Search results for "Ergoline"
showing 10 items of 30 documents
The effects of ergot and non-ergot-derived dopamine agonists in an experimental mouse model of endometriosis
2011
Implantation of a retrogradely shed endometrium during menstruation requires an adequate blood supply, which allows the growth of endometriotic lesions. This suggests that the development of endometriosis can be impaired by inhibiting angiogenesis. The growth of endometriotic foci is impaired by commercial oncological antiangiogenic drugs used to block vascular endothelial growth factor (VEGF) signaling. The dopamine agonist cabergoline (Cb2) inhibits the growth of established endometriosis lesions by exerting antiangiogenic effects through VEGFR2 inactivation. However, the use of ergot-derived Cb2 is associated with an increased incidence of cardiac valve regurgitation. To evaluate the pot…
Dopamine agonist cabergoline reduces hemoconcentration and ascites in hyperstimulated women undergoing assisted reproduction.
2007
Abstract Context: Ovarian hyperstimulation syndrome (OHSS) results from increased vascular permeability (VP) caused by ovarian hypersecretion of vascular endothelial growth factor (VEGF), which activates its receptor-2. In animals, the dopamine receptor 2 agonist cabergoline (Cb2) inactivates VEGF receptor-2 and prevents increased VP. Objective: Our objective was to test whether Cb2 reduces VP and prevents OHSS in humans. Design: We conducted a prospective, randomized, double-blind study on oocyte donors at risk of developing OHSS (>20 follicles, >12 mm developed, and >20 oocytes retrieved). Interventions: Cb2 0.5 mg/d (n = 37) or a placebo (n = 32) was administered fro…
Partialsynthese neuer Ergolinderivate aus Clavinalkaloiden, 3. Mitt.1) O-Acyl- und O-Alkyl-1,6-dimethyl-8-hydroxymethyl-ergol-9-ene
1983
Elymoclavin (1), Lysergol (2) und O-Acyl-lysergole werden in flussigem Ammoniak mit Kalium und Methyliodid zunachst am Indolstickstoff methyliert. Durch Variation der Versuchsbedingungen werden 1 und 2 sekundar auch an der Hydroxylgruppe methyliert. Aus 1-Methyl-lysergol (3) sind daher nach der gleichen Methode mit verschiedenen Alkyliodiden 1-Methyl-lysergol-ether darstellbar. Dagegen gelingt die Ethersynthese nach Williamson aus 17-Halogen-ergolenen nicht. Partial Synthesis of New Ergoline Dervatives from Clavine Alkaloids, III: O-Acyl-and O-Alkyl-1,6-dimethyl-8-(hydroxymethyl)ergol-9-enes Elymoclavine (1), lysergole (2) and O-acyllysergoles are primarily methylated at the indole nitrogen…
Partialsynthese neuer Ergolinderivate aus Clavinalkaloiden, 4. Mitt. N-1-, C-2- und N-6-monosubstituierte Agroclavine
1985
Agroclavin (1) wird in flussigem Ammoniak/Kaliumamid mit Alkyliodid am Indolstickstoff alkyliert. 1 last sich mit N-Iodsuccinimid zu 2-Iod-1 (3) umsetzen. Mit der Bromcyan-Methode wird 6-Nor-1 (4b) gewonnen und danach an N-6 alkyliert. Partial Synthesis of New Ergoline Derivatives from Clavine Alkaloids, IV: Agroclavines Monosubstituted at N-1, C-2, and N-6 Agroclavine (1) is alkylated at the indole nitrogen with alkyl iodide in ammonia/potassium amide. It is convertible to 2-iodo-1 (3) with N-iodosuccinimide. Compound 6-nor-1 can be prepared by means of the cyanogen bromide method; alkylation at N-6 is described exemplarily for the ethyl derivative.
Roquefortine C occurrence in blue cheese.
2001
Several strains of Penicillium are used for the production of mold-ripened cheeses, and some of them are able to produce mycotoxins. The aims of the research were the determination of roquefortine C and PR toxin in domestic and imported blue cheeses, the identification of the penicillia used as starter, and the investigation of their capacity for producing toxins in culture media. Roquefortine C was always found in the cheeses at levels ranging from 0.05 to 1.47 mg/kg, whereas the PR toxin was never found. The identification of the fungal strains present in the domestic cheeses included Penicillium glabrum, Penicillium roqueforti, and Penicillium cyclopium in the Gorgonzola "dolce" and Peni…
Clavines as antitumor agents. 3: Cytostatic activity and structure/activity relationships of 1-alkyl agroclavines and 6-alkyl 6-noragroclavines.
1986
The cytostatic potential of twenty antibiotic agroclavines has been examined in the L5178y mouse lymphoma cell system. Twelve of these compounds are described for the first time. It is shown that the substituent at N-1 of agroclavine is very important whereas the substituent at N-6 is of less influence if it is not hydrogen. Incorporation studies in the presence of 1-propylagroclavine suggest that DNA synthesis in the lymphoma cells is inhibited. The effect on the corresponding [3H]thymidine incorporation in murine spleen lymphocytes is comparably low. Neither a significant change of mRNA efflux nor of DNA polymerase alpha and beta activities was caused. The mechanism of action seems to be …
Regulation of noradrenergic coerulean neuronal firing mediated by 5-HT2 receptors: involvement of the prepositus hypoglossal nucleus.
1991
Abstract Previous studies have indicated a 5-HT2-mediated inhibitory influence on unit activity in the locus coeruleus. In the present work, attempts were made to determine which area(s) of the brain is (are) involved in this effect: (1) Microiontophoretic application of serotoninergic compounds (quipazine, ketanserin, RU 24969 (Roussel Uclaf), 8-hydroxy-2(di-n-propylamino) tetralin (8-OH-DPAT), metergoline, serotonin) in the locus coeruleus, did not alter the coerulean discharge. Local microinjection of quipazine or ketanserin in the area of the locus coeruleus, as well as in one of its major afferents, the prepositus hypoglossi, had no effect on the unit activity in the locus coeruleus. 1…
Effect of prolactin and the anti-prolactin bromocriptin on the testosterone uptake and metabolism in androgen-sensitive and insensitive canine organs
1976
Prolactin promotes the growth and function of the prostate in low doses, whereas high doses or previous castration reduce this effect. The antiprolactin bromocriptin should reverse the prolactin action. In the castrated dog the highest accumulation of H3-testosterone given i.v. occurred in the prostate as compared with muscle, urethra, penis, liver and kidney. Prolactin pretreatment increased the radiosteroid uptake only in the liver. Converseley, bromocriptin suppressed the tracer incorporation into the liver, but increased prostatic accumulation. The highest testerone reduction occurred in the prostate of the untreated castrated dogs as compared with other organs. Prolactin suppressed 5 a…
Efficacy of combined treatment with pasireotide, pegvisomant and cabergoline in an acromegalic patient resistant to other treatments: a case report
2018
Abstract Background The approach to acromegalic patients with persistent acromegaly after surgery and inadequate response to first-generation somatostatin receptor ligands (SRLs) should be strictly tailored. Current options include new pituitary surgery and/or radiosurgery, or alternative medical treatment with SRLs high dose regimens, pegvisomant (PEG) as monotherapy, or combined therapy with the addition of PEG or cabergoline to SRLs. A new pharmacological approach includes pasireotide, a second-generation SRL approved for patients who do not adequately respond to surgery and/or for whom surgery is not an option. No reports on efficacy and safety of combined therapy with pasireotide and p…
Effect of antiangiogenic treatment on peritoneal endometriosis-associated nerve fibers
2012
Objective To investigate the effect of antiangiogenic treatment on experimental endometriotic lesion nerve fibers. Design Heterologous mouse model of endometriosis. Setting University Institute IVI, University Hospital La Fe. Animal(s) Ovariectomized nude mice (n = 16) receiving human endometrial fragments from oocyte donors (n = 4). Intervention(s) Endometrium fragments stuck in the peritoneum of 5-week-old female nude mice treated with vehicle (n = 8) and antiangiogenic agent cabergoline (n = 8; Cb 2, 0.05 mg/kg/day) for 14 days. Main Outcome Measure(s) Immunofluorescence analysis of von-Willebrand factor (vWF) and vascular smooth muscle cells (αSMA) for evaluating the number of immature …