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Biomedical subjects

E Nakao

Publications and source records attributed to E Nakao.

30 records · Page 2Linked to original sources
PubMed1994

Pharmacological profile of the novel, potent and selective peptide leukotriene antagonist (E)-2,2-diethyl-3'-[2-[2-(4-isopropyl)thiazolyl]ethenyl]succinanilic acid.

In this report, the in vitro and in vivo pharmacological profile of MCI-826 ((E)-2,2-diethyl-3'-[2-[2-(4-isopropyl) thiazolyl]ethenyl]succinanilic acid, CAS 121230-22-6) is described. In isolated guinea pig ileum, MCI-826 inhibited LTD4 (a peptide leukotriene, 10(-9) mol/l)-induced contraction in a concentration-dependent manner with an IC50 of 6.8 x 10(-12) mol/l. It had no effect on histamine (10(-5) mol/l)-, serotonin (2.5 x 10(-5) mol/l)-, or acetylcholine (5.5 x 10(-6) mol/l)- induced contractions in isolated guinea pig ileum. In isolated guinea pig trachea, MCI-826 demonstrated competitive antagonism of the contractile activity of LTD4 and LTE4 with pA2 values of 9.0 and 8.8, respectively. MCI-826 inhibited LTC4-induced contraction in a concentration-dependent manner. However, in the presence of an inhibitor of the metabolism of LTC4 to LTD4, MCI-826 (10(-6) mol/l) produced no effect on LTC4 concentration-response curves in guinea pig trachea. In the in vivo study, the oral administration of MCI-826 caused a dose-dependent inhibition of LTC4- and LTD4-induced bronchoconstrictions in guinea pigs with an ED50 of 0.049 and 0.013 mg/kg, respectively. However, MCI-826 (3 mg/kg p.o.) showed no effect on histamine-induced bronchoconstriction in guinea pigs. The pharmacological half-life of orally administered MCI-826 as assessed by LTD4-induced bronchoconstriction was more than 12 h in guinea pigs. MCI-826 also inhibited antigen-induced bronchoconstriction in a dose-dependent manner with a MID (minimum dose that causes significant inhibition) of 0.1 mg/kg p.o. in guinea pigs.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetylcholine↗
PubMed1993

Glomerulocystic kidney--report of an adult case.

A 32-year-old adult case of glomerulocystic kidney disease (GCK) is reported. He had brain and muscle atrophy, probably due to congenital malformation. Progressive renal failure developed and he died. Autopsy disclosed multiple tiny cysts exclusively in the renal cortices. Microscopic study revealed that the cysts were dilated Bowman's spaces. This case is the 12th adult case reported in the world.

Adult↗
PubMed1991

Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17 alpha-esters containing a functional group.

A series of 21-desoxy-21-chlorocorticosteroids that contain a functionalized ester group at 17 alpha has been prepared and examined to separate their systemic activity from topical antiinflammatory activity. Introduction of the functionalized ester group at 17 alpha was carried out by an acid-catalyzed formation of cyclic ortho esters with 17 alpha,21-hydroxyl groups of corticosteroids and subsequent acid-catalyzed hydrolysis. As for the functional group, chloro, methoxy, acetoxy, cyano, cyclopropyl, or alkoxycarbonyl group was introduced at the terminal carbon atom of the 17 alpha-alkanoate group. The topical antiinflammatory activity and systemic activity of these compounds were examined and found to be significantly dependent on the functionalities in the 17 alpha-esters. Among these derivatives, a series of 17 alpha-(alkoxycarbonyl)alkanoates (17 alpha-OCO(CH2)nCOOR) showed an excellent separation of the systemic activity from topical activity. The effects of the number of methylene groups (n) and of the alkyl groups of the ester (R) on either topical or systemic activity of the corticosteroid derivatives were also investigated.

Administration, Topical↗
PubMed1991

Significance of levels of circulating IgA-class immune complex in discriminant analysis of patients with IgA nephropathy before renal biopsy.

Discriminant analysis of clinical markers including circulating IgA-class immune complex (IgA-CIC) before renal biopsy in patients with IgA nephropathy is described. Fifty-six patients with IgA nephropathy (IgA nephropathy group) and 54 patients with other primary chronic glomerulonephritis (non-IgA nephropathy group) were examined. Discriminant analysis was applied to separate these two groups by using 21 clinical markers including levels of IgA-CIC. The levels of IgA-CIC in sera were measured by a solid-phase anti-C3 Facb enzyme immunoassay (EIA). Among these clinical markers, the levels of serum IgA, IgA-CIC and creatinine, and the degree of microhematuria in the IgA nephropathy group were significantly higher than those in the non-IgA nephropathy group. Contributions of IgA and IgA-CIC to the classification were very high and both had almost the same effect. The correct classification rate was 80.00% using five clinical markers: serum IgA, microhematuria, IgA-CIC, serum creatinine, and blood urea nitrogen. It was shown that the levels of serum IgA and IgA-CIC were major markers for the clinical diagnosis of patients with IgA nephropathy. It was concluded that discriminant analysis before renal biopsy was useful for the diagnosis of IgA nephropathy.

Adolescent↗
PubMed1978

Basic experiments on oral administration of 5-fluorouracil emulsion as adjuvant chemotherapy to surgical treatment for gastric cancer.

Oral administration of 5-fluorouracil (5-FU) emulsion was compared experimentally with that of 5-FU aqueous solution as to the degree of absorption and tissue distribution. After oral administration of both the 5-FU emulsion and the 5-FU solution, 5-FU was detected at the highest level in both the stomach and the duodenum. This seems to suggest that 5-FU is strongly affinitive to the tissues of the gastrointestinal tract. As to the relative concentration of these two forms of the drug, the oral administration of the 5-FU emulsion resulted in a maximum value 1.5 times higher than that of the 5-FU solution. An appreciable concentration of 5-FU was maintained for a considerably long time with the administration of 5-FU emulsion. In the lymph, the maximum level of the 5-FU emulsion was three times higher than that of the 5-FU solution. The drug concentration of the 5-FU emulsion remained higher than that of the 5-FU solution through the entire duration of the experiment. Regarding the drug concentration in the regional lymph nodes, the pattern demonstrated was almost the same as in the lymph itself. It is expected that the oral administration of 5-FU emulsion may be useful as an adjuvant to the surgical treatment of gastric cancer, because of the high drug concentration resulting both in the gastrointestinal tract and in the regional lymph nodes.

Administration, Oral↗
PubMed1978

Histological evaluation of the effect of 5-FU emulsion on lymph node metastasis of stomach cancer.

In order to evaluate the effect of anticancer drugs on the metastatic lesions of the regional lymph nodes from stomach cancers removed after oral administration of 5-FU emulsion, histological examinations of the specimens obtained from 107 surgical cases were carried out. In additional 13 cases with gastric cancer, the active 5-FU concentrations in the regional lymph nodes were determined. The effect of 5-FU emulsion in metastatic lesions as determined was histologically classified into Grades 0 to III according to the severity and extent of damaged cells and cell nests Grades II and III were judged to demonstrate the beneficial effect of the 5-FU emulsion. Such changes were identified in 62.0 per cent of the 242 metastatic lymph nodes, and the effectiveness increased as the total dose of the 5-FU emulsion administered increased (50.9 per cent for 5,000 mg or less, 70.9 per cent for 5,000 to 6,000 mg, and 72.7 per cent for 6,000 mg or more). The rate of effectiveness also varied with the histological type of the primary carcinoma, i.e. the differentiated type being more sensitive. The mean active 5-FU level in the regional lymph nodes was higher after the administration of 5-FU emulsion than of 5-FU solution supporting the earlier animal experiments.

Adenocarcinoma↗
PubMed1973

Immunogenicity of purified, inactivated chikungunya virus in monkeys.

Chikungunya (CHIK) virus, harvested from infected BHK-21 cell cultures and highly purified by a method combining zinc acetate precipitation, Sephadex-Sepharose column chromatography, and sucrose density gradient centrifugation, was subjected to ultraviolet (UV) irradiation and treatment with formalin. Inactivation of the virus by UV light was apparently a first-order reaction. The virus treated with 0.05% formalin at 4 degrees C was inactivated completely after 7 weeks, but when treated with 0.025% formalin retained its plaque infectivity at least 17 weeks. Both UV- and formalin-inactivated viruses induced production of anti-CHIK neutralizing antibodies in Japanese monkeys with no preimmune antibodies. Judging by the titres of antibodies produced, the immunogenic effect of the UV-irradiated virus was superior to that of the formalin-treated virus.

Animals↗
PubMedDate not supplied

Knot formation in a long tube used in the treatment of a post-operative adhesive small bowel obstruction.

The complications specific to the management of the nasointestinal long tubes for small bowel obstruction are not generally appreciated. We report here of a case of knot formation of the long tube which was inserted for a 60 year-old male. Because it was difficult to place the tube in the distal stomach despite frequent changes in patient position, two coiled loops were noted at the fornix as the tip of the tube reached the antrum. The tube was gently removed without injury to the esophagus or stomach under fluoroscopic control. This case illustrates that when a long tube is used, the formation of multiple coils in the stomach should be avoided during placement to prevent knotting. Furthermore, a knotted tube can be gently removed non-operatively without esophageal injury. A short tube may be superior to a long tube because most of the complications can be avoided.

Catheters, Indwelling↗