Effect of antiemetics on zolbetuximab-induced gastric injury and emesis in ferrets.

Claudin-18 splice variant 2 (CLDN18.2), a tight junction protein, is a highly cell type-specific antigen that is expressed by differentiated gastric mucosa cells. The expression of CLDN18.

Effect of ASP8062 on morphine self-administration and morphine-induced respiratory suppression in monkeys.

ASP8062 is an orally available GABA receptor positive allosteric modulator (PAM). This study assessed the potential of ASP8062 for treating opioid use disorder (OUD). Three rhesus monkeys were pretreated with ASP8062 (0.

Brachial plexus injury and upper rib fracture after median sternotomy in cardiac surgery.

Objectives: Sternal retractors utilized during open-heart surgeries through median sternotomy can cause upper rib fractures which sometimes further leads to brachial plexus injury. We aimed to investigate the incidence of brachial plexus injury and upper rib fractures in open-heart surgeries and how these injuries are associated with each other.

Methods: We investigated 1050 cases during the past five years.

A novel GABA receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia.

The gamma-aminobutyric acid type B (GABA) receptor agonist, the sodium salt of gamma-hydroxybutyrate (GHB), significantly improved pain, sleep disturbance and fatigue in fibromyalgia (FM) patients. However, the use of GABA receptor agonists is limited by their undesirable side-effects. To clarify whether GABA receptor positive allosteric modulator (PAM) approach would achieve analgesia with less side-effects than GABA receptor agonist in FM, we investigated the potential of a novel GABA receptor PAM, ASP8062, for FM treatment.

Gene Expression Profiling in Short-Term Imbibition of Wheat: Tools for Dissecting of Pasting Properties of Imbibed Wheat Seeds.

Germination of wheat maximizes phytochemical content and antioxidant activity while altering chemical composition, gluten content, and pasting properties. This study investigated the effect of short-term imbibition on gene expression profiles and the physical and functional characteristics of wheat. Changes in gene expression profiles of wheat during short-term imbibition (0, 16, and 24 hr) were evaluated by DNA microarray analysis.

[Treatment of Mediastinitis after Open Heart Surgery Using Negative Pressure Wound Therapy with Irrigation].

Mediastinitis occurs after open heart surgery in a small number of cases. When it occurs, early diagnosis and treatment are important. A 69-year-old male patient suffered from mediastinitis after total aortic arch replacement.

Draft Genome Sequence of Bacillus licheniformis Heshi-B2, Isolated from Fermented Rice Bran in a Japanese Fermented Seafood Dish.

Heshi-B2 was isolated from fermented rice bran in Heshiko, a food produced by aging salted mackerel with fresh rice bran. Here, we report the draft genome sequence of Heshi-B2, originating from a Heshiko sample from Fukui Prefecture, Japan.

A comparison of the effects of heat moisture treatment (HMT) on rheological properties and amylopectin structure in sago () and arenga () starches.

The objective of this study was to study and compare the impact of HMT on rheology and textural properties observed between sago and arenga starces, and then related to structural change of amylopectin. The HMT were conducted using the autoclaving method at 20% moisture content and heated to 120 C for 60 min for sago and 90 min for arenga starch as optimum condition. The HMT shifted gelatinization temperature higher and reduced the enthalpy of both starches.

GABA-B Agonist Baclofen Normalizes Auditory-Evoked Neural Oscillations and Behavioral Deficits in the Knockout Mouse Model of Fragile X Syndrome.

Fragile X syndrome is a genetic condition resulting from gene mutation that leads to intellectual disability, autism-like symptoms, and sensory hypersensitivity. Arbaclofen, a GABA-B agonist, has shown efficacy in some individuals with FXS but has become unavailable after unsuccessful clinical trials, prompting interest in publicly available, racemic baclofen. The present study investigated whether racemic baclofen can remediate abnormalities of neural circuit function, sensory processing, and behavior in knockout mice, a rodent model of fragile X syndrome.

Draft Genome Sequence of Paenibacillus amylolyticus Heshi-A3, Isolated from Fermented Rice Bran in a Japanese Fermented Seafood Dish.

Paenibacillus amylolyticusstrain Heshi-A3 was isolated in Fukui prefecture, Japan, from fermented rice bran in Heshiko, a traditional dish that is produced by aging salted mackerel with fresh rice bran at an ambient temperature for around 7 months to over one year. Here, we report the draft genome sequence ofPaenibacillus amylolyticusstrain Heshi-A3.

Draft Genome Sequence of Oceanobacillus picturae Heshi-B3, Isolated from Fermented Rice Bran in a Traditional Japanese Seafood Dish.

Oceanobacillus picturae strain Heshi-B3 was isolated from rice bran in a traditional fermented seafood dish named Heshiko, which was produced in Fukui Prefecture in Japan. Here, we report the draft genome sequence of O. picturae strain Heshi B-3.

Synthesis and pharmacological evaluation of optically pure, novel carbonyl guanidine derivatives as dual 5-HT2B and 5-HT7 receptor antagonists.

A series of 9-disubstituted N-(9H-fluorene-2-carbonyl)guanidine derivatives have been discovered as potent and orally active dual 5-HT(2B) and 5-HT(7) receptor antagonists. Upon screening several compounds, N-(diaminomethylene)-4',5'-dihydro-3'H-spiro[fluorene-9,2'-furan]-2-carboxamide (17) exhibited potent affinity for both 5-HT(2B) (Ki = 5.1 nM) and 5-HT(7) (K(i) = 1.

Inactivation of Kudoa septempunctata in olive flounder meat by liquid freezing.

Kudoa septempunctata in olive flounder meat was inactivated using 3 distinct freezing methods：liquid freezing for 5 min, air blast freezing at －30℃ for 5 h, and －80℃ for 1 h. The fracture curve of olive flounder meat subjected to liquid freezing resembled that of meat stored at 4℃, indicating that the structure of olive flounder muscle was well preserved. In contrast, air blast freezing induced the disappearance of the fracture point in the fracture curve, indicating that there was deterioration in the meat quality.

Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT₂B and 5-HT₇ receptor antagonists. Part 2.

We previously reported that the novel dual 5-HT₂B and 5-HT7 receptor antagonist N-(9-hydroxy-9H-fluorene-2-carbonyl)guanidine (4) exerted a suppressing effect on 5-HT-induced dural protein extravasation in guinea pigs. To develop a synthetic strategy, we performed docking studies of lead compound 4 bound to 5-HT₂B and 5-HT₇ receptors, and observed that the carbonyl guanidine group forms a tight interaction network with an active center Asp (D135:5-HT2B, D162:5-HT₇), Tyr (Y370:5-HT₂B, Y374:5-HT₇) and aromatic residue (W131:5-HT2B, F158:5-HT₇). Based on molecular modeling results, we optimized the substituents at the 5- to 8-position and 9-position of the fluorene ring and identified N-(diaminomethylene)-9-hydroxy-9-methyl-9H-fluorene-2-carboxamide (24a) exhibits potent affinity for 5-HT₂B (Ki=4.

Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists.

To identify potent dual 5-HT2B and 5-HT7 receptor antagonists, we synthesized a series of novel carbonyl guanidine derivatives and examined their structure-activity relationships. Among these compounds, N-(9-hydroxy-9H-fluorene-2-carbonyl)guanidine (10) had a good in vitro profile, that is, potent affinity for human 5-HT2B and 5-HT7 receptor subtypes (Ki=1.8 nM and Ki=17.

Surgical treatment of papillary fibroelastoma in the aortic valve: a case report.

With the exception of myxomas, primary tumors of the heart are very rare. We present here our experience with papillary fibroelastoma in the aortic valve. We could not preserve the aortic valve because of the wide attachment of the tumor to the valve and aortic regurgitation.

Congenital systemic and coronary-to-pulmonary artery fistulas.

Congenital systemic-to-pulmonary artery fistulas are very rare, with the exception of congenital heart disease and pulmonary sequestration. We describe the first reported case of left internal mammary and bronchial artery to pulmonary artery fistulas associated with bilateral coronary arteries to pulmonary artery fistulas.

Intrathecal injection of hepatocyte growth factor gene-modified marrow stromal cells attenuates neurologic injury induced by transient spinal cord ischemia in rabbits.

Background: Our previous studies showed that transfer of hepatocyte growth factor (HGF) gene or transplantation of marrow stromal cells (MSCs) remarkably attenuated neurologic injuries after spinal cord ischemia. We sought to investigate a novel neuroprotective strategy of transplantation of human HGF gene-modified MSCs on ischemic spinal cords.

Methods: Human HGF gene was transferred into MSCs in vitro.

Characterization of pullulanase (PUL)-deficient mutants of rice (Oryza sativa L.) and the function of PUL on starch biosynthesis in the developing rice endosperm.

Rice (Oryza sativa) allelic sugary1 (sug1) mutants defective in isoamylase 1 (ISA1) accumulate varying levels of starch and phytoglycogen in their endosperm, and the activity of a pullulanase-type of a debranching enzyme (PUL) was found to correlate closely with the severity of the sug1 phenotype. Thus, three PUL-deficient mutants were generated to investigate the function of PUL in starch biosynthesis. The reduction of PUL activity had no pleiotropic effects on the other enzymes involved in starch biosynthesis.

Interleukin-1 receptor antagonist attenuates the severity of spinal cord ischemic injury in rabbits.

Objective: Thoracic and thoracoabdominal aortic surgery is sometimes complicated by subacute or delayed paraplegia. Pro-inflammatory cytokine interleukin-1 (IL-1) beta has been implicated in extensive inflammation and progressive neurodegeneration after ischemia. Using a rabbit model, we investigated the neuroprotective effects of IL-1 receptor antagonist (IL-1ra) in a temporal fashion.

Effects of serotonin 5-HT(3) receptor antagonists on CRF-induced abnormal colonic water transport and defecation in rats.

The effects of corticotropin releasing factor (CRF) and serotonin (5-HT)(3) receptor antagonists on intestinal water transport are not well understood. Hence, we established a CRF-induced abnormal water transport model in rat colon, and evaluated the effects of 5-HT(3) receptor antagonists including ramosetron, alosetron, and cilansetron, and the antidiarrheal agent loperamide, in this model. In addition, the effects of 5-HT(3) receptor antagonists and loperamide on abnormal defecation induced by CRF in rats were examined.