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11.
Preclinical Research
This work was performed to assess the effects of intrathecal serotonin 2B (5‐HT2B) receptor antagonists in rats with neuropathic pain. With RS‐127445, its effect was also determined on 5‐HT2B receptor expression. Neuropathic pain was induced by L5/L6 spinal nerve ligation. Western blotting was used to determine 5‐HT2B receptor expression. Dose‐response curves with the 5‐HT2B receptor antagonists 2‐amino‐4‐(4‐fluoronaphth‐1‐yl)‐6‐isopropylpyridine (RS‐127445, 1–100 nmol) and 1‐[(2‐chloro‐3,4‐dimethoxyphenyl)methyl]‐2,3,4,9‐tetrahydro‐6‐methyl‐1H‐pyrido[3,4‐b]indole hydrochloride (LY‐266097, 1–100 nmol) were performed in rats. Tactile allodynia of the left hind paw (ipsilateral) was assessed for 8 h after compound administration. Intrathecal injection of the 5‐HT2B receptor antagonists RS‐127445 and LY‐266097 diminished spinal nerve ligation‐induced allodynia. In contrast, intrathecal injection of the 5‐HT2 receptor agonist (±)‐2,5‐dimethoxy‐4‐iodoamphetamine hydrochloride (DOI, 10 nmol) did not modify tactile allodynia induced by nerve ligation. L5/L6 nerve ligation increased expression of the 5‐HT2B receptors in the ipsilateral, but not contralateral, dorsal root ganglia. Furthermore, nerve injury also enhanced 5‐HT2B receptor expression in the ipsilateral dorsal part of the spinal cord. Intrathecal treatment with RS‐127445 (100 nmol) diminished spinal nerve injury‐induced increased expression of 5‐HT2B receptors in dorsal root ganglia and spinal cord. Our results imply that spinal 5‐HT2B receptors are present on sites related to nociception and participate in neuropathic pain. © 2014 Wiley Periodicals, Inc Drug Dev Res 76 : 31–39, 2015  相似文献   
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The aim of this study was to evaluate the susceptibility of 20 clinical isolates of Fusarium spp. to classic antifungals [amphotericin B (AmB), itraconazole (ITR), voriconazole (VRC) and caspofungin (CAS)] and to non-antifungal agents [amiodarone (AMD), doxycycline (DOX) and moxifloxacin (MFX)] by the broth microdilution method. Combinations between these antifungal and non-antifungal agents were also evaluated to determine the fractional inhibitory concentration indices using the chequerboard technique. Synergistic interactions were observed for the following combinations (% synergism): AMD?+?VRC, 80%; MFX?+?AmB, 75%; AMD?+?AmB, 65%; DOX?+?VRC, 60%; MFX?+?VRC, 55%; DOX?+?AmB, 50%; and AMD?+?CAS, 30%. Synergism was not observed for associations with ITR. Antagonism was not seen in any combination. These findings suggest that the combinations of AMD, DOX or MFX with AmB or VRC to have potential for future in vivo investigations.  相似文献   
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目的探究mCD99L2基因沉默对小鼠B淋巴瘤细胞系A20细胞转化为H/RS样细胞的影响。方法重组SiRNA表达质粒LV-mCD99L2,体外转染内源性mCD99L2表达阳性的A20细胞,筛选出稳定表达LV质粒的细胞株并扩增培养;采用免疫荧光技术和流式细胞仪检测转化前后两组细胞鼠源CD30表达;透射电镜观察转化后细胞超微结构的形态特点;细胞计数方法动态观测培养细胞干扰组A20-LV-mCD99L2和未经干扰组A20细胞的H/RS样细胞(直径≥25μm)转型率,以人霍奇金淋巴瘤细胞系L428作为对照;采用流式细胞仪检测细胞周期变化。结果获得了稳定表达LV质粒的单克隆细胞株A20-LV-mCD99L2;免疫荧光标记显示转化细胞CD30( );流式细胞仪检测A20-LV-mCD99L2细胞CD30阳性率为54.4%;透射电镜观察转化后细胞核增大,可见单核、双核及多核,核仁明显的H/RS样细胞;干扰组H/RS样细胞的转型率明显高于未经干扰组(P<0.01)。两组处于S期的细胞无明显差异,两组细胞均未见凋亡峰。结论mCD99L2基因沉默可诱导小鼠B淋巴瘤细胞系A20细胞转化为H/RS样细胞。  相似文献   
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Jia W  Qiu M  Sun X  Qiu Y  Su M 《Advances in therapy》2004,21(4):238-246
During the process of developing a slow-release formulation of indapamide, researchers created a drug-containing pellet coated with Eudragit RS100 (Rohm GMbH & Co. KG, Darmstadt, Germany) to control the rate at which the drug was released. The two main variables were the agglomerants used in the pellet preparation and the amount of Eudragit RS100 used to coat them. The optimal outcome was indicated by the greatest number of drug-containing pellets recovered through an 18- to 24-mesh sieve and a satisfactory 24-hour release curve. The kinetics of dissolution fit the Higuchi kinetics model. Stability tests of the drug pellets showed no notable changes in the rate of drug release, related substances (mean byproducts or impurities from interactions or decompositions), and drug content.  相似文献   
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Objective

This study examined if ongoing support delivered by telephone following pulmonary rehabilitation (PR) assisted chronic obstructive pulmonary disease (COPD) patients to maintain health outcomes.

Methods

Phase one (n = 79) compared post-rehabilitation telephone-based support delivered by peers compared to usual care (UC). The second phase (n = 168) compared post-rehabilitation support from peer educators, respiratory therapists (RT), or UC. Primary outcome variables were St. George's Respiratory Questionnaire (SGRQ) total score and the six minute walk test (6MWT). Measures were obtained at baseline, immediately following PR, and six-months post PR.

Results

Six-month follow-up data for phase one was collected for 66 COPD patients (n = 35 peer support, n = 31 UC) and 142 for phase two (n = 42 peer support, n = 52 RT support, n = 48 UC). Per-protocol and intention to treat (ITT) analysis in both phases found no significant group by time differences for SGRQ or 6MWT.

Conclusion

Providing peer or RT support via telephone following PR was not more effective than UC for maintaining health outcomes.

Practice implications

There are concerns with using peers to provide ongoing support to COPD patients. Additionally, COPD patients require a higher level of care than telephone support can provide.  相似文献   
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