Search results for "Ergoline"

Ipobscurines, Non-ergoline Type Indole Compounds from the Seeds of Ipomoea obscura.

1986

Evaluation of [11C]Metergoline as a PET Radiotracer for 5HTR in Nonhuman Primates

2010

Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [{sup 11}C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [{sup 11}C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.

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…

Physiology and Pathology of Ovarian Hyperstimulation Syndrome

2010

Ovarian hyperstimulation syndrome (OHSS) occurs when ovaries primed with follicle-stimulating hormone/leuteinizing hormone (LH) are subsequently exposed to human chorionic gonadotropin (hCG). The ultimate pathophysiological step underlying this clinical picture is increased vascular permeability (VP). With the administration of hCG, the expression vascular endothelial growth factor (VEGF) and VEGF receptor 2 (VEGFR-2) mRNA increases significantly rising to a maximum coinciding with peaked VP. Immunohistochemistry shows the presence of VEGF and VEGFR-2 proteins in the granulosa-lutein and endothelial cells of the entire corpus luteum. These findings suggest that the syndrome can be prevented…

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…

Partialsynthese neuer Ergolinderivate aus Clavinalkoloiden, 5. Mitt. N-1- und N-6-mono- und disubstituierte Festuclavine

1985

Festuclavin (1), 6-Cyano-6-nor-1 (3), 6-Nor-1 (5) und 6-Allyl-6-nor-1 (7) lassen sich in flussigem Ammoniak mit Kalium und dem entsprechenden Iodid in ihre 1-Allyl- und 1-Propyl-Derivate uberfuhren. Die Darstellung von 7 aus 5 wird beschrieben. Partial Syntheses of New Ergoline Derivatives from Clavine Alkaloids, V: Festuclavines Mono- and Disubstituted at N-1 and N-6 Festuclavine (1), 6-cyano-6-nor-1 (3), 6-nor-1 (5) and 6-allyl-6-nor-1 (7) were converted to their 1-allyl- and 1-propyl derivatives with potassium and the corresponding iodide in ammonia. The preparation of 7 from 5 is described.

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…

A Reassessment of the Therapeutic Potential of a Dopamine Receptor 2 Agonist (D2-AG) in Endometriosis by Comparison against a Standardized Antiangiog…

2021

Dopamine receptor 2 agonists (D2-ags) have been shown to reduce the size of tumors by targeting aberrant angiogenesis in pathological tissue. Because of this, the use of a D2-ag was inferred for endometriosis treatment. When assayed in mouse models however, D2-ags have been shown to cause a shift of the immature vessels towards a more mature phenotype but not a significant reduction in the amount of vascularization and size of lesions. These has raised concerns on whether the antiangiogenic effects of these compounds confer a therapeutic value for endometriosis. In the belief that antiangiogenic effects of D2-ags in endometriosis were masked due to non-optimal timing of pharmacological inte…

Inhibition of KIF20A by BKS0349 reduces endometriotic lesions in a xenograft mouse model

2019

AbstractSeveral studies have suggested a possible etiological association between ovarian endometriosis and ovarian cancer. Evidence has shown that KIF20A overexpression might confer a malignant phenotype to ovarian tumors by promoting proliferation and inhibiting apoptosis. However, no data about the role of KIF20A in endometriosis have been described. In this study, the human endometrium (n = 4) was transfected by mCherry adenovirus and intraperitoneally implanted in mice. Subsequently, mice were divided in three groups (n = 8/group) that were treated with Vehicle, BKS0349 (KIF20A-antagonist) or cabergoline (dopamine receptor agonist) for 21 days. mCherry-labeled endometriotic lesions wer…

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…