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Biomedical subjects

H Terauchi

Publications and source records attributed to H Terauchi.

At least 19 recordsLinked to original sources
PubMed1997

Nicotinamide derivatives as a new class of gastric H+/K(+)-ATPase inhibitors. 1. Synthesis and structure-activity relationships of N-substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides.

A new series of N-Substituted 2-(benzhydryl- and benzylsulfinyl)nicotinamides 7 and 8 were synthesized. Upon acid activation in the acidic environment of the parietal cell, these compounds are converted into their active forms, 2,3-dihydro-3-oxoisothiazolo[5,4-b]pyridines 5, which inhibit gastric H+/K(+)-ATPase. Inhibitory activities against [14C]aminopyrine accumulation stimulated by dibutyryl cAMP in isolated rabbit parietal cells in vitro and histamine-induced gastric acid secretion in pylorus-ligated rats by intraduodenal administration in vivo were evaluated, and the structure-activity relationships were examined. Among the compounds synthesized, 2-[(2,4-dimethoxybenzyl)sulfinyl]-N-(4-pyridyl)nicotinamide (8b) showed potent inhibitory activities in vitro and in vivo equivalent to those of omeprazole, a typical H+/K(+)-ATPase inhibitor. Moreover, 8b was much more stable at neutral and weakly acidic pH than omeprazole, lansoprazole, and pantoprazole. Compound 8b is considered to be a promising agent for treating acid-related gastrointestinal disorders.

Aminopyrine↗
PubMed1997

Nicotinamide derivatives as a new class of gastric (H+/K+)-ATPase inhibitors II. Synthesis and structure-activity relationships of 2[(2,4-dimethoxybenzyl)sulfinyl]-N-(4-pyridinyl)pyridine-3-carboxamides.

Members of a new series of 2-[(2,4-dimethoxybenzyl)sulfinyl]-N-(4-pyridinyl)pyridine-3-carboxamides were synthesized and evaluated for their gastric antisecretory activity and the ability to inhibit cytochrome P450-dependent O-dealkylation of 7-ethoxycoumarin (7-EC) in rat liver microsomes. Several of the compounds synthesized exhibited potent inhibitory activities against both [14C]aminopyrine accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells and histamine-induced gastric acid secretion in pylorus-ligated rats when administered intraduodenally; their inhibitory activities were equivalent to or superior to those of the parent compound [2- [(2,4-dimethoxybenzyl)sulfinyl]-N-(4-pyridinyl)pyridine-3-carboxamide] and omeprazole. Among the compounds having potent antisecretory activity in vitro and in vivo, 2-[(2,4-dimethoxybenzyl)sulfinyl]-N-(2,5-dimethyl-4-pyridinyl) pyridine-3-carboxamide and 2-[(2,4-dimethoxybenzyl)sulfinyl]-N-(2,6-dimethyl-4-pyridinyl)pyridine-3 - carboxamide in particular showed lower inhibitory activity against the 7-EC deethylase than omeprazole. It seems probable that, unlike omeprazole, these compounds do not interact with a metabolism of other drugs in vivo. These compounds, therefore, are considered to be more promising candidate agents for treating acid-related gastrointestinal disorders than the parent compound reported previously.

7-Alkoxycoumarin O-Dealkylase↗
PubMed1997

Nicotinamide derivatives as a new class of gastric (H+/K+)-ATPase inhibitors. III. Synthesis and gastric antisecretory activity of 2-[(2- and 4-aminobenzyl, and alpha-methylbenzyl)sulfinyl]-N-(4-pyridinyl) -3-pyridinecarboxamides.

A new series of 2-[(2-aminobenzyl, 4-aminobenzyl, and alpha-methylbenzyl) sulfinyl]-N-(4-pyridinyl)-3-pyridinecarboxamides. was synthesized and evaluated for gastric antisecretory activities. Several of the compounds synthesized exhibited potent inhibitory activities against [14C]aminopyrine accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells and histamine-induced gastric acid secretion in pylorus-ligated rats by intraduodenal administration. In particular, the more polar diastereoisomer of 2-[(4-methoxy-alpha-methylbenzyl)sulfinyl] -N-(4-pyridinyl)-3-pyridinecarboxamide (13b) showed in vivo inhibitory activity equivalent or superior to that of omeprazole and was a more selective (H+/K+)-ATPase inhibitor than omeprazole.

Animals↗
PubMed1997

[The long-term cystic bleb appearance and safety after trabeculectomy with mitomycin C].

The clinical appearance of cystic blebs and the incidence of bleb infection were retrospectively evaluated in 215 trabeculectomies with mitomycin C. The incidence of cystic bleb formation in trabeculectomy was 79% (169/215). The cumulative incidence of the cystic bleb survival when using the Kaplan-Meier method was 73% in the 50th month after surgery. The incidence of large cystic bleb survival was better than that of small and localized cystic blebs. There was statistically significant difference. The incidence of cystic bleb survival without Seidel phenomenon and bleb infection was 96% in the first year after surgery and 91% in the third year. Bleb infections occurred in two of 169 eyes (1.2%). Bleb infection was successfully treated and there were no cases of endophthalmitis. The large cystic blebs had a higher incidence of bleb infection than the small ones. In one of 25 eyes treated with antibiotic eye drops after surgery, the Seidel test was positive and bleb infection occurred. The Seidel test was positive in 5 of 96 eyes in which antibiotic eye drops were not used and bleb infection occurred in one of these 5 eyes.

Female↗
PubMed1996

[Long-term surgical effects of trabeculotomy combined with sinusotomy].

We retrospectively analyzed long-term effects of trabeculotomy combined with sinusotomy. We reviewed 29 eyes with primary open angle glaucoma and 6 eyes with psuedexfoliation glaucoma. The preoperative intraocular pressure was equal to or over 21 mmHg. All cases had been subjected to initial trabeculotomy combined with sinusotomy. The had been followed up for at least 3 years after surgery. The mean age was 57.8 years and the mean follow-up period was 40.5 months. The preoperative intraocular pressure was 24.3 +/- 5.9 mmHg (Mean +/- standard deviation) and the postoperative intraocular pressure was 15.8 +/- 3.8 mmHg. There was statistically significant difference between preoperative and postoperative intraocular pressure. The Kaplan-Meier life table method indicated a success rate at 50 months after surgery of 0.63 +/- 0.15, as defined by intraocular pressure of 20 mmHg or lower, and of 0.35 +/- 0.08 as defined by intraocular pressure equal to or lower than 14 mmHg. The success rate of filtering blebs was 0.10 +/- 0.05 at 50 months. Eleven of 35 eyes (37%) were controlled at equal to or below 14 mmHg and 20 of 35 (67%) eyes were controlled at equal to or lower than 16 mmHg at final postoperative intraocular pressure. The surgical results of trabeculotomy combined with sinusotomy remain effective in controlling intraocular pressure levels for long periods.

Adult↗
PubMed1996

[Intraocular pressure decrease after phacoemulsification-aspiration+ intraocular lens implantation in primary open angle glaucoma eyes].

Phacoemulsification-aspiration and intraocular lens implantation (PEA + IOL) were carried out in 40 primary open angle glaucoma (POAG) eyes without history of surgery and 53 control (cataract only) eyes. Postoperative change in intraocular pressure (IOP) was evaluated over a long period (at least 18 months, average follow-up period 34 months). The postoperative IOP was significantly lower than the preoperative level in every group from 6 months to 3 years. An IOP decrease of 1.5 mmHg was maintained for 3 years in the control group. A decrease of 2.5 mmHg was stable for 3 years in the good POAG group in which preoperative IOP was controlled (< or = 20 mmHg) with medication. IOP decrease in the poor POAG group in which preoperative IOP was over 21 mmHg with medication, was 5.5 mmHg, and was maintained for 3 years. Medication did not differ significantly before or after the operation. These results imply that in POAG an IOP decrease can be expected after PEA + IOL.

Aged↗
PubMed1996

[Surgical effects of trabeculotomy combined with sinusotomy in advanced glaucoma patients controlled in normal intraocular pressure of 15 mmHg or higher].

Trabeculotomy combined with sinusotomy was performed in 30 eyes with advanced open angle glaucoma, whose intraocular pressure (IOP) had been controlled in their high teens with only topical medications. The mean pre- and postoperative IOP levels were 18.2 +/- 1.2 mmHg (mean +/- standard deviation) and 13.2 +/- 1.2 mmHg and the pressure reduction was 4.6 +/- 2.4 mmHg. Average pressure reduction was 28.8 +/- 9.3% and pressure reduction of 30% or more was obtained in 45% of the treated eyes. The pre- and postoperative medication scores were 4.47 +/- 1.50 and 3.07 +/- 1.17, respectively. There was statistically significant difference between the pre- and postoperative medication score. We had no cases in which the IOP reduction was greater than 9 mmHg and postoperative IOP was 9 mmHg or less. A 3-line drop in visual acuity was seen in only one eye. Twenty two of 30 eyes (73%) were controlled at 14 mmHg or less with medications at the last examination. These results show that trabeculotomy combined with sinusotomy in effective, and this procedure can be considered as an alternative choice for surgical treatment in advanced glaucoma.

Aged↗
PubMed1995

Development of potent serotonin-3 (5-HT3) receptor antagonists. II. Structrue-activity relationships of N-(1-benzyl-4-methylhexahydro-1H-1,4- diazepin-6-yl)carboxamides.

Our studies on 4-amino-5-chloro-2-ethoxybenzamides led to the discovery that the N-(1,4-dimethylhexahydro-1H-1,4-diazepin-6-yl)benzamide 9 and the 1-benzyl-4-methylhexahydro-1H-1,4-diazepine analogue 10 are potent serotonin-3 (5-HT3) receptor antagonists. Structure-activity relationship (SAR) studies on the influence of the aromatic nucleus of 9 and 10 upon inhibition of the von Bezold-Jarisch reflex in rats are described. Heteroaromatic rings such as pyrrole, thiophene, furan, pyridine, pyridazine, 1,2-benzisoxazole, indole, quinoline, and isoquinoline rings showed weak 5-HT3 receptor antagonistic activity. Within this series, use of the 1H-indazole ring as an aromatic moiety led to a substantial increase of the activity; the 1H-indazolylcarboxamides 54, 57, 97, and 102 showed potent 5-HT3 receptor antagonistic activity. The optimal compound identified via extensive SAR studies was N-(1-benzyl-4-methylhexahydro-1H-1,4-diazepin-6-yl)-1H-indaz ole-3- carboxamide (54), whose effect was superior to that of the corresponding benzamide 10 and essentially equipotent to those of ondanbsetron (1) and granisetron (4).

Animals↗
PubMed1995

[Clinical study on total omentumectomy for ovarian cancer].

Omentumectomy as a basic surgical method at the site of metastasis of ovarian cancer was examined, and the importance of total omentumectomy was evaluated. Nineteen patients who underwent initial laparotomy and did not receive preoperative chemotherapy were examined histopathologically. 1. Omental metastasis was found in 9 of 19 patients (47%). 2. No significant correlation was seen between the maximum tumor diameter and omental metastasis. 3. No significant correlation was seen between the amount of ascites and omental metastasis. 4. Cytodiagnosis of the ascites and intraperitoneal lavage fluid showed significantly more omental metastasis in patients who tested positive. 5. Omentum in the upward direction from the teniae of the transverese colon showed a high incidence of metastasis. 6. Postoperative disturbances associated with total omentumectomy were mild. These results indicated that the omentum is the principle site of metastasis of ovarian cancer, and omentumectomy should be performed as total resection whenever possible since metastasis occurs in the upward direction because partial resection is not significant and postoperative disturbance is mild but there is the need for requiring further examination in the case of Ia stage.

Adult↗
PubMed1995

[Surgical effects of trabeculotomy after long-term topical antiglaucoma medications].

We retrospectively analyzed the effects of long-term topical antiglaucoma therapy on the results of trabeculotomy. We studied 83 eyes with 76 primary open angle glaucoma and 7 eyes with capsular glaucoma, each of which had undergone trabeculotomy alone and none of which had a history of laser trabeculoplasty or glaucoma surgery. The outcome of trabeculotomy was assessed after a minimum follow-up of 12 months. Using a life-table method, there was no significant difference in the outcome of trabeculotomy between groups divided by duration and type of preoperative topical therapy. There was not statistically significant difference in the intraocular pressure reduction between the groups of long or short duration of topical therapy. We concluded that the duration and type of topical antiglaucoma medications had no significant effect on the outcome of trabeculotomy.

Administration, Topical↗
PubMed1994

[Multicenter prospective study of retinopathy of prematurity--II. Optimum timing of the first examination].

We reviewed the records of 360 cases of retinopathy of prematurity (ROP) in 12 institutions in Japan, and investigated the optimum timing of the first examination. On the basis of the onset of ROP and the timing of the first treatment, the first ophthalmological examination should be performed 3 weeks after birth or 29 weeks of postconceptional age at the latest. Regarding the visibility of the fundus, there was little hazy media after 29 weeks of postconceptional age. Under the basic policy that the severe progressive "plus" disease should be properly treated, we concluded that the first ophthalmological examination should be performed 3 weeks after birth at the latest. When the gestational age at birth is less than 26 weeks, funduscopy at the post conceptional age of 29 weeks is advisable.

Humans↗
PubMed1994

[Multicenter prospective study of retinopathy of prematurity--III. Timing of the coagulation therapy and the course of retinopathy of prematurity after coagulation].

We reviewed the records of 360 cases of retinopathy of prematurity (ROP) in 12 institutions in Japan, and investigated the timing of the coagulation therapy and the course of ROP after coagulation. The first coagulation therapy was performed at 9.6 weeks after birth and 35.9 weeks of postconceptional age on the average. The severity index in individual infants also showed that the disease became worse during the period from 32 to 36 weeks of postconceptional age. However, the fundus was clearly visible and there was no primary hazy media during this period. On the basis of the results of the timing of the first treatment, the visibility of the fundus, and the severity index in individual infants, we concluded that an ophthalmological examination with special care should be performed during the period from 32 to 36 weeks of postconceptional age.

Humans↗
PubMed1994

[Multicenter prospective study of retinopathy of prematurity--IV. Comparison with the data from University of Miami].

We investigated the records of 360 cases of retinopathy of prematurity (ROP) in 12 institutions in Japan (we treated the severe progressive "plus" disease by coagulation therapy), and compared them with data from University of Miami (Ophthalmology 94: 620-629, 1987), as representative of the natural course of ROP without coagulation therapy in those days. The timing of the first examination and the first positive diagnosis were later at University of Miami than in Japan. The time of maximal severity of the disease and occurrence of regression were also later the University of Miami than in Japan. In Japan, the first examination was performed at 29 weeks of postconceptional age or at 3 weeks after birth. At the University of Miami, the first examination was performed at 32 weeks of postconceptional age. If the severe progressive "plus" disease is to be properly treated by photo-coagulation or cryotherapy, it is essential to commence fundus examination earlier.

Florida↗
PubMed1993

Surgical effects of trabeculotomy ab externo on adult eyes with primary open angle glaucoma and pseudoexfoliation syndrome.

OBJECTIVES: Retrospective and prospective studies examined the surgical effects in lowering intraocular pressure levels of trabeculotomy ab externo in adult eyes with either primary open angle glaucoma or pseudoexfoliation syndrome. We report the results of primary trabeculotomy as an intervention for glaucoma. PATIENTS: Included in the retrospective study were 357 eyes of 227 patients with primary open angle glaucoma and 82 eyes of 65 patients with pseudoexfoliation syndrome, each of which underwent trabeculotomy ab externo alone and none of which had a history of laser or surgical treatment for ocular disease. Included in the prospective study were 33 eyes of 22 patients with primary open angle glaucoma and 17 eyes of 15 patients (older than 40 years) with pseudoexfoliation syndrome. RESULTS: A life-table analysis for the retrospective study showed that the final success probability (mean +/- SE) at 5 years after surgery was 73.5% +/- 6.3% in eyes with pseudoexfoliation syndrome, which is significantly better than 58.0% +/- 3.1% in eyes with primary open angle glaucoma (P < .05). Also, the higher the preoperative intraocular pressure levels are, the less likely that the postoperative intraocular pressure levels will be brought under control (P < .01). Surgical outcome in the prospective study demonstrated success in 27 (79%) of 34 eyes after 3 years and in 16 (64%) of 25 eyes after 5 years, with medication. Complications included Descemet's membrane detachment (one eye), cyclodialysis (one eye), and decreased visual acuity due to progression of cataract (four eyes). CONCLUSION: The surgical results of trabeculotomy ab externo remain effective in controlling intraocular pressure levels for a long time in selected patients. It thus appears that trabeculotomy ab externo can be considered as an alternative choice of surgical treatment in some cases of glaucoma.

Adult↗