排序方式: 共有22条查询结果,搜索用时 359 毫秒
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Christina B. Madsen-Duggan John S. Debenham Thomas F. Walsh Lin Yan Pei Huo Junying Wang Xinchun Tong Julie Lao Tung M. Fong Jing Chen Xiao Cathy R.-R.C. Huang Chun-Pyn Shen D.Sloan Stribling Lauren P. Shearman Alison M. Strack Mark T. Goulet Jeffrey J. Hale 《Bioorganic & medicinal chemistry letters》2010,20(12):3750-3754
Synthesis and structure–activity relationships of cannabinoid-1 receptor (CB1R) inverse agonists based on dihydro-pyrano[2,3-b] pyridine and tetrahydro-1,8-naphtyridine scaffolds are presented. Rat food intake and pharmacokinetic evaluation of 13g, 13i, 13k and 17a revealed these compounds to be highly efficacious orally active modulators of CB1R. 相似文献
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R Moriggi Jr HS Di Mauro SC Dias JM Matos MB Urtado NF Camar?o IV Sousa Neto DC Nascimento RA Tibana CO Assump??o J Prestes CB Urtado 《Biology of sport / Institute of Sport》2015,32(4):289-294
Low intensity resistance exercise (RE) with blood flow restriction (BFR) has gained attention in the literature due to the beneficial effects on functional and morphological variables, similar to those observed during traditional RE without BFR, while the effects of BFR on post-exercise hypotension remain unclear. The aim of the present study was to compare the blood pressure (BP) response of trained normotensive individuals to RE with and without BFR. In this cross-over randomized trial, eight male subjects (23.8 ± 4 years, 74 ± 3 kg, 174 ± 4 cm) completed two exercise protocols: traditional RE (3 x 10 repetitions at 70% one-repetition maximum [1-RM]) and low intensity RE (3 x 15 repetitions at 20% 1-RM) with BFR. Blood pressure measurements were performed after 15 min of seated rest (0), immediately after and 10 min, 20 min, 30 min, 40 min, 50 min and 60 min after the experimental sessions. Similar hypotensive effects for systolic BP (SBP) were observed for both protocols (P < 0.05) after exercise, with no differences between groups (P > 0.05) and no statistically significant difference for diastolic BP (P > 0.05). These results suggest that in normotensive trained individuals, both traditional RE and RE with BFR induce hypotension for SBP, which is important to prevent cardiovascular disturbances. 相似文献
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John S. Debenham Christina B. Madsen-Duggan Junying Wang Xinchun Tong Julie Lao Tung M. Fong Marie-Therese Schaeffer Jing Chen Xiao Cathy C.R.-R. Huang Chun-Pyn Shen D. Sloan Stribling Lauren P. Shearman Alison M. Strack D. Euan MacIntyre Jeffrey J. Hale Thomas F. Walsh 《Bioorganic & medicinal chemistry letters》2009,19(9):2591-2594
The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R. 相似文献
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John S. Debenham Thomas H. Graham Andreas Verras Yong Zhang Matthew J. Clements Jeffrey T. Kuethe Christina Madsen-Duggan Wensheng Liu Urmi R. Bhatt Dunlu Chen Qing Chen Margarita Garcia-Calvo Wayne M. Geissler Huaibing He Xiaohua Li JeanMarie Lisnock Zhu Shen Xinchun Tong Dong-Ming Shen 《Bioorganic & medicinal chemistry letters》2013,23(23):6228-6233
The synthesis, SAR, binding affinities and pharmacokinetic profiles are described for a series of cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors discovered by high throughput screening. Compounds show high levels of ex vivo target engagement in mouse plasma 20 h post oral dose. 相似文献
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Madsen-Duggan CB Debenham JS Walsh TF Toupence RB Huang SX Wang J Tong X Lao J Fong TM Schaeffer MT Xiao JC Huang CR Shen CP Stribling DS Shearman LP Strack AM MacIntyre DE Van der Ploeg LH Goulet MT 《Bioorganic & medicinal chemistry letters》2007,17(7):2031-2035
Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1. 相似文献
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Although chemotherapy with procarbazine, lomustine and vincristine (PCV) is considered to be well tolerated, side effects
frequently lead to dose reduction or even discontinuation of treatment of oligodendroglial brain tumors. The primary objective
of the analysis was to retrospectively compare progression-free survival (PFS) after PCV vs. PC chemotherapy (without vincristine
to avoid side effects). Patients were retrospectively identified from a database containing our patients between 1990 and
2003. For the selected cases, all histopathology reports were re-evaluated by a local neuropathologist. Based on the updated
histology data, patients were included in the study if they had at least one histological diagnosis of an oligodendroglial
tumor. PFS after start of PCV (n = 61) and PC (n = 84) chemotherapy identical (median 30 months). Multivariate analysis adjusting
for prognostic imbalances favouring the PC group showed a minor, statistically non-significant benefit for PCV (hazard ratio
0.81, 95% confidence interval 0.53–1.25; p = 0.346). Younger age (< 50 y) was a statistically significant predictor of longer
PFS. Significant advantages in terms of overall survival after first diagnosis of oligodendroglial tumor (OS, n = 315) were
found for patients < 50 y (p < 0.001), oligodendrogliomas versus oligoastrocytomas (p = 0.002), and WHO°II vs. °III (p < 0.001).
Three risk groups regarding OS were identified. Findings support the hypothesis that PC may be as effective as PCV chemotherapy,
while avoiding the additonal risks of vincristine. Younger age, lower tumor grade and histology of an oligodendroglioma were
identified to be favorable prognostic factors. 相似文献