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S Sakai

Publications and source records attributed to S Sakai.

At least 541 records · Page 30Linked to original sources
PubMed1987

Ca2+ channel-blocking effect of the yohimbine derivatives, 14 beta-benzoyloxyyohimbine and 14 beta-pho-nitrobenzoyloxyyohimbine.

Yohimbine possesses a relatively selective alpha 2-adrenoceptor antagonistic effect and a weak Ca2+ channel blocking activity, so two derivatives, 14 beta-benzoyloxyyohimbine and 14 beta-rho-nitrobenzoyloxyyohimbine were compared with yohimbine using those parameters. The two derivatives blocked Ca2+-induced contraction of the rat perfused mesenteric vascular bed at 3 X 10(-6) M, and developed dose-dependent shifts of the dose-response curve to the right in concentrations from 3 X 10(-6) to 10(-5) M. Yohimbine showed a weak Ca2+ channel-blocking effect only at a concentration of 10(-5) M. On the other hand, both derivatives at 3 X 10(-6) M did not affect the dose-response curve to noradrenaline-induced vasoconstriction. Furthermore, at 10(-8) M they had no effect on the dose-response curve to clonidine-induced inhibition of the twitch response of the rat isolated vas deferens evoked by electric stimulation, whereas yohimbine significantly attenuated clonidine-induced inhibition. These results indicate that introduction of bulky substituents into the 14-position of yohimbine intensely potentiated the Ca2+ channel-blocking effects and reduced alpha-adrenoceptor antagonistic effects compared with those of yohimbine, and suggest that chemical modifications of yohimbine may lead to structurally new types of Ca2+ channel-blockers.

Adrenergic alpha-Antagonists↗
PubMed1987

Stage-specific initiation of milk synthesis in the ovariectomized pregnant mouse.

Stage-specific initiation of milk synthesis was investigated in mice ovariectomized on days 7, 9, 11 and 13 of pregnancy, and the lactogenic response of the mammary gland was monitored by using the synthesis of casein, lactose content and PRL binding as parameters. Pregnant mice ovariectomized on day 7 or 9 showed no increase in these parameters 24 h after operation. After day 11 of pregnancy, a clear response was induced by ovariectomy, characterized by a low level of casein synthesis, small amounts of lactose and PRL binding, which increased linearly in a time-dependent manner thereafter. These results indicate that pregnant mice after 11 days are able to initiate synthesis of casein and lactose in parallel. Mammary glands were cultured with insulin, cortisol and PRL. The mammary explants of pregnant mice at 7 and 9 days showed active synthesis of casein after a lag period of 2 days, suggesting that the mammary gland in early pregnancy is less sensitive to PRL, probably due to the absence of an increase in PRL binding after ovariectomy.

Animals↗
PubMed1987

Two separate receptors for prolactin in the rabbit mammary gland.

Rabbit mammary gland PRL receptors in the microsome fraction were solubilized with the zwitterionic detergent Chaps, and were separated into two fractions (Fr. A and B) by ion-exchange chromatography. The number of receptors in Fr. B was about 2.2 times greater than in Fr. A. In sucrose gradient centrifugation analysis, PRL receptors in Fr. A and Fr. B sedimented at different positions. After binding 125I-PRL, the apparent molecular weight (mol wt) of the PRL receptor in Fr. A changed from 42,400 to 65,500 and that in Fr. B changed from 89,400 to 108,000, suggesting that each binding subunit interacts with one PRL molecule. Cross-linking 125I-PRL to receptors revealed little change following SDS-PAGE, in the autoradiogram patterns of the microsome PRL receptors, either in the presence or absence of dithiothreitol. Both the microsome and the Chaps extract contained two major binding subunits (mol wt, 83,200 and 36,800) and one minor subunit (mol wt, 20,800). The mol wt of the dominant PRL receptors in Fr. A and Fr. B were 36,800 and 83,200, respectively. The latter form did not dissociate into a 36,800 mol wt form, suggesting that the rabbit mammary gland contains two independent binding subunits with mol wt of 36,800 and 83,200. Data showed that PRL receptors in the rabbit mammary gland are mostly the high Kd type receptor with a mol wt of 83,200.

Animals↗
PubMed1987

[Epidemiological and therapeutic studies on gonococcal infections--one shot therapy by spectinomycin--[Sapporo Clinical Research Group for STD]].

From January through March of 1985, the Sapporo Clinical Research Group for STD treated 69 cases of gonococcal infections (61 cases of male gonococcal urethritis and 8 cases of female gonococcal cervicitis) at its facilities in Sapporo City. The therapeutic efficacy of one shot therapy of Spectinomycin (SPCM) was investigated, and an epidemiological study on the cases and bacteriological studies on the isolated strains of Neisseria gonorrhoeae were made. The male patients were between 19 and 55 years old, with a peak age distribution in the younger half of the twenties. The female patients were between 18 and 40 years old. The major source of infections was a so-called special massage parlor which accounted for 36.1% of male cases. The isolation rate of PPNG were 16.7% (11/66). The MIC (inoculum size; 10(6) CFU/ml) of SPCM ranged from 3.13 to 25 micrograms/ml regardless of beta-lactamase production. In male patients, the eradication rate (efficacy rate) of N. gonorrhoeae by SPCM was 94.7% on the first day, 93.6% on the third day and 100% on the seventh day after 2 g one shot therapy. In female patients, the rate was 100% on the third and seventh day after 2 g one shot therapy, and 75% on the first day, 66.7% on third day and 100% on seventh day after 4 g one shot therapy. We considered that one shot therapy of SPCM was effective for gonococcal infection also in the present time. Especially SPCM was effective for infections by PPNG, since it was not resolved by beta-lactamase of N. gonorrhoeae. Positive rate of Chlamydia trachomatis was 16.3% in male gonococcal urethritis, and the serous discharge tended to remain longer in the positive patients than in the negative patients. There was only one side effect (1.4%), therefore SPCM was recognized to be a safely administrated antimicrobial agent.

Adult↗
PubMed1987

[Comparative studies on activities of antimicrobial agents against causative organisms isolated from urinary tract infections (1985). II. Background of patients].

We have investigated relationships between patients' backgrounds and isolates from urinary tract infections in reference to various conditions, such as sexes, age distribution by sex, species of causative organisms by sex, age distribution according to species and types of infections, species and infections before and after treatment with antibacterial agents, and species and detected places. As for the relationship between sexes and types of infections, although simple urinary tract infections were consistently found at about 20% in men and at about 80% in women between 1981 and 1983, these infections were seen at 24.4% in men and at 75.6% in women in 1984, and at 26.6% and at 73.4% in 1985, indicating slight decreases in the ratio of women. By contrast, complex urinary tract infections were found in men at about 60-70% from 1981 up to 1985, regardless of the presence or absence of indwelling catheter. There were no noticeable changes according to age during this 5-year period in incidences of infections including simple urinary tract infection and complex urinary tract infection with or without indwelling catheter. Thus, backgrounds of patients with urinary tract infections, including sex, age and simple or complex infections, were fairly consistent throughout this period, while there were relatively large changes in species of isolates. Enterococcus faecalis was isolated at about 8% of both men and women in 1982 and 1983, but its isolation rates were increased to 22.5% of men and 17.9% of women in 1984. In 1985 this species was isolated in 14.9% of men and 7.6% of women, and in 11.2% of all patients. Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus spp. and Enterococcus spp. were detected at rates of 3.2%, 8.1%, 0.7% and 1.0%, respectively, and 24.2% of isolated strains were Gram-positive organisms. When species of isolates before treatment with antibacterial agents and their isolation rates were analyzed, it was found that the isolation rate of E. faecalis increased dramatically in 1983, and that this tendency was still seen in 1984. The isolation rate of Gram-positive organisms was 25% in 1984 and 24.3% in 1985. Escherichia coli was consistently isolated at about 40%, but, as far as simple urinary tract infections are concerned, its isolation rate decreased by about 10% in 1985, compared to 1982 and 1983. These results suggested that causative organisms for simple urinary tract infections became similar to those for complex urinary tract infections. In other words, isolates obtained from complex urinary tract infections before treatment were similar to those of simple infections.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1987

[A case of ureteral polyp in childhood].

A case of ureteral polyp in a 7-year-old boy with the chief complaint of left flank pain was reported. The excretory urogram and retrograde pyelography showed left hydronephrosis and a filling defect at the pelvic-ureteric junction. Partial resection of the ureter containing the lesion and Anderson-Hynes pyeloplasty were performed. The pathological diagnosis was benign polyp of the ureter. Convalescence was uneventful and excretory urogram showed improvement of the hydronephrosis. Along with our case, 19 cases of ureteral polyp in childhood are briefly discussed.

Child↗
PubMed1987

[Comparative studies on activities of antimicrobial agents against causative organisms isolated from urinary tract infections (1985). I. Susceptibility distribution].

The results of determinations of sensitivities of bacterial strains to various antibiotics are summarized as follows: 1. Against Escherichia coli, ofloxacin (OFLX) showed the strongest activity among oral antibacterial and antibiotic agents. Its MIC90 was below 0.10 micrograms/ml. The next strongest activity was found in mecillinam (MPC), cefaclor (CCL) and pipemidic acid (PPA); MIC90's of these agents 3.13 micrograms/ml. Cefotiam (CTM), cefotaxime (CTX), ceftizoxime (CZX), cefmenoxime (CMX) and latamoxef (LMOX) had MIC90 below 0.39 micrograms/ml. MIC90's of cefmetazole (CMZ) and cefoperazone (CPZ) were 1.56 micrograms/ml. Aztreonam (AZT) and carumonam (CRMN) in the monobactam group showed strong activities with MIC90's at 0.20 micrograms/ml. 2. Although Klebsiella pneumoniae had a strong resistance to ampicillin (ABPC) and showed relatively low sensitivities to other oral antibacterial and antibiotic agents, OFLX maintained high activity against this species and showed MIC90 of 0.39 micrograms/ml. Among injectable antibiotics, third generation cephems showed the strongest activity to this species with MIC90 of CZX below 0.10 micrograms/ml, of CTX and CMX 0.20 micrograms/ml, and of LMOX 0.78 micrograms/ml. MIC90 of CPZ was 6.25 micrograms/ml, which was the same as those of cefazolin (CEZ) and cefoxitin (CFX). CTM had similar MIC90 to LMOX, namely, 1.56 micrograms/ml. MIC90 of CMZ was 3.13 micrograms/ml. Monobactams AZT and CRMN showed strong activities to this species; their MIC90's were below 0.10 micrograms/ml and 0.20 micrograms/ml. 3. Although Citrobacter freundii generally exhibited low sensitivities to antibacterial and antibiotic agents examined, it showed high sensitivity to OFLX, at MIC80 of 0.78 micrograms/ml. This species showed low sensitivities to MPC, nalidixic acid (NA), PPA, and sulfamethoxazole-trimethoprim (ST). Among injectable antibiotics, LMOX and CMX had activities against this species; namely, MIC80's were 6.25 and 3.13 micrograms/ml, respectively. Among monobactams, AZT showed MIC80 of 12.5 micrograms/ml, and CRMN had that of 6.25 micrograms/ml. 4. Against Enterobacter cloacae, the strongest antibacterial activity was found with OFLX which had MIC90 of 0.39 micrograms/ml. A relatively strong activity was seen with MPC. MIC80 of MPC was 1.56 micrograms/ml. Except to CTM, this species had poor sensitivities to injectable first and second generation cephems, and their MIC80's were over 200 micrograms/ml. MIC80 of CTM was 25 micrograms/ml.(ABSTRACT TRUNCATED AT 400 WORDS)

Administration, Oral↗
PubMed1987

[Comparative studies on activities of antimicrobial agents against causative organisms isolated from urinary tract infections (1985). III. Secular changes in susceptibility].

Sensitivities to antimicrobial agents of Escherichia coli, Klebsiella spp., Citrobacter spp., Enterobacter spp., Proteus spp., Pseudomonas aeruginosa and Serratia marcescens isolated from infected patients were evaluated and compared according to the types of their infections, i.e., simple and complicated urinary tract infections with or without indwelling catheter. There were no apparent decreases in the sensitivity of E. coli isolated from patients with simple urinary tract infections. When data obtained in 1982-1985 were summarized, it was found that a new quinoline derivative, ofloxacin (OFLX), showed the strongest activity among oral antimicrobial and antibiotic agents. This agent inhibited 100% of bacterial growth at MIC of 1.56 micrograms/ml. The next strongest activity was found with mecillinam (MPC) which showed 89.3% growth inhibition at the same concentration. Cefaclor (CCL) also showed 84.9% growth inhibition at the same concentration. When sensitivities of E. coli isolated from patients with complicated urinary tract infections with or without indwelling catheter to first and second generation cephems were determined, cefotiam (CTM), which inhibited 88.9%: 91.4% bacterial growth at MIC of 0.39 micrograms/ml, had the strongest activity among CTM, cefazolin (CEZ), cefoxitin (CFX) and cefmetazole (CMZ). Among third generation cephems, including cefmenoxime (CMX), latamoxef (LMOX), ceftizoxime (CZX), cefotaxime (CTX) and cefoperazone (CPZ), the strongest activity was observed with CZX, and the agent having the next strongest activity was CMX. LMOX and CPZ showed relatively low activities. Carumonam (CRMN) and aztreonam (AZT), monobactams, showed strong activities against E. coli. As for Klebsiella spp., activities of pencillins against these strains were low. When activities of oral cephems (cephalexin (CEX) and CCL) and of a quinoline derivative OFLX against these strains were determined, OFLX showed strong activity; i.e., the growth of Klebsiella spp. isolated from complicated urinary tract infections was inhibited at 87.2%: 82.1% at MIC of 0.20 micrograms/ml.(ABSTRACT TRUNCATED AT 400 WORDS)

Anti-Bacterial Agents↗
PubMed1987

[A case of lipoma of the spermatic cord].

A recently experienced case of lipoma of the spermatic cord is reported. The patient was a 42-year-old man with the chief complaint of indolent swelling of the left scrotal contents which had been noticed about six months earlier. An elastic firm, nontender and fist-sized mass with negative transillumination was palpated in the left spermatic cord. The tumor was removed and histologically diagnosed as lipoma originating in the left spermatic cord. The removed specimen weighed 72 g and was 8 X 5 X 3 cm. Including the present case, 40 cases of lipoma of the spermatic cord in the Japanese literature are reviewed.

Adult↗
PubMed1987

[The therapeutic effect of norfloxacin on chronic prostatitis].

The clinical efficacy of norfloxacin (NFLX) was evaluated in 74 patients having chronic prostatitis with the subjective symptoms suggesting the inflammations of prostate and more than five white bloodcells (WBCs)/hpf in their prostatic secretions (EPS). Of these, gram negative rods with greater than or equal to 10(3)CFU/ml (GNR group) were isolated from the EPS in 10 patients (13.6%) and gram positive cocci with greater than or equal to 10(3) CFU/ml (GPC group) were obtained in 46 patients (62.2%). E. coli (70.0%) was the most frequent strain isolated among GNR group and S. epidermidis (40.4%), S. aureus (19.1%), E. faecalis (17.0%) and S. haemolyticus (14.9%) were frequently isolated among the GPC group. The overall clinical efficacy of NFLX was determined at the second and fourth week by the three factors, (1) the effect on bacteria, (2) WBCs in the EPS and (3) the subjective symptoms in the patients with bacteria of greater than or equal to 10(3) CFU/ml being isolated. The overall clinical effectiveness rate was 71.4% and 100%, respectively, in the GNR group. In the GPC group, its rate was 79.3% and 88.0%, respectively. The patients with no bacteria or less than 10(3) CFU/ml isolated from the EPS had an overall clinical effectiveness rate of 89.8% at the second week and 90.0% at the fourth, when it was evaluated by the effect on WBCs and subjective symptoms. In the effect of NFLX on bacteria in the EPS, it eliminated them in 75.0% and 83.9% at the second and fourth week, respectively, of all patients with GNR or GPC of greater than or equal to 10(3) CFU/ml isolated from the EPS. The minimum inhibitory concentrations (MIC) of NFLX against E. coli isolated from the EPS was distributed from 0.025 microgram/ml to 3.13 micrograms/ml with most below 0.1 microgram/ml. Those against all other GNR were below 0.78 microgram/ml. NFLX showed good antimicrobial activities against GPC with most of MIC being distributed from 0.78 microgram/ml to 1.56 micrograms/ml. NFLX produced the highest eradication rate in bacteriological response not only against GNR such as 100% at the first, the second and fourth week but GPC as 89.2%, 93.8% and 96.0%, respectively. In the effect of NFLX on WBCs in EPS, 40-50% of patients got free from the inflammation of prostate by NFLX treatment. This became prominent in the GNR group as the treatment was continued although not in the GPC group. The subjective symptoms were improved by NFLX treatment in most of the patients.

Adult↗