Search results for "harm"
showing 10 items of 13866 documents
Capsaicin desensitization in vivo is inhibited by ruthenium red.
1990
The effect of systemic administration of Ruthenium Red on the excitatory and desensitizing effect of capsaicin was investigated in rats. Ruthenium Red was injected s.c. 30 min before capsaicin was administered. The excitatory effect of capsaicin on corneal, perivascular and visceral afferents was not influenced by treatment with Ruthenium Red. However, determination of the neuropeptide content and evoked neuropeptide release in peripheral organs and dorsal spinal cord 48 h after treatment showed that Ruthenium Red attenuated the 'desensitizing' effect of capsaicin at peripheral, but not at central, endings of primary afferents. On the other hand, a capsaicin-elicited autonomic reflex mediat…
closo-borane conjugated regulatory peptides retain high biological affinity: synthesis of closo-borane conjugated Tyr(3)-octreotate derivatives for B…
2008
Despite the improvements in cancer therapy during the past years, high-grade gliomas and many other types of cancer are still extremely resistant to current forms of therapy. Boron neutron capture therapy (BNCT) provides a promising way to destroy cancer cells without damaging healthy tissue. However, BNCT in practice is still limited due to the lack of boron-containing compounds that selectively deliver boron to cancer cells. Since many neuroendocrine tumors show an overexpression of the somatostatin receptor, it was our aim to synthesize compounds that contain a large number of boron atoms and still show high affinity toward this transmembrane receptor. The synthetic peptide Tyr (3)-octre…
Receptor-mediated uptake of boron-rich neuropeptide y analogues for boron neutron capture therapy.
2014
Peptidic ligands selectively targeting distinct G protein-coupled receptors that are highly expressed in tumor tissue represent a promising approach in drug delivery. Receptor-preferring analogues of neuropeptide Y (NPY) bind and activate the human Y1 receptor subtype (hY1 receptor), which is found in 90% of breast cancer tissue and in all breast-cancer-derived metastases. Herein, novel highly boron-loaded Y1 -receptor-preferring peptide analogues are described as smart shuttle systems for carbaboranes as (10) B-containing moieties. Various positions in the peptide were screened for their susceptibility to carbaborane modification, and the most promising positions were chosen to create a mu…
MONENSIN ENHANCES DIGOXIN-INDUCED ARRHYTHMIAS IN GUINEA-PIGS
1993
Effects of pretreatment with monensin (150 ug/kg), atenolol (0.3 mg/kg), atenolol plus monensin, verapamil (0.38 mg/kg), verapamil plus monensin, glibenclamide(0.38 mg/kg) and glibenclamide plus monensin on the dose of digoxin required to induce premature ventricular contractions (PVCS) in anaesthetized guinea-pigs were studied. Monensin reduced while atenolol increased the dose of digoxin required to produce PVCS. Atenolol plus monensin increased the dose of digoxin required to produce PVCS in presence of monensin alone. Verapamil reduces the arrhythmogenic effect of monensin on digoxin. Glibenclamide antagonises the effect of monensin on digoxin induced PVCS. From the present data it coul…
Synthese und pharmakologische Wirkung von carbocyclischen Muskarinanalogen
1974
Als carbocyclische Muskarinanaloga wurden das (3-Hydroxycyclopentylmethyl)trimethyl-ammonium-jodid und dessen Acetat dargestellt und am isolierten Ileum des Meerschweinchens untersucht. Synthesis and Pharmacological Activity of Carbocyclic Analogs of Muscarine As carbocyclic analogs of muscarine (3-hydroxycyclopentylmethyl)trimethylammonium iodide and (3-acetoxycyclopentylmethyl)trimethylammonium iodide were synthesized and tested on the isolated guinea pig ileum.
The iron-regulatory hormone hepcidin: A possible therapeutic target?
2015
The maintenance of stable extracellular and intracellular iron concentrations requires the coordinated regulation of iron transport into plasma. Iron is a fundamental cofactor for several enzymes involved in oxidation-reduction reactions. The redox ability of iron can lead to the production of oxygen free radicals, which can damage various cellular components. Therefore, the appropriate regulation of systemic iron homeostasis is decisive in vital processes. Hepcidin has emerged as the central regulatory molecule of systemic iron homeostasis. It is synthesized in hepatocytes and in other cells and released into the circulation. It inhibits the release of iron from enterocytes of the duodenum…
Crystal structure of a 1:1 salt of 4-aminobenzoic acid (vitamin B10) with pyrazinoic acid
2018
The paper reports the crystal structure of novel salt of 4-aminobenzoic acid (Vitamin B10) with pyrazinoic acid.
Crystal structure of hydrocortisone 17-butyrate
2014
In the title compound, C25H36O6, the two central cyclohexane rings exhibit a chair conformation. The terminal cyclohexene and cyclopentane rings are in half-chair and envelope conformations (with the C atom bearing the methyl substituent as the flap), respectively. The methyl group of the butyrate chain is disordered over two orientations, with a refined occupancy ratio of 0.742 (6):0.258 (6). Intramolecular O—H...O and C—H...O hydrogen bonds are observed. In the crystal, molecules are linked by O—H...O hydrogen bonds into chains running parallel to theaaxis.
Effects of magnesium chloride on the contractile response of uterus to several agonists in Ca-free solution
1987
Abstract The effects of MgCl2 on the oestrogen-dominated rat uterus have been examined. Tissues were preincubated in a Ca2+- and Mg2+-free medium containing 3 mM EDTA. Most experiments were subsequently performed in a similar medium containing either no EDTA or EDTA (1 mM). When MgCl2 was added cumulatively (1–32 mM) no contractile responses were obtained in Ca,Mg-free medium or in Ca,Mg-free high K+ solution. When 2 mM CaCl2 as added, a sustained contraction was obtained. Subsequent addition of cumulative concentrations of MgCl2 caused concentration-dependent relaxation. Oxytocin, 2 μM, produced a small and sustained contraction in a Ca,Mg-free medium. Addition of MgCl2, 2 mM, increased th…
Risques et bénéfices relatifs des alternatives aux produits phytopharmaceutiques comportant des néonicotinoïdes
2018
Risques et bénéfices relatifs des alternatives aux produits phytopharmaceutiques comportant des néonicotinoïdes. Tome 1 – Rapport du groupe de travail Identification des alternatives aux usages autorisés des néonicotinoïdes