Search results for "Ergolines"
showing 8 items of 18 documents
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 …
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 …
Pleuropulmonary changes induced by ergoline drugs.
1996
Classic ergolines, such as bromocriptine, methysergide and ergotamine, can induce chronic pleuropneumonitis. We present the cases of eight patients who developed similar changes whilst on other ergolines. In this retrospective case study spanning 1985-1995, clinical data, radiological material, pulmonary function, bronchoalveolar lavage and histopathology were reviewed. Earlier literature on ergoline-induced pleuropulmonary changes was reviewed. Eight middle-aged to elderly individuals of both sexes developed pleuropulmonary changes during long-term therapy with regular dosages of nicergoline (n = 4), dihydroergocristine (n = 3), or dihydroergotamine (n = 1). Bibasilar pleural thickening wi…
Dopamine agonist administration causes a reduction in endometrial implants through modulation of angiogenesis in experimentally induced endometriosis
2009
Survival of newly implanted retrograde-shed endometrial tissue during menstruation in an ectopic location requires an adequate blood supply. This suggests that angiogenesis is a prerequisite for the development of endometriosis and that its inhibition may be a target for preventing development. Previous studies have shown that vascular endothelial growth factor (VEGF), a heparin-binding glycoprotein, has an essential role in angiogenesis. The main regulatory factor for angiogenesis appears to be binding of VEGF to its type-2 receptor (VEGFR-2). Cabergoline (Cb2) and other dopamine agonists promote endocytosis of the VEGF receptor-2 (VEGFR-2) in endothelial cells, thereby preventing VEGF-VEG…
Targeting the vascular endothelial growth factor system to prevent ovarian hyperstimulation syndrome
2008
BACKGROUND: Ovarian hyperstimulation syndrome (OHSS) typically occurs when ovaries are primed with FSH/ LH and subsequently exposed to hCG. The ultimate pathophysiological step underlying this clinical picture is increased vascular permeability (VP). METHODS: A search of the literature was carried out using PubMed and the authors’ files. RESULTS: In rodents and humans, the expression of vascular endothelial growth factor (VEGF) and VEGF receptor 2 (VEGFR-2) mRNA increases during ovarian stimulation. With the administration of hCG, the expression of each rises to a maximum. Expression of VEGF/VEGFR-2 mRNAs correlates with enhanced VP, with both peaking 48 h following an injection of hCG. Imm…
Response to dopamine agonists of the rat isolated uterus.
1993
1. Quinpirole did not produce any effect in isolated uterus from oestrogenized rats even when it is contracted by KCl (37 mM). 2. Fenoldopam produced a relaxant effect on rat isolated uterus contracted by KCl which was not significantly modified by SCH 23390. 3. Reserpine decreased the effect of the lowest doses of fenoldopam. In reserpinized rats, propranolol (10(-9), 10(-8), 10(-7) M) antagonized the effect of the lowest doses of fenoldopam and neither SCH 23390, sulpiride nor ranitidine modified the effect of fenoldopam. 4. The results confirm our previous finding that DA1-receptors are not functional in our preparation. The effect of fenoldopam was partially due to a catecholamine-relea…