Search results for "Ileum"
showing 10 items of 154 documents
In situ kinetic modelling of intestinal efflux in rats: functional characterization of segmental differences and correlation with in vitro results.
2007
The objective was to devise and apply a novel modelling approach to combine segmental in situ rat perfusion data and in vitro cell culture data, in order to elucidate the contribution of efflux in drug absorption kinetics. The fluoroquinolone CNV97100 was used as a model P-gp substrate. In situ intestinal perfusion was performed in rat duodenum, jejunum, ileum and colon to measure the influence of P-gp expression on efflux. Inhibition studies of CNV97100 were performed in the presence of verapamil, quinidine, cyclosporin A and p-aminohippuric acid. Absorption/efflux parameters were modelled simultaneously, using data from both in situ studies as well as in vitro studies. The maximal efflux …
5-Oxo-1,4-dihydroindenopyridines: Calcium modulators with partial calcium agonistic activity
1990
The title compounds 4a-g were prepared by Knoevenagel reactions of 1,3-indandione (1) with the aromatic aldehydes 2a-g followed by cyclizing Michael addition of the products thus obtained with methyl β-aminocrotonate (3). The structures of products 4 were characterized by spectal data. Positive inotropic activities were observed on electrically stimulated, left atria of giunea pigs and these effects could be attributed to calcium agonism. On the other hand, barium chloride-induced contractions of guinea pig ileum were inhibited in a dose-dependent manner.
ChemInform Abstract: 5-Oxo-1,4-dihydroindenopyridines: Calcium Modulators with Partial Calcium Agonistic Activity.
1990
The title compounds 4a-g were prepared by Knoevenagel reactions of 1,3-indandione (1) with the aromatic aldehydes 2a-g followed by cyclizing Michael addition of the products thus obtained with methyl β-aminocrotonate (3). The structures of products 4 were characterized by spectal data. Positive inotropic activities were observed on electrically stimulated, left atria of giunea pigs and these effects could be attributed to calcium agonism. On the other hand, barium chloride-induced contractions of guinea pig ileum were inhibited in a dose-dependent manner.
Über basisch substituierte Tryptamine und Tryptophole. 3. Mitt.: Pharmakologische Prüfung in 1- und 2-Stellung basisch substituierter Derivate
1970
Es wird die pharmakologische Prufung von 1-(Dialkylaminomethyl)-tryptamin- und -tryptophol-Derivaten sowie von 2-(Piperidinomethyl)-tryptophol-Derivaten beschrieben. Die wirksamste Verbindung dieser Reihe ist das 1-(Piperidinomethyl)-benzoyltryptopholmethojodid, das am mit Doryl® stimulierten Ileum der Ratte etwa 4mal starker wirkt als Scopolamin-n-butylbromid (Buscopan®) und am mit Histamin stimulierten Ileum des Meerschweinchens gute Antihistamineigenschaften aufweist. Am isolierten Vorhof des Meerschweinchens konnte die positiv inotrope Wirkung dieser Substanz als ein indirekt sympathomimetischer Effekt charakterisiert werden. Basic Substituted Tryptamines and Tryptophols The pharmacolog…
ChemInform Abstract: Vinylogous and Coupled Hexahydroquinolinones and Dihydropyridines with Calcium-Modulating Effects.
1990
The vinylogous, anellated and non-anellated dihydropyridines 4 and their coupled analogues 5 are accessible through Hantzsch-type cyclization reactions. IR, 1H-NMR, and mass spectral data are in agreement with the postulated structures. Pharmacological investigations on electrically-stimulated left atria of guinea pigs with some of the compounds gave rise to positive inotropic activities whereas BaCl2-induced contractions of the ileum were inhibited in a dose-dependent manner by some of the products.
NK1- and NK3-receptor mediated inhibition of 5-hydroxytryptamine release from the vascularly perfused small intestine of the guinea-pig
1997
The effects of tachykinins on the spontaneous release of 5-hydroxytryptamine (5-HT) from the enterochromaffin cells into the portal circulation was investigated in vitro using the vascularly perfused isolated guinea-pig small intestine. 5-HT was determined by HPLC with electrochemical detection. Test substances were applied intraarterially. Substance P (SP) caused a concentration-dependent decrease in 5-HT outflow with an EC50 of 50 pmol/l. Similarly, the selective NK1 receptor agonist SP methyl ester (1 nmol/l) significantly inhibited 5-HT outflow (to 51 +/- 3%). When tetrodotoxin (1 mumol/l) was added to the arterial perfusion medium, the inhibition by SP of 5-HT outflow was not affected.…
Antispasmodic Effects and Structure−Activity Relationships of Labdane Diterpenoids from Marrubium globosum ssp. libanoticum
2009
Marrubium globosum ssp. libanoticum is a medicinal plant used in Lebanon to reduce pain and smooth muscle spasms. A chloroform extract obtained from M. globosum aerial parts reduced acetylcholine-induced contractions in the isolated mouse ileum. The purification of this extract identified, among 12 isolated labdane diterpenoids, four new compounds, named 13-epicyllenin A (4), 13,15-diepicyllenin A (5), marrulibacetal (9), and marrulactone (11). Their structures were determined by spectroscopic methods. Compound 9, which exerted antispasmodic activity, is likely the active ingredient of the extract. Preliminary structure-activity relationships for this class of compounds are suggested.
Ileal Melanoma, A Rare Cause of Small Bowel Obstruction: Report of a Case, and Short Literature Review.
2020
Background: Malignant melanoma frequently spreads to the gastrointestinal tract, with 60% of patients with advanced metastatic disease showing digestive involvement; however, primary MM of the small intestine is a controversial diagnosis. In fact, whether these lesions arise as true small bowel primary neoplasms or represent metastases from unidentified cutaneous melanomas remains debatable. The most common complications are intestinal obstruction, massive gastrointestinal bleeding, and perforation. Objective & Methods: We report a case of a 64-year-old patient, with an unremarkable medical history, in which a late diagnosis of primary ileal malignant melanoma in the setting of an emer…
Clinicopathological profile of gastrointestinal tuberculosis: a multinational ID-IRI study
2020
Data are relatively scarce on gastro-intestinal tuberculosis (GITB). Most studies are old and from single centers, or did not include immunosuppressed patients. Thus, we aimed to determine the clinical, radiological, and laboratory profiles of GITB. We included adults with proven GITB treated between 2000 and 2018. Patients were enrolled from 21 referral centers in 8 countries (Belgium, Egypt, France, Italy, Kazakhstan, Saudi Arabia, UK, and Turkey). One hundred four patients were included. Terminal ileum (n = 46, 44.2%), small intestines except terminal ileum (n = 36, 34.6%), colon (n = 29, 27.8%), stomach (n = 6, 5.7%), and perianal (one patient) were the sites of GITB. One-third of all p…
Glucagon-like peptide-1 modulates neurally evoked mucosal chloride secretion in guinea pig small intestine in vitro
2011
Glucagon-like peptide-1 (GLP-1) acts at the G protein-coupled receptor, GLP-1R, to stimulate secretion of insulin and to inhibit secretion of glucagon and gastric acid. Involvement in mucosal secretory physiology has received negligible attention. We aimed to study involvement of GLP-1 in mucosal chloride secretion in the small intestine. Ussing chamber methods, in concert with transmural electrical field stimulation (EFS), were used to study actions on neurogenic chloride secretion. ELISA was used to study GLP-1R effects on neural release of acetylcholine (ACh). Intramural localization of GLP-1R was assessed with immunohistochemistry. Application of GLP-1 to serosal or mucosal sides of fla…