检索结果-内蒙古大学图书馆

Dose-dependent effects of recombinant human interleukin-11 on contractile properties in rabbit 2,4,6-trinitrobenzene sulfonic acid colitis

引用

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS 2000年第3期294卷 983-990页

作者： Depoortere, I Thijs, T Van Assche, G Keith, JC Peeters, TL Univ Leuven Dept Pathophysiol Ctr Gastroenterol Res Louvain Belgium Genet Inst Inc Andover MA USA

We studied the effect of recombinant human interleukin-11 (rhIL-11), a cytokine with protective effects against injury to the intestinal mucosa, on inflammatory changes in the muscle layers of the gut, in rabbits with colitis. A single dose of rhIL-11 (4, 40, or 720 mu g/kg) was given 1 h before colitis was induced with 135 mg/kg 2,4,6-trinitrobenzene sulfonic acid (TNBS), followed by a continuous s.c. administration of 4, 40, or 720 mu g/kg . day rhIL-11 or saline for 5 days. Colitis affected mucosal architecture, general mechanical properties (passive tension increased with 12.3 g/mm(2), optimal stretch decreased with 26%), and collagen content (decreased from 366 +/- 25 to 237 +/- 13 mu g/mg of protein). Changes in passive tension and collagen content were normalized by the highest and lowest dose of rhIL-11, respectively, but neither dose could normalize the optimal stretch. Colitis also decreased maximal contractile tension in response to acetylcholine (ACh), motilin, substance P (SP), K+, and prostaglandin E-2 but this was normalized with 40 mu g/ kg day (motilin, SP) and 720 mu g/kg . day (ACh, K+) rhIL-11 but not for prostaglandin E-2. For motilin and SP, receptor density was decreased in colitis and normalized in treated rabbits. Colitis also increased the contractile potency toward ACh, an effect already reversed by rhIL-11, 4 mu g/kg . day. In conclusion, rhIL-11 partially normalizes disturbed tension generation in experimental colitis. The use of this cytokine in the treatment of irritable bowel disease may contribute to the restoration of motor dysfunction.

关键词：乙酰胆碱/药理学结肠炎/化学诱导结肠炎/病理学结肠炎/病理生理学结肠/药物作用结肠/病理学结肠/病理生理学地诺前列酮/药理学剂量效应关系药物白细胞介素11/药理学促胃动素/药理学肌收缩/药物作用肌平滑/药物作用氯化钾/药理学受体胃肠激素/代谢受体神经激肽1/代谢受体神经肽/代谢重组蛋白质类/药理学逆转录聚合酶链反应 P物质/药理学拉伸强度三硝基苯磺酸动物女(雌)性男(雄)性兔

来源：评论

学校读者我要写书评

暂无评论

Visceral pain.

引用

Current review of pain 2000年第6期4卷 499-506页

作者： Joshi, S.K. Gebhart, G.F. Department of Pharmacology The University of Iowa College of Medicine 2-302 Bowen Science Building Iowa City 52242 IA United States

Visceral pain, although different from somatic pain in several important features, is not as widely researched and consequently our knowledge of neurophysiologic mechanisms as well as clinical management of visceral pain states remains unsatisfactory. Several recent studies have employed different visceral pain animal models to provide insight into the peripheral and central nervous system mechanisms underlying pain originating from the urinary bladder, ureter, and gastrointestinal tract. The effects of opioid and nonopioid drugs in these models have also been evaluated and are reviewed in this article. The importance of anatomic pathways relaying pain sensation in the central nervous system, particularly the newly described dorsal column pathway, is also discussed. In human subjects, new techniques like positron emission tomography are now being used to better understand visceral pain perception. Such findings deriving from basic animal research and human studies summarized in the present overview lead to a better understanding of visceral pain states and may be helpful in developing better treatment strategies to combat visceral pain states in the clinical setting.

关键词：传入通路/病理学传入通路/病理生理学脑/病理学脑/病理生理学消化系统/神经支配消化系统/病理学消化系统/病理生理学疾病模型动物疼痛感受器/药物作用疼痛感受器/代谢疼痛/病理学疼痛/病理生理学受体神经肽/药物作用受体神经肽/代谢输尿管/神经支配输尿管/病理学输尿管/病理生理学膀胱/神经支配膀胱/病理学膀胱/病理生理学内脏/神经支配内脏/病理学内脏/病理生理学内脏传入神经/病理学内脏传入神经/病理生理学动物人类

来源：评论

学校读者我要写书评

暂无评论

2,3-dihydro-dithiin and -dithiepine-1,1,4,4-tetroxides: Small molecule non-peptide antagonists of the human galanin hGAL-1 receptor

引用

BIOORGANIC & MEDICINAL CHEMISTRY 2000年第6期8卷 1383-1391页

作者： Scott, MK Ross, TM Lee, DHS Wang, HY Shank, RP Wild, KD Davis, CB Crooke, JJ Potocki, AC Reitz, AB RW Johnson Pharmaceut Res Inst Drug Discovery Div Spring House PA 19447 USA

The neuropeptide galanin modulates several physiological functions such as cognition, learning, feeding behavior, and depression, probably via the galanin 1 receptor(GAL-R1). Using an HTS assay based on I-125-human galanin binding to the human galanin-l receptor (hGAL-R1), we discovered a series of 1,4-dithiin and dithiipine-1,1,4,4-tetroxides that exhibited binding affinity IC50's to hGAL-R1 ranging from 190 to 2700 nM. Two of the dithiepin analogues, 7 and 23, behaved pharmacologically as hGAL-R1 antagonists in secondary assays involving adenylate cyclase activity and GTP binding to G-proteins. Analogues 7 and 23 were also active in functional assays involving galanin, reversing the inhibitory effect of galanin on acetylcholine (ACh) release in rat brain hippocampal slices and electrically-stimulated guinea pig ileum twitch. (C) 2000 Elsevier Science Ltd. All rights reserved.

关键词：乙酰胆碱/代谢氨基酸序列加兰肽/化学加兰肽/代谢海马/药物作用海马/代谢回肠/药物作用回肠/生理学黑色素瘤/病理学分子序列数据受体甘丙肽受体神经肽/拮抗剂和抑制剂受体神经肽/代谢构效关系硫|艹卓|类/化学硫|艹卓|类/药理学肿瘤细胞培养的动物豚鼠人类男(雄)性大鼠

来源：评论

学校读者我要写书评

暂无评论

Anatomical distribution of prolactin-releasing peptide and its receptor suggests additional functions in the central nervous system and periphery

引用

ENDOCRINOLOGY 1999年第12期140卷 5736-5745页

作者： Roland, BL Sutton, SW Wilson, AJ Luo, L Pyati, J Huvar, R Erlander, MG Lovenberg, TW RW Johnson Pharmaceut Res Inst San Diego CA 92121 USA

A recently identified neuropeptide with PRL-releasing capabilities binds to and activates a previously known orphan G protein-coupled receptor, GPR10. We initiated a study to define the pharmacology of the peptide/receptor interaction and to identify the distribution of the peptide and its receptor in the central nervous system to elucidate sites of action of the peptide. The PRL-releasing peptide (PrRP) is a C-terminally amidated, 31-amino acid peptide derived from a 98-amino acid precursor. Radioiodinated PrRP-(1-31) binds to its receptor with high affinity (1 nM) and stimulates calcium mobilization in CHOK1 cells stably transfected with the receptor. A series of N-terminal deletions reveals that the PrRP-(12-31) amino acid is equipotent to PrRP-(1-31). Further N-terminal deletions reduce the affinity of the ligand considerably, although PrRP-(25-31) is still able to compete for binding and behaves as an agonist. The arginine residues at position 26 and 30 are critical for binding, as substitution with either lysine or citrulline reduces the affinity substantially. In situ hybridization reveals a distinct tissue distribution for both the peptide and receptor messenger RNAs. The receptor is expressed abundantly in the reticular thalamic nucleus, periventricular hypothalamus, dorsomedial hypothalamus, nucleus of the solitary tract, area postrema, anterior pituitary, and adrenal medulla. The peptide messenger RNA is expressed in the dorsomedial hypothalamus, nucleus of the solitary tract, ventrolateral reticular nucleus, and intestine. This tissue distribution suggests an alternative function of PrRP than its purported hypophysiotropic function, such as a potential role for PrRP in the central feedback control of neuroendocrine and autonomic homeostasis. Further work using selective agonists and antagonists should help define additional physiological roles of this novel mammalian neuropeptide.

关键词：脑/代谢脑化学 CHO细胞中枢神经系统/化学仓鼠亚科基因表达下丘脑激素类/分析下丘脑激素类/遗传学下丘脑激素类/代谢原位杂交碘放射性同位素神经肽类/分析神经肽类/遗传学神经肽类/代谢 RNA 信使/分析大鼠 Sprague-Dawley 受体神经肽/分析受体神经肽/遗传学受体神经肽/代谢丘脑核/化学促甲状腺素释放激素/遗传学组织分布转染酪氨酸单氧化酶/分析动物男(雄)性大鼠

来源：评论

学校读者我要写书评

暂无评论

Nicotine up-regulates expression of orexin and its receptors in rat brain

引用

ENDOCRINOLOGY 2000年第10期141卷 3623-3629页

作者： Kane, JK Parker, SL Matta, SG Fu, Y Sharp, BM Li, MD Univ Tennessee Dept Pharmacol Coll Med Memphis TN 38163 USA

Orexins are two recently discovered neuropeptides that can stimulate food intake. As the chronic use of tobacco typically leads to a reduction in body weight, it is of interest to determine whether nicotine, the major biologically active tobacco ingredient, has an effect on orexin metabolism in the brain. Using a semiquantitative RT-PCR technique, the levels of messenger RNA (mRNA) for prepro-orexin, orexin A (OX1-R) and orexin B (OX2-R) receptors were 20-50% higher in rats receiving nicotine for 14 days at the level of 2-4 mg/kg day compared with rats receiving saline solvent alone. In animals treated with nicotine at 4 mg/kg-day, the expression levels of mRNA for prepro-orexin, OX1-R, and OX2-R were significantly higher compared with those in either the free-feeding control or pair-fed saline control rats. RIA data indicated that both orexin A and orexin B peptide levels were significantly elevated (45-54%;P < 0.01) in the dorsomedial nucleus (DMH) of the nicotine-treated rats compared with either solvent-only or pair-fed controls. Additionally, orexin B was significantly elevated (83%;P < 0.01), over levels in both types of the control animals, in the paraventricular nucleus (PVN) region. In summary, we demonstrated that an inverse association between nicotine and food intake as well as body weight held with doses comparable to those consumed by average human smokers. Moreover, our data indicated that chronic exposure to nicotine can induce a long-term increase in the expression levels of prepro-orexin and their receptor mRNA in the rat hypothalamus and in the levels of orexin A in the DMH and orexin B in the DMH and PVN among the six hypothalamic regions that we examined.

关键词：体重/药物作用脑/代谢载体蛋白质类/遗传学载体蛋白质类/代谢剂量效应关系药物进食/药物作用下丘脑/代谢细胞内信号肽和蛋白质类神经肽类/遗传学神经肽类/代谢尼古丁/药理学蛋白质前体/遗传学 RNA 信使/代谢大鼠近交系大鼠 Sprague-Dawley 受体 G-蛋白偶联受体神经肽/遗传学受体神经肽/代谢组织分布增量调节动物男(雄)性大鼠

来源：评论

学校读者我要写书评

暂无评论

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

请选择保存的检索档案：

请选择收藏分类：

通借通还

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：