Synthesis of diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists.

We synthesized diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists with non-hypotensive activity. Compound 10c showed selective Ca(2+)-permeable AMPA receptor antagonist activity and neuroprotective effects in transient global ischemia models in gerbils.

Synthesis of polyamine derivatives having non-hypotensive Ca2 +-permeable AMPA receptor antagonist activity.

In order to obtain non-hypotensive and Ca2+-permeable AMPA receptor antagonists, we have synthesized a series of 1,4-bis(4-piperidinylmethyl)diaminobutanes. Compounds 13b, c, f had desirable properties.

Successful resection of ampullary carcinoma in a father and adenoma in a daughter with familial adenomatous polyposis following detection by surveillance: report of two cases.

This report describes the successful resection of ampullary carcinoma in a 58-year-old man and an adenoma in his 28-year-old daughter after they had undergone proctocolectomy for familial adenomatous polyposis (FAP). Both patients had been monitored by surveillance endoscopy once a year since their proctocolectomy. The father was found to have an ampullary adenoma 26 years after proctocolectomy, and ampullary carcinoma was detected 2 years later, for which pancreatoduodenectomy was performed. Histological examination of the specimen revealed an ampullary carcinoma, 2.5 x 1.7 cm, that had invaded the submucosal layer, but no lymph node metastasis was found. The patient's daughter underwent endoscopy, which showed an ampullary polyp 6 years after total colectomy. Endoscopic mucosal resection of the periampullary lesion was performed, and histological examination revealed a dysplastic tubular adenoma 0.6 x 0.4 cm in diameter. This report reinforces the importance of long-term periodic surveillance of patients with FAP by gastroduodenal endoscopy.

Flow cytometric analysis of nuclear DNA heterogeneity in gastric cancer.

Flow cytometric analysis of nuclear DNA ploidy was performed to evaluate the clinical significance of DNA-ploidy heterogeneity and DNA-index heterogeneity between the superficial layer and the deep layer of the tumor obtained from 88 advanced gastric cancer patients. DNA-ploidy heterogeneity was observed in 28 patients (31.8%) and characterized mainly by diploidy in the superficial layer and aneuploidy in the deep layer. More than 10% difference in the DNA index among aneuploidy (DNA-index heterogeneity) was observed in 10 (26.3%) of 38 patients with aneuploidy. There was no tendency for the DNA index to increase with deep infiltration. DNA-ploidy and DNA-index heterogeneities were not correlated with the various clinicopathological characteristics. Patients with aneuploidy had significantly poorer prognosis than did those with diploidy. The survival rate for patients with DNA heterogeneity was not significantly different from that for patients without DNA heterogeneity. These results suggest that the DNA-ploidy pattern may be an important prognostic factor, but that DNA heterogeneity may not have an impact on the survival in advanced gastric cancer.

[Preservation of anal transitional zone in restorative proctocolectomy].

Since 1980, restorative proctocolectomy has been established for surgical therapy to ulcerative colitis. The crucial points of this procedure are mucosectomy of the anorectal mucosa and pouch anal anastomosis. Mucosectomy is often difficult due to long standing acute and chronic inflammation and incomplete microscopically and leakage of pouch anal anastomosis is relatively high probably due to steroid given prior to surgery or direct effect of anorectal mucosal inflammation. Regards to postoperative bowel function, nocternal soiling is frequently recognized in the patients who received this operation. To overcome these technical and functional disadvantages, anal transitional zone preservation without mucosectomy and stapled anastomosis between pouch and the upper rim of the puborectalis muscle has been performed. Our series of 84 cases with this modified method, anastomotic leakage was significantly decreased and nocternal soiling was completely disappeared within 7 months postoperatively. And one stage procedure became possible unless severe, or high doses of steroid given prior to surgery. Only one case of mild dysplasia was experienced in the remaining rectal mucosa which was disappeared at the next examination. Medical treatment to the remaining lesion was not necessary in the most of cases. Anal canal preservation is superior to mucosectomy in the points of bowel function and minimizing postoperative complications.

[A case of thoracic empyema extended into the abdominal cavity].

A case of thoracic empyema after artificial pneumothorax for lung tuberculosis was presented, which extended into the abdominal cavity. 65 years old man, who was operated on for lung tuberculosis about 30 years ago, took the routine physical examination and the abdominal mass was picked up on examination. Echogram and CT showed huge homogeneous mass in the right thorax and the right upper abdominal cavity. The operative finding showed that thoracic empyema extended into the abdominal cavity and formed a huge mass. Decortication and extirpation of thoracic empyema and abdominal mass was performed with a combined partial resection of the lung, diaphragma, and thoracic wall. The histopathology of the abdominal mass showed chronic empyema and hematoma.

[Evaluation of surgical treatment for spontaneous pneumothorax].

To evaluate the effect of surgical treatment for spontaneous pneumothorax, we examined eighty patients who underwent the surgical treatment. Out of these, thirty five patients (53.0%) were the recurrent episode of the disease, since we vigorously chose surgical treatment for the second attack of the disease. Operative complications were observed in 6 cases (7.1%) including 2 cases of lasting air leakage and 1 case of bleeding, pneumonia, wound infection and atelectasis. Postoperative recurrence was not seen. From a viewpoint of prevention of the postoperative recurrence, the surgical treatment is effective and safe method.

[The efficacy of semiselective intraarterial infusion therapy in advanced or recurrent gastric cancer].

We use CDDP and have compared the semiselective intraarterial infusion (ia group) with intravenous infusion (i.v. group) by measuring levels of the administered drug in blood and the abdominal organ tissues. In portal blood, the ia group showed a significant increase compared with the i.v. group. The patient tissue level was compared between the two groups. Higher levels were obtained in the peritoneum in the ia group. These results suggest that semiselective intraarterial infusion therapy is effective in peritoneal dissemination.

[Dissolution of cholesterol mixed stones with methyl tertiary butyl ether in vitro].

Methyl tertiary butyl ether (MTBE) has been proposed as a new therapeutic material for the dissolution of pure cholesterol mixed stones. To determine the effect of solvent circulation and fragmentation on dissolution of cholesterol mixed stone in MTBE, we carried out in vitro experiments. The following results were obtained: 1) The addition of 1% EDTA and 0.5% UDCA in MTBE enhanced the dissolution of cholesterol mixed stones (56 +/- 8% of initial weight after 3 hours vs. 48 +/- 5% of initial weight after 3 hours in MTBE alone). 2) Cholesterol mixed stones with circulation of MTBE + 1% EDTA + 0.5% UDCA were dissolved more rapidly than those without. 3) Under in vitro condition, when cholesterol mixed stones were fragmented with URAT-1M stone disintegrator, fragments of stones were dissolved 96% of initial weight in solvent circulation of MTBE + 1% EDTA + 0.5% UDCA after 3-6 hours. In conclusion, these data indicated that both fragmentation of cholesterol mixed stones and solvent circulation of MTBE + 1% EDTA + 0.5% UDCA considerably accelerated dissolution of cholesterol mixed stones in vitro.

[Experimental study of the effect of an elemental diet on liver regeneration].

The influence of branched chain amino acids and lipid on liver regeneration was examined after two-thirds hepatectomy in rats. Elemental diet (ED) as components of enteral nutrition was given through the gastrostomy tube. The rats were divided into four groups according to the amounts of branched chain amino acids (BCAA) and lipid in the diet as follows: ED-I; BCAA 27%, Cal/N ratio: 74, ED-II; BCAA 37%, Cal/N ratio: 95, ED-III; BCAA 37% + lipid emulsion, Cal/N ratio: 99, ED-AC; commercially available elemental diet. The degree of liver regeneration of these groups of rats were compared with that of the control rats which were fed per os ad libitum. The liver regeneration rate of each group was as follows: ED-I; 59%, ED-II; 88%, ED-III; 92%, ED-AC; 79%, the control group; 89%. Remarkable fatty deposits were microscopically observed in each liver of ED-I, II and AC groups. Fatty change in the liver of ED-III group was minimum. The observation indicates that administration of branched chain amino acid enriched elemental diet and lipid emulsion is effective for regeneration of the liver after partial hepatectomy.

Extraction of retained gallstones using a fiber-choledochoscope through a PTC-drainage fistula.

After unsuccessful attempts to completely remove gallstones, endoscopic papillotomy was carried out to remove the stones after closure of the T-tube tract. We treated two patients with successful extraction of retained gallstones using a fiber-choledochoscope through a percutaneous transhepatic cholangio-drainage (PTCD) fistula. This technique can be applied in cases when endoscopic papillotomy cannot be performed or for patients who are poor risks for repeat surgery.

Intestinal responses to hyperosmolar glucose infusion in dogs.

Physiological and morphological changes of small intestine after hyperosmolar glucose infusions into canine jejunum were studied using in vivo perfusion model. Infusions of 40 ml of 50% and 20% glucose solution into the jejunal loops induced biphasic osmolar degression in the lumen. Osmolarity of jejunal venous blood was rapidly increased and maintained the maximal level (approximately 320 mOM/L). Blood flow to the jejunal loop was significantly increased after 50% glucose infusion compared to 5% glucose infusion. Most characteristic electron microscopic change of jejunal epithelial cell was pseudo-pod like process projected into the jejunal lumen, which was very similar to that of cholera.