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Ramón Cacabelos
Parkinson's disease (PD) is the second most important age-related neurodegenerative disorder in developed societies, after Alzheimer's disease, with a prevalence ranging from 41 per 100,000 in the fourth decade of life to over 1900 per 100,000 in people over 80 years of age. As a movement disorder, the PD phenotype is characterized by rigidity, resting tremor, and bradykinesia. Parkinson's disease -related neurodegeneration is likely to occur several decades before the onset of the motor symptoms. Potential risk factors include environmental toxins, drugs, pesticides, brain microtrauma, focal cerebrovascular damage, and genomic defects...
March 4, 2017: International Journal of Molecular Sciences
Munki Kim, Sijoon Lee, Jeahyeon Cho, Gonsup Kim, Chungkil Won
Dopamine (DA) contributes to the regulation of voluntary movement, and a deficiency in DAergic neurons leads to movement disorders. The objective of this study was to examine the neuroprotective effect of DA D2-like receptor agonist, lisuride, and the role of DA receptors in this protection. Treatment with lisuride alleviated loss of tyrosine hydroxylase (TH) both direct and intraperitoneal injection in 6-hydroxydopamine (6-OHDA) mouse model. Similar results were obtained in primary neuronal cultures treated with lisuride...
May 1, 2017: Neuropharmacology
Marie-Victoire Sénat, Loïc Sentilhes, Anne Battut, Dan Benhamou, Sarah Bydlowski, Anne Chantry, Xavier Deffieux, Flore Diers, Muriel Doret, Chantal Ducroux-Schouwey, Florent Fuchs, Geraldine Gascoin, Chantal Lebot, Louis Marcellin, Genevieve Plu-Bureau, Brigitte Raccah-Tebeka, Emmanuel Simon, Gérard Bréart, Loïc Marpeau
OBJECTIVE: To make evidence-based recommendations for the postpartum management of women and their newborns, regardless of the mode of delivery. MATERIAL AND METHODS: Systematic review of articles from the PubMed database and the Cochrane Library and of recommendations from the French and foreign societies or colleges of obstetricians. RESULTS: Because breast-feeding is associated with reductions in neonatal, infantile, and childhood morbidity (lower frequency of cardiovascular, infectious, and atopic diseases and infantile obesity) (LE2) and improved cognitive development in children (LE2), exclusive and extended breastfeeding is recommended (grade B) for at least 4-6 months (professional consensus)...
July 2016: European Journal of Obstetrics, Gynecology, and Reproductive Biology
L Marcellin, A A Chantry
OBJECTIVE: Provide guidelines for clinical use of non-pharmacological and pharmacological treatments of inhibition of lactation and the management of the weaning. MATERIALS AND METHODS: Systematically review of the literature between 1972 and May 2015 from the databases Medline, Google Scholar, Cochrane Library, and the international recommendations about inhibition of lactation with establishment of levels of evidence (LE) and grades of recommendation. RESULTS: The available data on the effectiveness of non-pharmacological measures are limited, with very low levels of evidence that fail to make recommendations (Professional consensus)...
December 2015: Journal de Gynécologie, Obstétrique et Biologie de la Reproduction
M-V Sénat, L Sentilhes, A Battut, D Benhamou, S Bydlowski, A Chantry, X Deffieux, F Diers, M Doret, C Ducroux-Schouwey, F Fuchs, G Gascoin, C Lebot, L Marcellin, G Plu-Bureau, B Raccah-Tebeka, E Simon, G Bréart, L Marpeau
OBJECTIVE: To determine the post-partum management of women and their newborn whatever the mode of delivery. MATERIAL AND METHODS: The PubMed database, the Cochrane Library and the recommendations from the French and foreign obstetrical societies or colleges have been consulted. RESULTS: Because breastfeeding is associated with a decrease in neonatal morbidity (lower frequency of cardiovascular diseases, infectious, atopic or infantile obesity) (EL2) and an improvement in the cognitive development of children (EL2), exclusive and extended breastfeeding is recommended (grade B) between 4 to 6 months (Professional consensus)...
December 2015: Journal de Gynécologie, Obstétrique et Biologie de la Reproduction
Paweł Zajdel, Marek Bednarski, Jacek Sapa, Gabriel Nowak
Ergotamine, being a representative of naturally occurring ergoline alkaloids, derived from d-lysergic acid, and nicergoline, a d-lumilysergic acid derivative belonging to semi-synthetic ergot-derived alkaloids, display diversified affinity for adrenergic, serotoninergic, and dopamine receptors. Although introduction of triptans marginalized use of ergotamine, nicergoline is used in cerebral metabolic-vascular disorders, and dementia. Additionally, nicergoline exhibits a safety profile comparable to that of placebo, and none of the reviewed studies reported any incidence of fibrosis or ergotism with nicergoline treatment...
April 2015: Pharmacological Reports: PR
Madhuri Behari, Kapil Kumar Singhal
Parkinson's disease (PD) is the second most common neurodegenerative disorder after Alzheimer's disease. It is characterized by bradykinesia, hypokinesia/ akinesia, rigidity, tremor, and postural instability, caused by dopaminergic (DA) striatal denervation. The prevalence of PD increases from 50 years of age with steep rise after age 60 years. Current treatment of PD relies heavily on replacing lost dopamine either with its precursor L-dopa or dopamine agonists (ropinirole, pramipexole, bromocriptine, lisuride etc)...
April 2011: Annals of Neurosciences
Fumiki Oana, Hiroshi Onozuka, Akihiro Tsuchioka, Takayuki Suzuki, Nobuyuki Tanaka, Kouichi Kaidoh, Yuji Hoyano, Masahiro Hiratochi, Shinji Kikuchi, Yasuo Takehana, Nobuo Shibata
BACKGROUND AND AIM OF THE STUDY: The symptoms of Parkinson's disease are alleviated by dopamine D2 agonists, which are classified as ergot dopamine D2 agonists and non-ergot D2 agonists. Among the former, pergolide has been associated with valvular heart disease, since it has both potent D2 receptor and serotonin 5-HT(2B) receptor agonistic properties. Among the latter, pramipexole has few incidences of heart valve disease onset, since it has an absence of 5-HT(2B) receptor agonism. METHOD: A [3H]thymidine incorporation assay was performed to monitor function, and microarray global analysis to monitor gene expression, on porcine heart valve interstitial cells (VICs) treated with pergolide or pramipexole...
March 2014: Journal of Heart Valve Disease
Z Hliñák, I Dvorská
Lisuride was reported as drug stimulating sexual behaviour in the adult male rats. It was stated that lisuride is effective through central serotonergic and dopaminergic systems. The present study deals with the effects of lisuride on the sexual behaviour of juvenile Wistar male rats, 43 days old. The animals were injected i.p. with lisuride /0.4 mg/kg/ or saline 40 min prior to testing. When the males were put into a box with the floor prescented by an oestrous female, the males treated with lisuride devoted significantly more time to the sniffing of the scent traces...
April 1984: Behavioural Processes
Samah Karaki, Carine Becamel, Samy Murat, Clotilde Mannoury la Cour, Mark J Millan, Laurent Prézeau, Joël Bockaert, Philippe Marin, Franck Vandermoere
The serotonin 5-HT(2A) receptor is a primary target of psychedelic hallucinogens such as lysergic acid diethylamine, mescaline, and psilocybin, which reproduce some of the core symptoms of schizophrenia. An incompletely resolved paradox is that only some 5-HT(2A) receptor agonists exhibit hallucinogenic activity, whereas structurally related agonists with comparable affinity and activity lack such a psychoactive activity. Using a strategy combining stable isotope labeling by amino acids in cell culture with enrichment in phosphorylated peptides by means of hydrophilic interaction liquid chromatography followed by immobilized metal affinity chromatography, we compared the phosphoproteome in HEK-293 cells transiently expressing the 5-HT(2A) receptor and exposed to either vehicle or the synthetic hallucinogen 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI) or the nonhallucinogenic 5-HT(2A) agonist lisuride...
May 2014: Molecular & Cellular Proteomics: MCP
(no author information available yet)
Cardiac valve disease can involve one or more of the four heart valves. Chronic valve damage may remain asymptomatic for long periods but ultimately leads to haemodynamic overload of the heart. The most common causes of valve disease are rheumatic diseases, infections, chronic renal failure, malformations, and genetic diseases. Valve disease is often attributed to degeneration with no known cause.The frequency of drug-related valve disease has long been underestimated. Most implicated drugs have serotonergic properties, such as fenfluramine-derived amphetamines, including benfluorex...
December 2013: Prescrire International
Tania Có Rdova-Sintjago, Nancy Villa, Clinton Canal, Raymond Booth
Activation of the serotonin (5-hydroxytryptamine, 5-HT) 5HT2C G protein-coupled receptor (GPCR) is proposed as novel pharmacotherapy for obesity and neuropsychiatric disorders. In contrast, activation of the 5-HT2A and 5-HT2B GPCRs is associated with untoward hallucinogenic and cardiopulmonary effects, respectively. There is no crystal structure available to guide design of 5-HT2C receptor-specific ligands. For this reason, a homology model of the 5-HT2C receptor was built based on the crystal structure of the human β 2 adrenoceptor GPCR to delineate molecular determinants of ligand-receptor interactions for drug design purposes...
January 1, 2012: International Journal of Quantum Chemistry
Michelle G Baladi, Amy H Newman, Charles P France
RATIONALE: The contribution of dopamine receptor subtypes in mediating the discriminative stimulus effects of cocaine is not fully established. Many drug discrimination studies use food to maintain responding, necessitating food restriction, which can alter drug effects. OBJECTIVE: This study established stimulus control with cocaine (10 mg/kg) in free-feeding and food-restricted rats responding under a schedule of stimulus shock termination (SST) and in food-restricted rats responding under a schedule of food presentation to examine whether feeding condition or the reinforcer used to maintain responding impacts the effects of cocaine...
February 2014: Psychopharmacology
Dirk Deleu, Margaret G Northway, Yolande Hanssens
Apomorphine and certain ergot alkaloids (bromocriptine, lisuride and pergolide) have been available for several decades; for the last few years, they were joined by newer dopamine agonists (cabergoline, pramipexole and ropinirole) most of them are non-ergolines. Each of these dopamine agonists has its own pharmacological characteristics and occupies a place in the pharmacotherapy of Parkinsons disease. In this evidence-based review, emphasis is put on the clinical efficacy of dopamine agonists in early and advanced Parkinsons disease, and where possible comparative evidence regarding their efficacy and safety is provided...
October 2002: Neurosciences: the Official Journal of the Pan Arab Union of Neurological Sciences
Jianguo Huang, Qiying Gong, Chaodi Huang, Guiming Li
Cutaneous fibrosis seen in systemic sclerosis (SSc) is a generalized connective tissue disorder, characterized by a wide spectrum of microvascular and immunological abnormalities. Serotonin (5-hydroxytryptamine; 5-HT) is a neurotransmitter and immune modulator, is also an important mediator of bidirectional interactions between the vasoactive amines and the skin.5-HT, a commonly secreted amine, is a known inducer of fibrosis, although the mechanistic basis for it and growth factors regulating fibrosis and proliferation in the microenvironment are unclear...
March 2014: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
Tahani A Alahmadi, Quais M Mujawar
Lisuride Maleate (Dopergin) is semi synthetic ergot alkaloid used for a variety of medical conditions. It is licensed for use in Canada, EU and Middle East countries and is marketed by various drug companies. There are no reported cases of lisuride toxicity in the literature on Google Search or Pub med Search. Herein, we present a case of accidental overdose of lisuride maleate in a 21-month-old Saudi male and further clinical course and management. The aim of this report was to document the unusual features of lisuride toxicity in pediatric patients and to guide physicians for its management...
April 2013: Journal of Emergencies, Trauma, and Shock
José A G Agúndez, Elena García-Martín, Hortensia Alonso-Navarro, Félix Javier Jiménez-Jiménez
INTRODUCTION: The development of pharmacogenetic-based clinical practice guidelines for the use of anti-Parkinson's disease drugs requires, as a pre-requisite, the identification and validation of genetic biomarkers. These biomarkers are then used as surrogate endpoints. This review analyzes potential genetic biomarkers which can be used to improve anti-Parkinson's disease therapy. AREAS COVERED: The authors present an overview of current knowledge of pharmacogenetic implications of anti-Parkinson's disease drugs, including genes coding for the corresponding drug-metabolizing enzymes and drug targets...
July 2013: Expert Opinion on Drug Metabolism & Toxicology
Adam L Halberstadt, Mark A Geyer
RATIONALE: The head-twitch response (HTR) is a rapid side-to-side rotational head movement that occurs in rats and mice after administration of serotonergic hallucinogens and other 5-HT2A agonists. The HTR is widely used as a behavioral assay for 5-HT2A activation and to probe for interactions between the 5-HT2A receptor and other transmitter systems. OBJECTIVE: High-speed video recordings were used to analyze the head movement that occurs during head twitches in C57BL/6J mice...
June 2013: Psychopharmacology
Luis Velázquez-Pérez, Roberto Rodríguez-Labrada, Lázaro Álvarez-González, Raúl Aguilera-Rodríguez, Mario Álvarez Sánchez, Nalia Canales-Ochoa, Lourdes Galicia Polo, Reyes Haro-Valencia, Jacqueline Medrano-Montero, Yaimeé Vázquez-Mojena, Arnoy Peña-Acosta, Annelié Estupiñán-Rodríguez, Noemí Rodríguez Pupo
Periodic leg movements (PLMs) are a common sleep disorder in spinocerebellar ataxia type 2 (SCA2) being associated to higher disease severity and altered sleep patterns. To assess the efficacy and safety of lisuride for the treatment of PLMs in SCA2 patients, an open-label clinical trial was conducted in 12 SCA2 patients suffering from PLMs associated to other subjective sleep complaints. All subjects received 0.1 mg of oral lisuride daily for 4 weeks. Primary outcome measure was the change of PLMs index. Changes in the subjective sleep quality, other polysomnographical sleep parameters, Scale for the Assessment and Rating of Ataxia score, and saccadic velocity were assessed as secondary outcome parameters...
December 2012: Cerebellum
Alexandra Kekewska, Tilo Görnemann, Florian Jantschak, Erika Glusa, Heinz H Pertz
Serotonin (5-hydroxytryptamine; 5-HT) is involved in heart valve tissue fibrosis, pulmonary arterial fibrosis, and pulmonary hypertension. We aimed at characterizing the antiserotonergic properties of the ergot alkaloid derivative terguride [1,1-diethyl-3-(6-methyl-8α-ergolinyl)urea] by using functional receptor assays and valvular interstitial cell culture. Terguride showed no vasoconstrictor effect in porcine coronary arteries (5-HT(2A) receptor bioassay) and no relaxant effect in porcine pulmonary arteries (5-HT(2B) receptor bioassay)...
February 2012: Journal of Pharmacology and Experimental Therapeutics
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