Abstract:
:The evaluation of a group of polyamine analogs as agents to ameliorate diarrhea-predominant irritable bowel syndrome is described. Each compound was assessed when administered subcutaneously in a psychological stress-induced model of irritable bowel syndrome in rodents for its ability to reduce stool output in a dose-dependent manner. The spermine pharmacophore is shown to be an excellent platform from which to construct compounds to treat irritable bowel syndrome. The activity of the compounds is very dependent on both the nature of the terminal alkyl groups and the geometry of the methylene spacers separating the nitrogens. In addition to the subcutaneous studies, several compounds, N1,N11-diethylnorspermine, N1,N12-diethylspermine, N1,N12-diisopropylspermine, N1,N14-diethylhomospermine, N,N'-bis[5-(ethylamino)pentyl]-1,4-butanediamine, N,N'-bis[2-(4-piperidinyl)ethyl]-1,4-diaminobutane, and N,N'-bis[3-(ethylamino)propyl]-trans-1,4-cyclohexanediamine, were subsequently evaluated for oral efficacy. The remarkable activity of N,N'-bis[3-(ethylamino)propyl]-trans-1,4-cyclohexanediamine underscores the need to explore this framework further as a pharmacophore for the construction of other analogues to relieve the symptoms of diarrhea-predominant IBS.
journal_name
Dig Dis Scijournal_title
Digestive diseases and sciencesauthors
Bergeron RJ,Wiegand J,Fannin TLdoi
10.1023/a:1012750723644subject
Has Abstractpub_date
2001-12-01 00:00:00pages
2615-23issue
12eissn
0163-2116issn
1573-2568journal_volume
46pub_type
杂志文章abstract:BACKGROUND:Lymphocytic esophagitis is a rare esophageal condition. Our knowledge of potential risk factors and treatment outcomes of lymphocytic esophagitis is limited. AIM:To investigate potential risk factors associated with the development of lymphocytic esophagitis and compare clinical characteristics and treatmen...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-020-06706-4
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abstract:BACKGROUND:Pancreatic cancer can be difficult to diagnose. Fine-needle aspiration (FNA) biopsies may be negative even when malignancy is present. AIMS:To identify endosonographic features predictive of malignancy that will separate patients into high- and low-risk groups, in whom a negative FNA effectively rules out m...
journal_title:Digestive diseases and sciences
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doi:10.1007/s10620-009-0889-y
更新日期:2010-04-01 00:00:00
abstract::It is known that the muscularis mucosae and mucosa are not pharmacologically homogeneous throughout the rat colon. The aim of this study was to simultaneously characterize all three neurokinin (NK) receptors in the muscularis mucosae and mucosa along the length of the rat colon. Strips of proximal, mid, and distal col...
journal_title:Digestive diseases and sciences
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doi:10.1007/s10620-006-3163-6
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abstract::Metoclopramide tablets have been approved for use in the acute and chronic management of diabetic gastroparesis. Its efficacy as an antiemetic has been well documented. We measured the acute and chronic effects of oral metoclopramide on gastric liquid emptying in 12 diabetic patients with symptoms of stasis using scin...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/BF01318364
更新日期:1985-01-01 00:00:00
abstract::Recent data would limit indications for serum CEA measurement primarily to follow-up of resected colonic malignancy, yet physician attitude and usage patterns may lag far behind current findings. This discrepancy was investigated at our institution, where more than 1100 CEAs costing $71,000 are ordered each year. Of 4...
journal_title:Digestive diseases and sciences
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abstract:BACKGROUND:Topical pharyngeal anesthesia as an adjunct to intravenous sedation to facilitate gastroscopy has been widely acknowledged; however, its efficacy has not been established when it is used in patients under deep sedation with propofol. AIMS:To demonstrate the limited value of topical pharyngeal anesthesia in ...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章,随机对照试验
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abstract::We measured suprahepatic vein and arterial partial oxygen pressure in 35 alcoholics with severe (N = 7) or mild (N = 28) histological liver damage and without evidence of clinical liver failure. The suprahepatic vein was punctured with a fine needle, using a percutaneous approach. Suprahepatic vein partial oxygen pres...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
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更新日期:1995-06-01 00:00:00
abstract:BACKGROUND AND PURPOSE:Inflammatory bowel disease (IBD) consists of ulcerative colitis (UC) and Crohn's disease (CD), which are complex genetic disorders resulting from the interplay between several genetic and environmental risk factors. The arylamine N-acetyltransferase 2 (NAT2) enzyme detoxifies a wide spectrum of n...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-010-1527-4
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journal_title:Digestive diseases and sciences
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doi:10.1007/BF01540167
更新日期:1990-06-01 00:00:00
abstract::Serum levels of immunosuppressive acidic protein (IAP) were determined in 68 patients undergoing resection of colorectal cancer and 21 healthy subjects. Eighteen patients had perioperative transfusion of allogeneic blood (transfused patients) and 50 patients had no blood transfusion (nontransfused patients). Transfuse...
journal_title:Digestive diseases and sciences
pub_type: 临床试验,杂志文章
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更新日期:1999-08-01 00:00:00
abstract::A case of small bowel ulceration and perforation possibly due to therapy with Klotrix in a patient with Crohn's disease is presented. Following emergent surgery with creation of a diverting loop jejunostomy, subsequent reestablishment of intestinal continuity was carried out with excellent clinical results. Gastrointe...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/BF01299819
更新日期:1986-12-01 00:00:00
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journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1023/a:1005527230346
更新日期:2000-07-01 00:00:00
abstract:BACKGROUND AND AIMS:The purpose of this prospective study was to demonstrate the ability to measure pancreatic tumor tissue blood flow (TBF) with a noninvasive method using xenon inhalation computed tomography (xenon-CT) and to correlate TBF with histological features, particularly microvascular density (MVD). METHODS...
journal_title:Digestive diseases and sciences
pub_type: 临床试验,杂志文章
doi:10.1007/s10620-011-1915-4
更新日期:2012-03-01 00:00:00
abstract::In a double-blind study on 19 patients with the diagnosis of chronic pancreatitis, the effects of treatment with a granulated pancreatic enzyme preparation (Pankreon) were compared with those of placebo administration. One week of treatment with each preparation was preceded by one week without any medication. The pat...
journal_title:Digestive diseases and sciences
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF01315137
更新日期:1983-02-01 00:00:00
abstract::Fish oil (a very long chain triglycerides, VLCT) has received much attention because of its favorable metabolic properties; however, its effect on gastrointestinal function has not been studied. We investigated the effects of intraduodenally administered VLCT on gut-hormone release [cholecystokinin (CCK), neurotensin,...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1023/a:1005594514399
更新日期:2000-09-01 00:00:00
abstract::Free radical damage in reflux esophagitis of rats induced by 24-hr duodenojejunal ligation was studied. Oxygen free radicals were selectively blocked. Groups were: sham operation, reflux, reflux + superoxide dismutase (SOD), catalase, dimethylthiourea, allopurinol, and inactivated SOD or inactivated catalase alone or ...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/BF02065541
更新日期:1995-06-01 00:00:00
abstract:BACKGROUND:The presence of necrotic collection in acute necrotizing pancreatitis (ANP) at intra-abdominal sites other than the retroperitoneum has not been systematically studied. AIM:To investigate unusual sites of necrotic collections at computed tomography (CT) and to evaluate association with pancreatic necrosis a...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-020-06526-6
更新日期:2020-08-10 00:00:00
abstract:BACKGROUND:Eosinophilic esophagitis is among the causes of refractory reflux disease. Biopsy of esophagus is the gold standard for diagnosis. In this study we determined the frequency of eosinophilic esophagitis (EE) in refractory reflux cases referred to Motility Department of Shahid Beheshti Research Center of Gastro...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-008-0706-z
更新日期:2010-01-01 00:00:00
abstract::Apoptosis is an important process in a wide variety of different biological systems. In addition to caspases, recently, calpains, another family of proteases, have been found to be involved in apoptosis of many cell systems. This study is designed with the aims to evaluate the possible effect of Z-LLY-FMK (a calpain i...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-008-0652-9
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abstract:BACKGROUND:Obesity is associated with NAFLD, and bariatric surgery has significant impact on this liver disease, with reported improvement in hepatic fibrosis. AIMS:To investigate the effects of bariatric surgery on long-term liver disease-related outcome in obese patients with nonalcoholic fatty liver disease (NAFLD)...
journal_title:Digestive diseases and sciences
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更新日期:2018-07-01 00:00:00
abstract::The interaction of [35S]methionine with hepatic tRNA in normal, carcinogen-treated, and partially hepatectomized rats was studied. tRNA was preferentially labeled following [35S]methionine (1.6 mCi, 25 mg/kg body wt) administration by intraperitoneal injection. The extent of [35S]methionine-tRNA interaction was impair...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/BF01297152
更新日期:1991-07-01 00:00:00
abstract:BACKGROUND AND AIMS:Ulcerative colitis (UC) patients with progression of their disease despite optimized medical therapy may warrant "curative" proctocolectomy with end ileostomy or ileo-anal pouch (IPAA) anastomosis. The aim of our study was to assess the incidence of later recurrent ileitis that lead to altering the ...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-017-4873-7
更新日期:2018-02-01 00:00:00
abstract::The protein ornithine decarboxylase antizyme (AZ) is inhibitory to both polyamine transport and synthesis. Experiments were performed to examine the distribution and regulation of AZ mRNA in cells of the small intestinal epithelium, a tissue exposed to high concentrations of extracellular polyamines and high levels of...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1023/a:1015886212653
更新日期:2002-07-01 00:00:00
abstract::Twelve partially gastrectomized subjects who have consecutively undergone total biliary diversion for severe bilious vomiting were studied before and after operation in order to assess the effects of surgery on gastric histology and enterogastric reflux. Before and six months after operation, the following protocol wa...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/BF01536682
更新日期:1988-10-01 00:00:00
abstract:BACKGROUND:Data on real-life patterns of biologic use for inflammatory bowel disease (IBD) are scarce. AIMS:We aimed to examine the patterns of biologic use and the factors associated with non-persistence and switching of biologics in Korean IBD patients. METHODS:Using National Health Insurance claims, we collected d...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-019-05867-1
更新日期:2020-05-01 00:00:00
abstract:BACKGROUND AND AIM:Negative association has been reported between presence of Helicobacter pylori and developing gastroesophageal reflux disease (GERD) and its complications. The aim of this study was to determine whether H. pylori (HP) can be protective against GERD in an African American (AA) population. METHODS:Fro...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-012-2349-3
更新日期:2012-11-01 00:00:00
abstract::Prevalence estimates for irritable bowel syndrome from surveys in Western countries are 4.4% to 22%, generally higher in women than men, and only a minority seek health care. There are few studies of bowel patterns in Asian countries. We conducted a survey of a nonpatient population in Ho Chi Minh City, Vietnam, to de...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-005-9005-0
更新日期:2006-05-01 00:00:00
abstract::Cyclic vomiting syndrome is a disorder characterized by recurrent episodes of nausea and vomiting with complete resolution of symptoms between attacks. Nitric oxide plays a critical role in regulating several components of gastrointestinal mucosal defense and injury. Interleukin-6 has a wide variety of actions in the ...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1023/a:1010712703685
更新日期:2001-04-01 00:00:00
abstract::Assessment of disease activity by clinical parameters in ulcerative colitis is still controversial. Different clinical indexes have been proposed. Colonoscopy provides detailed information on mucosal damage. The aim of this study was to identify, among 21 clinical and laboratory parameters, which were predictive of en...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/s10620-005-1590-4
更新日期:2005-02-01 00:00:00
abstract::The association of chronic intestinal pseudoobstruction with ophthalmoplegia has been reported previously in visceral myopathies. We report a case of this association in which muscle mitochondria had a crystalline appearance, a dense core, and decreased cytochrome c oxidase and succinate cytochrome c reductase activit...
journal_title:Digestive diseases and sciences
pub_type: 杂志文章
doi:10.1007/BF01307743
更新日期:1992-03-01 00:00:00