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41.
Binding profile of SM-9018, a novel antipsychotic candidate 总被引:3,自引:0,他引:3
T Kato A Hirose Y Ohno H Shimizu H Tanaka M Nakamura 《Japanese journal of pharmacology》1990,54(4):478-481
The present study employed various receptor-binding assays to clarify the biochemical characteristics of SM-9018. SM-9018 possessed very high affinity for 5-HT2, D2 and 5-HT1A receptors (Ki = 0.61, 1.4 and 2.9 nM, respectively), and it had moderate affinity for alpha 1 and D1 receptors (Ki = 17 and 41 nM, respectively). However, SM-9018 had only negligible affinity for alpha 2, opiate, glutamate, phencyclidine, benzodiazepine and GABAA receptors. These results suggest that SM-9018 may be a novel antipsychotic agent with binding affinity for 5-HT2 and 5-HT1A receptors. 相似文献
42.
43.
Tsuyoshi Takeda Hiroyuki Ishida Yukio Horiuchi Yasushi Nakao Yutaka Yabe 《Journal of orthopaedic science》1997,2(6):372-377
We examined radiographs of the elbows of the pitching arms of 79 professional baseball pitchers (mean age, 25.1 years; mean
duration of professional career, 4.7 years) and noted the frequency and size of spurs, bone fragments, and intra-articular
loose bodies according to site. The influence of duration of professional baseball career on these osteoarthritic changes
was also investigated. The olecranon tip was the most frequent site of spurs (62/79; 78.5%), and fragmentation of the spur
was detected in 17 joints. The frequency of spurs was also high at the medial margin of the olecranon, the tip of the coronoid
process, the medial margin of the sigmoid notch, the medial margin of the trochlea and the olecranon fossa. In 38 subjects,
spurs were observed at the distal portion of the radial notch of the ulna. However, few pitchers had osteoarthritic changes
in the humeral capitellum or radial head. Intra-articular loose bodies were detected in 4 of 79 joints (5.1%), and bone fragments
were present below the medial humeral epicondyle in 25 of 79 joints (31.6%). Osteoarthritic changes in the elbow joint appeared
to be attributable mainly to traction stress and impingement associated with extension and valgus strain. Significant osteoarthritic
changes were often found in professional pitchers whose careers exceeded 5 years. 相似文献
44.
Kodama Hideya; Fukuda Jun; Karube Hiroko; Matsui Toshihiko; Shimizu Yasushi; Tanaka Toshinobu 《Human reproduction (Oxford, England)》1995,10(8):1962-1967
This study was aimed at assessing the outcome of in-vitro fertilization(IVF) and embryo transfer in patients with polycystic ovariansyndrome (PCOS). The results of IVF and embryo transfer in PCOSpatients (PCOS group, 78 cycles of 26 patients) were comparedwith those of a control group (423 cycles in 202 patients withoutmale factor; age and ovarian stimulation protocol were matched).Although the pregnancy rate per transfer was not different inthe two groups of patients (25 versus 34%, PCOS versus controlgroup), the PCOS group had a significantly lower pregnancy rateper follicle aspiration (19 versus 31%, P < 0.05). A notableresult was a significantly higher incidence of embryo transfercancellations in the PCOS group (22 versus 8%, P < 0.01),which resulted from unpredictable failure of either oocyte recoveryor fertilization. The incidence of unexplained complete failureof fertilization was significantly higher in the PCOS group(18 versus 5%, P < 0.01). These results may reflect a reducedquality of the oocytes in the PCOS group, and there was a subgroupof PCOS patients who repeatedly produced poor results of treatment.Although the ovarian stimulation regimen best suited to PCOSpatients remains to be determined, special care should be takenduring ovarian stimulation, especially when the PCOS patientshad experienced unexplained failure of oocyte recovery or fertilizationin the previous treatment cycle(s). 相似文献
45.
The authors applied combined depth and subdural electrodes in patients with intractable complex partial seizures to detect the precise extent of epileptic foci and functionally map speech-related areas. The medial temporal structures were explored with depth electrodes and the lateral temporal cortex with subdural electrodes. On the speech-dominant side, electrical stimulation was given to demarcate the speech-related areas in the lateral temporal cortex. Based on these data, the extent of surgical resections was tailored to include as much of the epileptogenic areas as possible while preserving the functionally essential zones of the lateral cortex. According to the range of resection, three different approaches were employed for en bloc ablation of the lateral cortex and opening of the inferior ventricle. The results thus acquired have been satisfactory in terms of seizure control and the preservation of speech function. 相似文献
46.
The effect of dietary manipulation on global tooth uptake of 47Ca-chloride was evaluated in three rat models of metabolic bone diseases verified by histologic bone study. The 24-hr tooth uptake of 47Ca-chloride was significantly decreased in the osteomalacic group, and was increased in the osteoporotic group at the fourth week. Tooth uptake closely paralleled femoral uptake at a correlation coefficient of 0.73 (p less than 0.01). The uptake of 47Ca-chloride in tooth was found to be more affected by dietary manipulation than that in femur in our rat models. 相似文献
47.
Hiroyuki Yamamoto Fumio Itoh Akinori Senota Yasushi Adachi Mitsuru Yoshimoto Takao Endoh Yuji Hinoda Akira Yachi Kohzoh Imai 《Journal of clinical laboratory analysis》1995,9(5):297-301
The matrix metalloproteinase matrilysin (MMP-7) is a member of the matrix metallo-proteinase gene family, which is believed to play an important role in tumor invasion and metastasis. We have previously found that matrilysin mRNA is specifically expressed in colorectal cancers and adenomas and that its message is localized in the tumor cells themselves. We examined the effects of activated Ki-ras oncogene on the expression of matrilysin in colon cancer cells. We showed that both mRNA and the enzymatic activity of matrilysin were induced by the introduction of activated Ki-ras into SW1417 colon cancer cells. To understand the mechanisms regulating this induction, we analyzed alterations of AP-1 activity induced by activated Ki-ras, using the chloramphenicol acetyltransferase assay. AP-1 activity in SW1417 cells expressing activated Ki-ras was higher than that in control cells. The gel-shift assay also showed higher levels of AP-1 binding protein in SW1417 cells expressing activated Ki-ras than those in control cells. Our results suggest that activated Ki-ras may play a role in inducing expression of matrilysin through an AP-1-dependent pathway in colon cancer cells. 相似文献
48.
49.
Protective effect of prostaglandins D2, E1 and I2 against cerebral hypoxia/anoxia in mice 总被引:3,自引:0,他引:3
Yoshinobu Masuda Yuko Ochi Yoshiaki Ochi Tadahiko Karasawa Naonobu Hatano Toshiaki Kadokawa Masanao Shimizu 《Naunyn-Schmiedeberg's archives of pharmacology》1986,334(3):282-289
The protective effect of prostaglandins (PGs) against cerebral hypoxia/anoxia was investigated with a variety of experimental models in relation to their CNS depressant effects in mice. Furthermore, the effect of PGs on the changes of cerebral energy metabolites and cyclic nucleotide was examined in hypoxic mice. Mice were given s.c. doses of PGs 30 min before tests. Among the PGs tested, treatment with PGD2, PGE1 and PGI2 Na showed a consistent and dose-dependent protection against cerebral anoxia induced by all models studied: histotoxic anoxia by KCN, hypobaric hypoxia, normobaric hypoxia and decapitation-induced gasping. However, PGA1, PGA2, PGB1, PGB2, PGE2, PGF1 alpha, PGF2 alpha and 6-keto-PGF1 alpha at a dose of 3 mg/kg were without effect against normobaric hypoxia and gasping duration. The three PGs, i.e. PGD2, PGE1 and PGI2 which showed anti-hypoxic effects decreased locomotor activity and potentiated hexobarbital-induced sleep. On the other hand, PGE2, PGA1, PGA2 and PGB2 also caused a decrease in locomotor activity. Similarly, PGE2 and PGA1 caused a potentiation of hexobarbital-induced sleep, but interestingly they did not cause clear-cut increase in cerebral resistance to hypoxia, in contrast with the former three PGs. Thus general depression of CNS function appears not to be responsible for the PGD2-, PGE1- and PGI2-induced increase in cerebral resistance to hypoxia. The levels of Cr-P and ATP were significantly reduced and those of ADP and AMP were markedly elevated in hypoxic brain, resulting in a decrease in a calculated energy charge potential. The lactate level and lactate/pyruvate ratio increased and the glucose level decreased markedly.(ABSTRACT TRUNCATED AT 250 WORDS) 相似文献
50.