetane precursor, the carbonyl adduct. The formation of cycloadducts of highly different structures in SCL was ascribed to competitive collapse of the involved exciplex to the products.

The solubilization of d-α-tocopherol (VE) in micellar solutions of various bile salts, mean aggregation numbers of the micelles, and absorption of VE from each micellar solution in rat small intestine were studied. The micellar solutions were prepared by sodium glycocholate (NaGC), sodium glycodeoxycholate (NaGDC), sodium glycochenodeoxycholate (NaGCDC), sodium taurocholate (NaTC), sodium taurodeoxycholate (NaTDC) and a mixed system containing five bile salts.The amount of solubilized VE generally increased with the concentrations of bile salts in each micellar solution above the critical micellar concentration (cmc). Micelles of dihydroxy bile salts solubilized more VE than trihydroxy ones. Mean aggregation numbers of bile salt micelles ranged from 14 to 18, and were virtually independent of saturated amounts of solubilized VE. The intestinal absorption of VE appeared to be affected by the surface of the intestinal microvillous membrane and bile salt concentration.

Irradiation of (E)-3-(p-methoxyphenyl)-3-pentenyl, (E)-4-(p-methoxyphenyl)-4-hexenyl, and (E)-5-(p-methoxyphenyl)-5-heptenyl 9-phenanthrenecarboxylates (B-2E, B-3E, and B-4E, respectively) in benzene gave intramolecular [2+2] cycloadducts, cyclobutane derivatives (CB-2, CB-3, and CB-4, respectively) possessing the same conformation as an intermolecular [2+2] cycloadduct (CB-0) between methyl 9-phenanthrenecarboxylate (9-MCP) and trans-anethole (t-AN), and oxetane derivatives (OX-2, OX-3, and OX-4, respectively) arising from intramolecular cycloaddition between the carbonyl group and the olefinic double bond. However, (E)-4-(p-methoxyphenyl)-3-butenyl and (E)-5-(p-methoxyphenyl)-4-pentenyl 9-phenanthrenecarboxylates (A-2E and A-3E, respectively) afforded only products derived from oxetane precursors.

The efficiency of [2+2] photocycloadduct formation was examined by measuring fluorescence lifetimes and the quantum yields of fluorescence and product formation in two series of p-methoxyphenylalkenyl 9-phenanthrenecarboxylates (A-nE and B-nE). In (E)-3-(p-methoxyphenyl)-3-pentenyl, (E)-4-(p-methoxyphenyl)-4-hexenyl, and (E)-5-(p-methoxyphenyl)-5-heptenyl 9-phenanthrenecarboxylates (B-2E, B-3E, and B-4E, respectively) the intramolecular quenching leads to product (cyclobutane+oxetane) formation in almost unit efficiency, while in (E)-4-(p-methoxyphenyl)-3-butenyl and (E)-5-(p-methoxyphenyl)-4-pentenyl 9-phenanthrenecarboxylates (A-2E and A-3E, respectively) exciplex→product efficiency is a half to three quarters. Intermediacy of plural exciplex intermediates is suggested in the present bichromophoric systems on the basis of exciplex quenching results.

Aims It has been reported that cytochrome P450 (CYP)3A activity increases significantly in patients with end stage renal disease (ESRD) after kidney transplantation, with wide interindividual variability in the degree of increase. The aim of this study was to evaluate the influence of CYP3A5 polymorphism on the increase in CYP3A activity after living kidney transplantation, by measuring the plasma concentration of 4β-hydroxycholesterol. Methods This prospective study recruited 22 patients with ESRD who underwent a first living kidney allograft transplantation, comprising 12 patients with CYP3A5*1 allele (CYP3A5*1/*1 or *1/*3) and 10 patients without CYP3A5*1 allele (CYP3A5*3/*3). Results No significant difference in estimated glomerular filtration rate over time was observed between patients with the CYP3A5*1 allele and patients without the CYP3A5*1 allele, suggesting that the degrees of recovery in renal function after living kidney transplantation were similar in the two groups. However, plasma concentrations of 4β-hydroxycholesterol on days 90 (57.1 ± 13.4 vs. 39.5 ± 10.8 ng ml−1) and 180 (55.0 ± 14.5 vs. 42.4 ± 12.6 ng ml−1) after living kidney transplantation were significantly higher in the presence of the CYP3A5*1 allele than in the absence of the CYP3A5*1 allele [P = 0.0034 (95% confidence interval of difference 6.55, 28.6) and P = 0.043 (95% confidence interval of difference 0.47, 24.8), respectively], suggesting that CYP3A activity may increase markedly associated with recovery of renal function in patients with the CYP3A5*1 allele. Conclusions These findings suggest that the presence of the CYP3A5*1 allele contributes to marked elevation of CYP3A activity associated with recovery of renal function after kidney transplantation.

Photopolymer compositions for a high density black matrix, which was applied to a flat-bed display, have been investigated.To obtain the higli density matrix, new epoxyacrylate monomers, which worked as a dispersing reagent of carbon black (CB) and as a polymerizing reagent, and high speed photo-initiator systems containing a new singlet-sensitizer dye were developed.The relation of the image formation and the pigment dispersing character with the chemical structure of the monomers, and photo-initiating mechanisms, which wen analyzed by a laser flash photolysis in a polymer film, are discussed.

Pharmaceutical development starts with the discovery of a new compound. Drugs become commercially available after non-clinical and clinical studies, but processes that take place after marketing are also important for pharmaceutical development. In recent years, use of the phrase "Ikuyaku" meaning postmarketing development has become more common. Sometimes, the proper usage, indications and harmful effects of a drug are discovered only after it becomes commercially available and is administered to many patients. Hence, pharmacists need to actively perform postmarketing studies to reveal the true nature of drugs. In the present clinicopharmacological study, we investigated the effects of histamine H(2) receptor antagonists (H(2)-RAs) on the plasma concentrations of gastrointestinal peptides from the viewpoint of postmarketing development. First we established an enzyme immunoassay for secretin, which is involved in gastrointestinal motility. Then we used this and existing peptide assays to investigate the above-mentioned issues. Ranitidine and nizatidine increased the plasma concentration of motilin. It is believed that the plasma concentration of Ach is elevated by ranitidine and nizatidine, which possesses an anti-AchE activity, and that the increased the plasma concentration of Ach facilitated release of motilin, elevating the plasma concentration of motilin. When compared to the placebo, lafutidine significantly increased the plasma concentration of CGRP (calcitonin gene-related peptide) and substance P. Furthermore, released CGRP stimulated CGRP1 receptors to facilitate secretion of somatostatin. Therefore, lafutidine appears to protect the gastric mucosa and regulate gastrointestinal motility. The same results were obtained with ranitidine and nizatidine. While H(2)-RAs have a common function in suppressing the secretion of gastric acid, they do not exhibit the same effects on factors related to recurrence of peptic ulcer, such as gastrointestinal motility and blood flow in the gastrointestinal mucosa. Hence, measuring the plasma concentration of gastrointestinal peptides can be used to estimate the effects of drugs on gastrointestinal motility. From the viewpoint of postmarketing development, we are in the process of establishing indicators for the proper usage of pharmaceutical drugs. Pharmacists need to closely follow and monitor adverse reactions. In order to further improve monitoring of drug therapy, it will be necessary to assess not only the blood concentrations of drugs, but also biological reactions to the drugs. Since the levels of peptides reflect the clinical efficacy of gastrointestinal drugs, measuring peptide levels appears to be useful for selecting appropriate drugs.

The hypothalamo-pituitary-adrenal (HPA) axis is known to relate with energy homeostasis. Appetite and food intake are assumed to be regulated by the HPA axis. Among lots of medicines that act gastrointestinal system, we focused proton pump inhibitors, which are widely used to treat peptic ulcer, gastro esophageal reflux disease and eradication of Helicobacter pylori. In this study, we investigated that the effect of three proton pump inhibitors (omeprazole, lansoprazole and rabeprazole) on plasma adrenocorticotropic hormone (ACTH) and cortisol levels in healthy human subjects. Five healthy male volunteers were treated to omeprazole, lansoprazole, rabeprazole or placebo. Venous blood samples were taken repetitively from a forearm vein before and after administration. Plasma ACTH-like immunoreactive substance (IS) levels were measured using a sensitive enzyme immunoassay, and plasma cortisol levels were measured using a fluorescence polarization immunoassay. Single administration of lansoprazole caused significant (P

Itopride hydrochloride (itopride), a gastrokinetic drug, has recently been evaluated for its clinical usefulness in functional dyspepsia. We investigated effects of itopride on human plasma gastrin-, somatostatin-, motilin-, and cholecystokinin (CCK)-like immunoreactive substances (IS); adrenocorticotropic hormone (ACTH)-immunoreactive substances (IS), and cortisol under stress conditions in healthy subjects. A single administration of itopride caused significant increases in plasma somatostatin- and motilin-IS levels compared to placebo. Itopride significantly decreased plasma CCK-IS, and suppressed the ACTH-IS level compared to placebo. We hypothesize that itopride may have an accelerating gastric emptying effect, and a modulatory effect on the hypothalamo-pituitary-adrenal axis and autonomic nervous functions. These effects might be beneficial in stress-related diseases, suggesting that itopride has clinicopharmacological activities.

Some traditional Chinese herbal (Kampo) medicines have recently been evaluated for their clinical usefulness in stress and depression. These medicines have modulatory effects on the hypothalamic-pituitary-adrenal axis and sympathetic nervous system (SNS). We examined the effects of Rikkunshi-to, Hange-shashin-to, Hange-koboku-to, and Ninjin-to on plasma levels of neuropeptide Y (NPY), which is the representative neurotransmitter of the SNS, under venipuncture stress. Rikkunshi-to and Hange-shashin-to suppressed increases in plasma NPY-immunoreactive substance levels compared with the response to a placebo. In this study, Rikkunshi-to and Hange-shashin-to altered plasma levels of NPY under venipuncture stress. These effects might be beneficial in stress-related diseases and our results suggest that these medicines have clinical pharmacologic activity.

Domperidone, an upper gastrointestinal function regulatory medicine, has recently been evaluated for its clinical usefulness in the treatment of stress and depression. We examined the effects of domperidone on the plasma levels of motilin-immunoreactive substance (IS), somatostatin-IS, gastrin-IS, adrenocorticotropic hormone (ACTH)-IS, and cortisol under stress conditions by repetitive blood sampling. After a single oral administration of domperidone (30 mg), the plasma domperidone level was highest (58.6+/-6.4 ng/ml) in the sample taken 40 min after administration, after which the plasma level fell. Peak plasma motilin-IS levels (23.1+/-1.4 pg/ml) were achieved 40 min after administration of domperidone (p < 0.01 vs. placebo), and returned to baseline levels within a further 40 min. Plasma somatostatin-IS levels (13.0+/-1.2 pg/ml) increased 60 min after administration of domperidone (p < 0.01 vs. placebo). Plasma gastrin-IS levels did not change significantly. These results suggest that the pharmacological effects of domperidone on gastrointestinal functions are closely related to changes in motilin-IS and somatostatin-IS levels. Domperidone significantly suppressed increases in plasma ACTH-IS and cortisol levels compared with the response to a placebo. These modulatory effects might be beneficial in stress-related diseases and suggest that this medicine has clinical pharmacological activity.

Ecabet sodium (ecabet), a cytoprotective drug, produces an increase in mucosal blood flow. One of the gastrointestinal motility regulatory factors has been assumed to be the induction of changes in the levels of peptides (gastrin, somatostatin and motilin) in plasma. On the other hand, recently, capsaicin-sensitive afferent nerves were shown to play an important role in gastric mucosal defensive mechanism. Capsaicin stimulates afferent nerves and enhances the release of calcitonin gene-related peptide (CGRP) and substance P in the stomach. We studied the effect of ecabet on human plasma gastrin-, somatostatin-, motilin-, CGRP- and substance P-like immunoreactive substance (IS) in healthy subjects. Ecabet sodium at a dose of 3.0 g, or placebo, was orally administered in five healthy males. The blood samples were taken before and at 20, 40, 60, 90, 120, 180 and 240 min after administration, subjected to extracting procedures, and submitted to a highly sensitive enzyme immunoassay system. Single administration of ecabet caused significant (P < 0.05) increases in plasma CGRP-, substance P- and somatostatin-IS concentration compared with placebo. Ecabet significantly decreased plasma gastrin-IS levels compared with placebo. In this study, we hypothesized that ecabet might stimulate capsaicin-sensitive afferent nerves indirectly and improve mucosal blood flow; this might be a key mechanism underlying its gastroprotective action.

Omeprazole, a proton pump inhibitor (PPI), is widely used in treatment of peptic ulcer, gastro esophageal reflux disease and eradication of Helicobacter pylori. PPIs inhibit final gastric acid secretion stage by blocking H+/K+-ATPase. But the mechanism except for gastric antisecretory effect has not understood clearly. So, we examined the effects of omeprazole on the levels of gastrointestinal peptides (somatostatin, motilin, gastrin, vasoactive intestinal peptide (VIP), substance P (SP) and calcitonin gene-related peptide (CGRP)) in plasma from healthy subjects. After a single oral administration of omeprazole, the plasma omeprazole concentration was highest at 120 min. Omeprazole caused a significant increase of plasma somatostatin-immunoreactive substance (IS) levels at 60-240 min and plasma motilin-IS levels at 120-180 min, compared with a placebo group, respectively. The physiological release of plasma gastrin-IS was reduced by the administration of omeprazole at 60 min, but the medicine did not alter the levels of VIP-, CGRP- and SP-IS. These results suggested that the pharmacological effects of omeprazole on regulation of gastrointestinal function are closely related to changes of somatostatin-, motilin- and gastrin-IS levels in human plasma.

The herbal medicine Ninjin-to has been used for the treatment of gastroenteritis, esogastritis, gastric atony, gastrectasis, vomiting, and anorexia. One of the mechanisms of the empirical effects is assumed to be due to local changes in neuropeptide levels. Sensory afferent neurons in the gastrointestinal mucosa regulate neuropeptides [calcitonin gene-related peptide (CGRP), substance P, etc.], which play various physiologic roles. To determine whether the pharmacologic effects of Ninjin-to on the gastrointestine are due to changes in gastrointestinal mucosa regulatory peptide levels, we examined the effects of Ninjin-to on the levels of CGRP-like immunoreactive substances (IS) and substance P-IS in plasma taken from five healthy subjects. A single oral administration of 6.0 g of Ninjin-to caused significant increases in plasma CGRP-IS at 40 min and 60 min, and in substance P-IS levels at 90 min, compared with a placebo group. These results may indicate that the pharmacologic actions of Ninjin-to are closely related to changes in CGRP-IS and substance P-IS levels.

Sho-hange-ka-bukuryo-to and Nichin-to, traditional Chinese herbal (Kampo) medicines have been used to treat vomiting and nausea. Traditional herbal medicines have frequently been used in the empirical treatment. Some patients who take these medicines have no organic disease but have conditions classified as non-ulcer dyspepsia (NUD). To determine the pharmacological effects of Sho-hange-ka-bukuryo-to, Nichin-to, and the two herbs (Pinelliae Tuber and Zingiberis Rhizoma, both of which are included in Sho-hange-ka-bukuryo-to and Nichin-to), we examined the effects of these medicines on the plasma levels of adrencorticotropic hormone (ACTH) and cortisol under stress conditions by repetitive blood sampling. After a single administration of Kampo medicine or a placebo, venous blood samples were taken before and 20-240 min after administration. A single administration of Sho-hange-ka-bukuryo-to caused significant suppression of an increase in plasma ACTH-immunoreactive substance (IS) levels at 120 to 180 min and tended to suppress increases in plasma cortisol levels at 240 min, compared with the response to a placebo. A single administration of Nichin-to caused significant suppression of increases in plasma ACTH-IS levels at 120 min compared with a placebo group, but had no effect on plasma cortisol levels. Pinelliae Tuber had no significant effects in plasma ACTH-IS or cortisol, but Zingiberis Rhizoma significantly suppressed the increase of ACTH-IS (120 min) and cortisol (180 min). These medicines have a modulatory effect on the hypothalamo-pituitary-adrenal (HPA) axis and autonomic nervous function. These effects might be beneficial in stress-related disease and suggest that this medicine has clinical pharmacological activity.

Hange-koboku-to (Banxia-houpo-tang), a Chinese herbal (Kampo) medicine, has been used for improvement of hoarse voice, something foreign body sensation in the throat and/or esophagus, and swallowing reflex, among other conditions. One of the mechanisms of the empirical effects is assumed to be due to local changes in neuropeptide levels locally. We investigated the effects of Hange-koboku-to on neuropeptides, calcitonin gene-related peptide (CGRP), substance P, somatostatin, and vasoactive intestinal peptide (VIP) in plasma and saliva, as well as on salivary secretion in healthy subjects. A single oral administration of Hange-koboku-to caused significant increases in substance P-immunoreactive substance (IS) (40 min) in plasma, and slightly increased in CGRP-IS and somatostatin-IS in plasma compared with placebo. In saliva neuropeptides, Hange-koboku-to caused significant increases in substance P-IS (20 min) and somatostatin-IS (40, 60 min), and a slight increase in VIP-IS. However, a single Hange-koboku-to stimulation did not have a significant effect of sialosis volume. These results seem to suggest that Hange-koboku-to improves hoarse voice, something foreign body sensation in the throat and esophagus, and swallowing reflex disorder, by stimulation of neuropeptidergic nerves locally.

Synchronous switching controller (SSC) applied to gas circuit breakers (GCB) has been developed. The SSC is able to open and close the contacts of the GCB at the pre-determined point on wave for minimizing the switching surges. This paper proposes the new controlled switching algorithm to minimize the total delay time and the control error. A new algorithm for detecting voltage and current zero crossing points and predicting the next operating time of the GCB is introduced. For a 145 kV GCB with the SSC installed the proposed algorithm has been verified by various tests. The SSC performed successful operations and the standard deviation from the target point is within 0.5 msec at ambient temperatures from -30 to 60 degrees C for different control voltages. The making tests at voltage zero also works well in a capacitive load circuit at 145 kV and 362 kV ratings.

Rikkunshi-to, a gastrointestinal function regulatory traditional Chinese herbal (Kampo) medicine, has recently been evaluated for its clinical usefulness in stress and depression. This medicine has modulatory effects on the hypothalamo-pituitary-adrenal axis and autonomic nervous function. We examined the effect of Rikkunshi-to and the other gastrointestinal function regulatory Kampo medicines, Hange-shashin-to, Hange-koboku-to, and Ninjin-to, on the plasma levels of adrenocorticotropic hormone (ACTH) and cortisol under stress conditions by repetitive blood sampling. Rikkunshi-to, Hange-shashin-to, and Hange-koboku-to significantly suppressed increases in plasma ACTH-immunoreactive substance (IS) levels compared with the response to a placebo. Rikkunshi-to and Hange-shashin-to significantly suppressed increases in plasma cortisol levels compared with the response to placebo. Ninjin-to had no significant effect on plasma ACTH-IS and cortisol levels. In this study, Rikkunshi-to, Hange-shashin-to, and Hange-koboku-to (partially) regulated plasma ACTH and cortisol levels under stress. These modulatory effects might be beneficial in stress-related disease and suggest that these medicines have clinical pharmacologic activity.

The effects of the histamine H2-receptor antagonists (H2-antagonists), ranitidine, nizatidine, cimetidine and famotidine, on plasma levels of gastrointestinal peptides, calcitonin gene-related peptide (CGRP), substance P (SP), and vasoactive intestinal peptide (VIP) was investigated with respect to regulation of gastric mucosal blood flow, in healthy volunteers. H2-Antagonists or placebo was orally administered to five healthy male volunteers. Venous blood samples were taken before and after drug administration. The levels of plasma gastrointestinal peptides were determined by enzyme immunoassay. The administration of ranitidine and nizatidine caused significant increases in plasma CGRP and SP levels at 30 to 120 min compared with the placebo group. Peak plasma CGRP levels (39.8 ± 3.1 and 40.6 ± 3.6 pg mL−1) were achieved 60 min after administration of ranitidine and nizatidine, respectively. Maximum plasma SP levels (21.3 ± 5.2 and 22.8 ± 4.2 pg mL−1) were reached 60 min after administration of ranitidine and nizatidine, respectively. However, all H2-antagonists did not alter the levels of VIP. The released CGRP and SP by ranitidine and nizatidine administration may produce a gastroprotective effect, increase mucosal blood flow, and inhibit acid secretion in the gastrointestinal tract.

Hange-shashin-to has been used for chronic hypofunction of the gastrointestinal tract and to improve functional abnormalities of the upper and lower gastrointestinal system. To determine whether the pharmacological effects of Hange-shashin-to are due to gut-regulatory peptide levels, we developed a sensitive and specific double-antibody enzyme immunoassay (EIA) for detecting motilin and also examined the levels of somatostatin-, motilin-, gastrin-, and vasoactive intestinal peptide (VIP)-immunoreactive substances (IS) in plasma from healthy subjects. We developed a sensitive (3.5 pg, 1.4 pg/well) and specific (carboxy-terminal region) EIA for motilin. A single oral administration of Hange-shashin-to 6.0 g caused significant increases somatostatin-IS (20-60 min), motilin-IS (40 min), and gastrin-IS (40-90 min) levels in plasma compared with levels in a placebo group. Hange-shashin-to had no significant effect on VIP-IS levels after single administration. These changes in hormone levels (somatostatin, motilin, and gastrin) might relate to normalization of the upper and lower gastrointestinal system by Hange-shashin-to.

Purpose: Platinum-based chemotherapy is widely recognized to cause severe gastrointestinal disorders. The aim of this study was to assess the plasma gastrointesitinal peptide levels and their association with appetite during chemotherapy in patients with esophageal cancer. Methods: Five patients with esophageal cancer who underwent platinum-based chemotherapy were enrolled in this study. Plasma gastrointestinal peptides (Acylated ghrelin, Desacyl-ghrelin, leptin, motilin, and substance P) levels and platinum concentrations were measured before and at day 3, 8, and 28 after chemotherapy. Appetite profile was evaluated by visual analog scale (VAS). Results: Plasma acylated ghrelin and substance P were significantly decreased at day 8 of chemotherapy but recovered at day 28. No changes were noted in plasma desacyl-ghrelin, leptin, and motilin. VAS score of appetite was significantly decreased at day 8. There was significantly correlation between plasma acylated ghrelin/total ghrelin levels ratio (A/T ratio) and VAS score, and between plasma substance P levels and VAS score. Conclusion: Platinum-based chemotherapy significantly reduced plasma ghrelin and feeding activity. The A/T ratio and substance P levels in plasma might be good indicators of the expression of the gastrointestinal disorders by platinum-based chemotherapy in esophageal cancer patients.

The effect of mosapride citrate (mosapride) on plasma levels of gastrointestinal peptides (motilin, gastrin, somatostatin, and secretin) was studied in five healthy volunteers. After a single oral administration of mosapride (15 mg), the plasma mosapride level (85.0+/-13.7 ng/ml) was highest in the 60-min sample after the administration and then the plasma level fell. Peak plasma motilin levels (18.6+/-1.7 pg/ml) were achieved 60 min after administration of mosapride (p0.01 vs. placebo), and returned to baseline levels within a further 120 min. Plasma gastrin levels (42.4+/-3.6 pg/ml) increased 60 min after administration of mosapride (p0.01 vs. placebo). Plasma somatostatin and secretin levels did not change significantly. These results suggest that the pharmacological effects of mosapride on gastrointestinal functions are closely related to changes in motilin-immunoreactive substance levels in human plasma.

The effect of cisapride on plasma concentrations of paracetamol was investigated with respect to hepatic metabolism. Paracetamol (1 g) together with cisapride (7.5 mg) or placebo was orally administered to five healthy male volunteers. Venous blood samples were taken before and after administration. Plasma paracetamol and its glucuronide and sulfate conjugates were measured by HPLC. The pharmacokinetic variables were calculated from the plasma concentration-time curves of each volunteer. The area under the plasma paracetamol concentration-time curve from 0 to 180 min (mean ± s.d.) increased from 1875.0 ± 112.8 μg min mL−1 (placebo coadministration) to 2238.8 ± 125.8 μg min mL−1 (cisapride coadministration) (P < 0.01). The mean maximum plasma paracetamol concentration (18.2 μg mL−1) with placebo was reached 30 min after administration, whereas mean maximum plasma paracetamol concentration (21.2 μg mL−1) with cisapride occurred 45 min after administration. The plasma paracetamol concentrations with cisapride were significantly greater at 45 to 120 min after administration compared with placebo. Plasma paracetamol glucuronide conjugate concentrations with cisapride were decreased at 15 to 60 min compared with placebo (P < 0.05), whereas plasma paracetamol sulfate conjugate concentrations did not change significantly. Hence the coadministration of paracetamol with cisapride reduced plasma paracetamol glucuronide concentrations and increased plasma paracetamol concentrations, presumably due to inhibition of paracetamol metabolism via paracetamol glucuronyltransferase. Thus, care is necessary when paracetamol and cisapride are coadministered.

We examined the effects of Dai-kenchu-to (DKCT) on the levels of vasoactive intestinal peptide (VIP) and 5-hydroxytryptamine (serotonin; 5-HT) in plasma taken from 6 healthy subjects. A single oral administration of 7.5 g DKCT caused significant increases in plasma VIP at 30, 60 to 90 and 120 min (3.5-5.5 pg/ml), compared with the response in a placebo group (about 1.0 pg/ml). DKCT also caused significant increases in plasma 5-HT at 30 (121.8+/-7.3 ng/ml) and 60 (156.5+/-8.0 ng/ml) min, compared with the response in the placebo group (about 101 ng/ml). These results indicate that the stimulatory effect of DKCT on VIP-immunoreactive substance (VIP-IS) secretion is due, at least in part, to increased 5-HT levels in the abdomen. As a consequence, increased VIP-IS may improve feelings of coldness in the abdomen.

We examined the effect of Dai-kenchu-to (DKCT), a traditional Chinese (Kampo) medicine, on the levels of 3 brain-gut peptides (motilin, gastrin and somatostatin) in plasma from 24 healthy subjects. A single oral administration of DKCT, at a dose of 7.5 g, caused significant increases in plasma motilin levels (about 12 pg/ml) at 60 to 90 min, compared with a placebo-treated group. Transient elevations of gastrin levels were noted after administration of both DKCT (25.9+/-1.4 pg/ml) and placebo (23.5+/-1.3 pg/ml). DKCT did not alter the levels (about 5.7 pg/ml) of somatostatin. In conclusion, these results indicate that the action of DKCT closely relates to changes in motilin-immunoreactive substance levels in human plasma.

Purpose Chemotherapy-induced nausea and vomiting (CINV) is one of the major adverse events in patients receiving cancer chemotherapy. Preventing CINV is the key to maintaining a patient's quality of life. At Oita University Hospital, the antiemetic regimen was standardized based on the antiemetic guidelines for CINV published by the Japanese of Society Clinical Oncology (JSCO) in May 2010. In the present study, we retrospectively evaluated the clinical and economic effects of standardizing the antiemetic regimen. Methods Palonosetoron, dexamethasone aprepitant, was administered as antiemetics according to the newly standardized regime. The efficacy and costs of antiemetic treatment of chemotherapy before and after standardization of the antiemetic regimen between July 2010 and December 2010 were compared between patients receiving high-grade emetogenic chemotherapy (HEC) and those receiving moderate-grade emetogenic chemotherapy (MEC). The efficacy was evaluated by the proportion of patients without nausea ( Results A total of 50 and 38 patients were treated by the HEC and MEC regimens, respectively. In the HEC group, the proportion of patients without nausea (90.0% versus 92.0%) and complete response (89.0% versus 92.0%) were not significantly different between before and after the standardization. In the MEC group, the proportion of patients without nausea after the standardization was significantly higher than that before the standardization (94.7% and 76.7%, respectively, P Conclusion Using the standardized antiemetic treatment may help reduce the nausea or vomiting suffered by patients receiving cancer chemotherapy and will be less of a financial burden to these patients.

9-Anthroyloxyl radicals are generated from photocleavage of the N-O bond of N-(9-anthroyloxy)-9-fluorenylideneamine and 1-(9-anthroyloxy)-2-pyridone in acetonitrile. They are much less reactive in decarboxylation, addition to olefins, and hydrogen-atom abstraction than benzoyloxyl and 1-naphthoyloxyl radicals, and supposedly undergo intramolecular addition to the ipso position to give α-lactonic spiroanthracenyl radicals.

To investigate the effect of intramolecular hydrogen bonding on the photoisomerization of carbon–carbon double bond, photoisomerization of 2′-hydroxychalcone has been studied. Based on the quantum yield measurements and laser flash photolysis studies, it was found that 2′-hydroxychalcone isomerized only from cis- to trans-isomer. The one-way cis-trans isomerization is induced by the adiabatic hydrogen atom tranfer in the triplet state.

The transient absorption spectrum of o-iodobenzoyloxyl radicals was observed for the first time in acetonitrile using 1-(o-iodobenzoyloxy)-2-pyridone as a precursor. On the basis of the comparison of the spectra of o-halobenzoyloxyl radicals, it is proposed that the o-iodobenzoyloxyl radicals take a planar structure with a strong interaction between the radical center oxygen atom and the neighboring iodine atom.

A study has been made on the polarization dependence of absorption and luminescence spectra of a 1,5-dihydroxyanthraquinone single crystal with the thickness of 0.5 mm, which was prepared by gas ph...

Background Traditional Chinese herbal (Kampo) medicines, Dai-kenchu-to (DKCT) have been frequently used in the empirical treatment of gastrointestinal obstructions. Although it has been already reported that DKCT increases in the plasma levels of gastrointestinal peptides {vasoactive intestinal polypeptides (VIP) and motilin}, which improves feelings of abdominal coldness and gastrointestinal motility, the mechanism is not yet well understood. In this study, we examined effects of DKCT on the plasma calcitonine gene-related peptide (CGRP), substance P (SP) and somatostatin (SS) levels. Methods DKCT or placebo was orally administered to five healthy male volunteers aged 25–30 years. Venous blood samples were taken before and 20, 40, 60, 90, 120, 180 and 240 min after administration of DKCT. Peptide levels in plasma were measured using a sensitive enzyme immunoassay. Results DKCT (7.5 g) significantly increased in CGRP-like immunoreactive substances (IS) at 40 min, SP-IS at 20–60 min and SS-IS at 180–240 min compared with the each response of placebo. Conclusions In this study, DKCT raised plasma CGRP-, SP- and SS-IS levels. CGRP and SP participate in the control of mucosal blood flow in the gastrointestinal tract. Also, SS participates in the regulation of gastrointestinal motility. DKCT might regulate to the mucosal blood flow by increasing in plasma CGRP- and SP-IS levels. Besides, DKCT might improve the gastrointestinal motility by increasing in plasma SS-IS levels. Clinical Pharmacology & Therapeutics (2005) 77, P13–P13; doi: 10.1016/j.clpt.2004.11.052

Background Ecabet, an antiulcer drug, has gastric protective effects that are improvement of blood flow or promotion of bicarbonate secretion. Recently, capsaicin sensitive afferent nerves play an important role in gastric mucosal defensive mechanism. Capsaicin stimulates afferent nerves and enhances the release of calcitonine gene-related peptide (CGRP) and substance P in the stomach. We studied the effect of ecabet on human plasma CGRP and substance P in healthy subjects. Methods Ecabet at a dose of 1000 mg or placebo was orally administered in five healthy male volunteers. The blood samples were taken before and till 240 min after administration, followed by the extracting procedure, and submitted to the high sensitive enzyme immunoassay system for CGRP and substance P as previously developed. Results Single administration of ecabet caused significant (P

Purpose Omeprazole, proton pump inhibitor, is widely used in treatment of peptic ulcer, Gastro esophageal reflux disease and eradication of Helicobacter pylori. But the mechanism is not well understood. So we examined the effects of omeprazole on plasma levels of gastrointestinal peptides {somatostatin, gastrin, motilin, vasoactive intestinal peptide (VIP), substance P (SP) and calcitonin gene related peptide (CGRP)}. Methods: Omeprazole or placebo was orally administered in five healthy male volunteers aged 25–30 years. Venous blood samples were taken before and at 30, 60, 90, 120, 180, 240 and 360 min after administration of the drug. Plasma peptide levels were measured using a sensitive enzyme immunoassay. Results: Omeprazole (20mg) causes significant increase in somatostatin-IS at 60-240 min compared with the response of the placebo treated group. Furthermore omeprazole showed 35.1 % (60min) increase of placebo motilin levels and 38.5 % (60min) inhibition of placebo gastrin levels. But omeprazole had no effect on plasma VIP-IS, SP-IS and CGRP-IS levels compared with the placebo treated groups. Conclusions: In this study, omeprazole enhanced somatostatin-IS levels. Somatostatin, a polypeptide, which distributes widely in the gastrointestinal tract, participates in the control of gut motility and hormones secretion. Omeprazole might have pharmacological mechanism not only inhibition of gastric acid secretion but also regulation of gastrointestinal peptide. Clinical Pharmacology & Therapeutics (2004) 75, P11–P11; doi: 10.1016/j.clpt.2003.11.042

We show that all-optical switching is feasible by means of cascading of sum-frequency-generation and difference-frequency-generation processes under phase-matched conditions. Three-terminal switching is demonstrated experimentally with bulk periodically poled LiNbO(3). The cascading under phase-matched conditions facilitates switching with lower power than that required under phase-mismatched conditions.

Binding of the oxygen atom of iron(III)–peroxide adducts to phenol rings has been found to be highly controlled by the substituents on the ring, implying that the interaction between the adduct and the ring involves an electronic attractive force, whereby the adduct acts as an electrophile.

Laser-diode-driven all-optical switching is demonstrated with an As2S3-based glass fiber only 2 m long and assistance from an erbium-doped fiber amplifier. The laser-diode operation makes it easy to control ultrafast pulse trains with low timing jitter. Ultrafast switching at as much as 80-GHz repetition rates is successfully demonstrated. The nonlinear refractive index of the fiber is estimated to be 9.3 × 10−15 (cm2/W) at a 1.55-μm wavelength.

The relative reactivities of cyclohexanones in which the 2-axial position is substituted by methyl or methoxy group in LiAlH4 reduction strongly support the Cieplak model which focuses on the importance of stabilisation of the transition state by antiperiplanar allylic bonds.

Dimethylpiperidinones and dimethylmethylenepiperidines have been hydrogenated over several Group 8, 9 and 10 transition metal catalysts and the stereochemistry of the products compared with those of the carbocyclic analogues. The results obtained suggest that intramolecular interactions between the nitrogen lone pair and the unsaturated bond play a major role in determining the stereochemistry of hydrogenation.

High Delta, small core single-mode fibers were investigated with emphasis on clarifying both their fundamental optical characteristics and on possible uses. Preparation of such high Delta single-mode fibers through the vapor phase axial deposition process made it possible to achieve the low transmission losses of 0.82 dB/km (at 1.61 microm) for a 2.9%-Delta fiber and 0.68 dB/km (at 1.62 microm) for a 1.9%-Delta fiber. Measurements of fundamental characteristics such as transmission loss spectrum, bending loss, dispersion, stimulated Raman scattering, and frequency chirping were made for high Delta single-mode fibers. Two possible uses were investigated: a direct coupling experiment achieved 43% coupling efficiency between high Delta fiber and a LED, and an optical pulse compression experiment in the 1.5-microm wavelength region provided pedestal-free optical pulses with 1.2-ps (FWHM) width.

Direct observation of a small magnetic moment distributed around sulfur atoms in CoS 2 has been made by means of polarized neutron diffraction technique. The observed data are analyzed on the basis of the theory by Hubbard and Marshall. The analysis shows that the observed magnetic moment distribution is aspherical around sulfur nuclei, and it can be interpreted in terms of asphericity of atomic 3p orbital for S - free ion. The magnetic moment may be considered to result from a covalent bonding effect between 3d-e g orbitals of cobalt atoms and 3p π orbitals of sulfur atoms. Here, 3p π orbitals point perpendicular to the axis of S 2 molecule which consists of sulfur atoms in CoS 2 .

The polarization analysis for the (200)M1 reflection has been made on a twin free single crystal of NiS 2 at ∼5 K. The final polarization ( P f ) was measured as a function of the rotating angle (ϕ) about the scattering vector. ( P f is approximately expressed by -0.95 cos 2ϕ.) The antiferromagnetic structure with respect to the first kind ordering was determined under the assumption that a particular domain distribution is not realized in the sample. The previously proposed non-collinear structure was confirmed. A weakferromagnetic moment more than 0.01 (µ B ) was observed on each nickel ion forming the pyrite structure by measuring the flipping ratio of the (400) nuclear reflection. Mechanisms for weakferromagnetism are discussed.