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51.
R Wrigglesworth CS Walpole S Bevan EA Campbell A Dray GA Hughes I James KJ Masdin J Winter 《Canadian Metallurgical Quarterly》1996,39(25):4942-4951
Structural features of three regions of the capsaicin molecule necessary for agonist properties were delineated by a previously reported modular approach. These in vitro agonist effects were shown to correlate with analgesic potency in rodent models. Combination of optimal structural features from each of these regions of the capsaicin molecule have led to highly potent agonists (eg., 1b). Evaluation in vivo established that 1b had analgesic properties but poor oral activity, short duration of action, and excitatory side effects which precluded further development of this compound. Preliminary metabolism studies had shown that the phenol moiety of 1b was rapidly glucuronidated in vivo, providing a possible explanation for the poor pharmacokinetic profile. Subsequent specific modification of the phenol group led to compounds 2a-j, which retained in vitro potency. The in vivo profiles of two representatives of this series, 2a,h, were much improved over the "parent" phenol series, and they are candidates for development as analgesic agents. 相似文献
52.
CS Walpole R Wrigglesworth S Bevan EA Campbell A Dray IF James KJ Masdin MN Perkins J Winter 《Canadian Metallurgical Quarterly》1993,36(16):2381-2389
Structural variants of the hydrophobic side chain ("C region") of the capsaicin molecule have been incorporated into a series of vanillylamides and vanillylthioureas. These compounds have been tested in an in vitro assay for agonism (45Ca2+ influx into dorsal root ganglia neurones), previously shown to be predictive of analgesic activity. The results of this study have established the requirement for a hydrophobic substituent of limited size (molar refractivity, MR, < 55) in order to obtain high potency. Combination of the information gained here about the "C-region" of the capsaicin molecule with the studies described in the preceding two papers provides a rational basis for the design of compounds of increased potency. 相似文献
53.
MA Bloomberg HS Jordan KO Angel MH Bailit KJ Goonan J Straus 《Canadian Metallurgical Quarterly》1993,19(12):586-595
This article describes a collaborative effort between a major health care purchaser, three area health maintenance organizations, and a state Medicaid agency to develop clinical indicators as the basis for a comparison database. Some of the difficulties in developing a "common yardstick" of quality and value are candidly discussed. 相似文献
54.
GG Stone MM Chengappa RD Oberst NH Gabbert S McVey KJ Hennessy M Muenzenberger J Staats 《Canadian Metallurgical Quarterly》1993,5(3):378-385
The polymerase chain reaction was employed to correlate Salmonella serovars isolated from fecal material of greyhounds suffering from gastroenteritis with those isolated from the diet fed to the greyhounds prior to onset of diarrhea. Kennels around the Abilene, Kansas, area were contacted and supplied with materials needed to collect a portion of the diet each day. With the onset of diarrhea, the kennels were instructed to ship the fecal material and diet from the previous 10 days to the laboratory for testing. Forty-one fecal samples and corresponding diets were screened for Salmonella, Clostridium perfringens, Campylobacter jejuni, Staphylococcus aureus, Staphylococcus intermedius, and pathogenic (piliated) Escherichia coli by direct culture using standard procedures. The fecal material was also screened for coronavirus and parvovirus using electron microscopy. Thirty-five "normal" fecal samples were screened for all of the above mentioned microorganisms as a control. In addition, the fecal material was screened for E. coli verotoxins I and II and clostridial enterotoxins. A total of 61 Salmonella isolates were recovered from the 41 samples of feces and diet submitted for testing; 31 were recovered from the feces and 30 from the diet. Four Salmonella isolates were recovered from the normal fecal samples. Results obtained by PCR, plasmid profiles, antigenic analysis, and antibiogram profiles indicated that 16 of the 31 isolates recovered from the fecal material were the same strain as that recovered from the diet. 相似文献
55.
Skin tests on patients suffering from pollinosis suggest frequently an antigenic relationship between various grass and cult. rye pollens. This problem was further studied using both, RAST and RAST inhibition test. The tests were performed with commercial grass pollen discs as well as with self-prepared disc labeled with cult. rye pollens and a combination of various grass antigens. Good agreement was found between self-made and commercial (single antigen) grass pollen discs (95.9%). RAST and skin test correlated also extremely well (92.3%). Mutual inhibition between grass and cult. rye pollens was measured by RAST inhibition test using self-prepared discs. High antigenic relationship between grass and cult. rye pollens was found, however, it could be demonstrated that the antibody pattern varies and contains "grass specific" antibodies. 相似文献
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This paper presents some of the theoretical predictions and experimental results for the steady-state characteristics of a gas-lubricated, pivoted-pad journal bearing of finite length. An analytical expression for the prediction of load-carrying capacity for these bearings is developed from numerical computer solutions. Sample calculations are presented to show how the theoretical data may be utilized in the design of an actual pivoted-pad bearing. Improvements over previous approximate theories are discussed. 相似文献
59.
W.KJ 《军民两用技术与产品》2014,(8):4-4
6月6日,中央全面深化改革领导小组第三次会议召开,会议审议通过了“关于设立知识产权法院的方案》等方案。 相似文献
60.