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Michael O Thorner
Ergotism is the long term ergot poisoning by ingestion of rye or other grains infected with the fungus Claviceps purpurea and more recently by excessive intake of ergot drugs. It has either neuropsychiatric or vascular manifestations. In the Middle Ages the gangrenous poisoning was known as St Anthony's fire, after the order of the Monks of St Anthony who were particularly skilled at treating the condition. In 1917, Professor Arthur Stoll returned home to Switzerland from Germany, to lead the development of a new pharmaceutical department at Sandoz Chemical Company...
May 11, 2018: European Journal of Endocrinology
Wanchao Yin, X Edward Zhou, Dehua Yang, Parker W de Waal, Meitian Wang, Antao Dai, Xiaoqing Cai, Chia-Ying Huang, Ping Liu, Xiaoxi Wang, Yanting Yin, Bo Liu, Yu Zhou, Jiang Wang, Hong Liu, Martin Caffrey, Karsten Melcher, Yechun Xu, Ming-Wei Wang, H Eric Xu, Yi Jiang
5-hydroxytryptamine (5-HT, also known as serotonin) regulates many physiological processes through the 5-HT receptor family. Here we report the crystal structure of 5-HT1B subtype receptor (5-HT1B R) bound to the psychotropic serotonin receptor inverse agonist methiothepin (MT). Crystallization was facilitated by replacing ICL3 with a novel optimized variant of BRIL (OB1) that enhances the formation of intermolecular polar interactions, making OB1 a potential useful tool for structural studies of membrane proteins...
2018: Cell Discovery
Yao Peng, John D McCorvy, Kasper Harpsøe, Katherine Lansu, Shuguang Yuan, Petr Popov, Lu Qu, Mengchen Pu, Tao Che, Louise F Nikolajsen, Xi-Ping Huang, Yiran Wu, Ling Shen, Walden E Bjørn-Yoshimoto, Kang Ding, Daniel Wacker, Gye Won Han, Jianjun Cheng, Vsevolod Katritch, Anders A Jensen, Michael A Hanson, Suwen Zhao, David E Gloriam, Bryan L Roth, Raymond C Stevens, Zhi-Jie Liu
Drugs frequently require interactions with multiple targets-via a process known as polypharmacology-to achieve their therapeutic actions. Currently, drugs targeting several serotonin receptors, including the 5-HT2C receptor, are useful for treating obesity, drug abuse, and schizophrenia. The competing challenges of developing selective 5-HT2C receptor ligands or creating drugs with a defined polypharmacological profile, especially aimed at G protein-coupled receptors (GPCRs), remain extremely difficult. Here, we solved two structures of the 5-HT2C receptor in complex with the highly promiscuous agonist ergotamine and the 5-HT2A-C receptor-selective inverse agonist ritanserin at resolutions of 3...
February 8, 2018: Cell
Manoj B Kudupoje, James L Klotz, Alexandros Yiannikouris, Karl A Dawson, Kyle R McLeod, Eric S Vanzant
Ergot alkaloids, in their active isomeric form, affect animal health and performance, and adsorbents are used to mitigate toxicities by reducing bioavailability. Adsorbents with high specificity (molecularly imprinted polymers: MIP) adsorb ergot alkaloids in vitro, but require evaluation for biological implications. Using ex vivo myography, synthetic polymers were evaluated for effects on the bioactivity of ergotamine tartrate (ETA). Polymers were first evaluated using isotherms. Lateral saphenous veins were collected from 17 steers for four independent studies: dose response of ETA, adsorbent dose response, validation of pre-myograph incubation conditions and MIP/ non-molecularly imprinted polymer (NIP) comparison...
January 30, 2018: Toxins
Yung-Chu Hsu, Kao-Chang Lin, Treatment Guideline Subcommittee Of Taiwan Headache Society Taiwan Headache Society
In 2015, the American Headache Society (AHS) amended the treatment guideline of acute migraine based on evidence-based medicine (EBM) that all triptans in any form of preparations, acetaminophen, and non-steroid anti-inflammation drugs-NSAID (aspirin, diclofenac, ibuprofen, naproxen), sumatriptan/naproxen, combined acetaminophen/aspirin/caffeine are considered effective (Level A). Previously effective drugs as prochlorperazine, and dihydroergotamine-DHE (excluded inhaled form) were downrated to probable effective (Level B)...
June 15, 2017: Acta Neurologica Taiwanica
Chu-Ling Chen, Yi-Chun Yeh, Yen-Yu Chen
OBJECTIVE: The aim of this study was to investigate the pattern of ergotamine prescription and overuse in Taiwan. BACKGROUND: Ergotamine is a frequently prescribed medication for the treatment of migraine, although excessive use may lead to medication-overuse headache. METHODS: We conducted a retrospective cohort study by using the Longitudinal Health Insurance Database 2005 in Taiwan. Patients enrolled in the study were between the ages of 18 and 80 years, received at least two prescriptions of ergotamine, and follow-up for more than 1 year at outpatient clinics during 1999 to 2013...
March 2018: Headache
D S Antonelo, N A Lancaster, S Melnichenko, C R Muegge, J P Schoonmaker
Three experiments were conducted to determine the effect of increasing concentrations of a smectite clay on toxin binding capacity, ruminal fermentation, diet digestibility, and growth of feedlot cattle. In Exp. 1, 72 Angus × Simmental steers were blocked by BW (395 ± 9.9 kg) and randomly allotted to 3 treatments (4 pens/treatment and 6 steers/pen) to determine the effects of increasing amounts of clay (0, 1, or 2%) on performance. The clay was top-dressed on an 80% concentrate diet at a rate of 0, 113, or 226 g/steer daily to achieve the 0, 1, and 2% treatments, respectively...
October 2017: Journal of Animal Science
Karolis Kluonaitis, Elena Petrauskiene, Kristina Ryliskiene
According to Eurolight project's results, frequency of medication overuse headache in Lithuania is similar to other European countries. However, data on the characteristics of the disorder is lacking. OBJECTIVE: The aim was to analyze clinical characteristics and overuse patterns of patients with medication overuse headache. PATIENTS AND METHODS: Retrospective study was conducted in out-patient department of university hospital. 57.0% of the patients were from Vilnius and 43...
December 2017: Clinical Neurology and Neurosurgery
M Yu Maksimova, T Yu Сhochlova, L A Mota
Rebound headache (RH) is a chronic daily headache which occurs when analgesics, triptans, ergotamines are taken frequently (more than 15 days/month for more than 3 months) to relieve headaches. The prevalence of RH is 1 to 4% in the general population. RH commonly occurs in patients with migraine and tension-type headache. The deficit of central sensitization and psychological factors play an important role in initiating and maintaining of RH. Treatment of noofen for 2 months is effective in 75% of patients with RH...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Madeleine Gross, Valeriu Curtui, Ewald Usleber
Four sets of polyclonal antibodies against ergot alkaloids ergometrine, ergotamine, α-ergocryptine, and ergocornine were produced and characterized in a competitive direct or indirect enzyme immunoassay (EIA). Standard curve LODs were 0.03 ng/mL (ergometrine EIA) to 2.0 ng/mL (ergocornine EIA). Three EIAs were highly specific, whereas the ergometrine EIA had a broad specificity pattern and reacted, albeit weakly, with all seven major ergot alkaloids and their epimeric forms. Using the ergometrine EIA, a generic test system was established in which total ergot alkaloids are quantified by a standard curve for a toxin mixture composed of three alkaloids that matched the ergot alkaloid composition in naturally contaminated rye and wheat products...
October 2, 2017: Journal of AOAC International
Laura Ciaffi, Sinata Koulla-Shiro, Adrien Bruno Sawadogo, Cheik Tidiane Ndour, Sabrina Eymard-Duvernay, Pretty Rosereine Mbouyap, Liliane Ayangma, Jacques Zoungrana, Ndeye Fatou Ngom Gueye, Mohamadou Diallo, Suzanne Izard, Guillaume Bado, Coumba Toure Kane, Avelin Fobang Aghokeng, Martine Peeters, Pierre Marie Girard, Vincent Le Moing, Jacques Reynes, Eric Delaporte
BACKGROUND: Despite satisfactory efficacy of WHO-recommended second-line antiretroviral treatment for patients with HIV in low-income countries, the need for simplified, low-cost, and less-toxic maintenance strategies remains high. We compared boosted protease inhibitor monotherapy with dual therapy with boosted protease inhibitor plus lamivudine in patients on second-line antiretrovial therapy (ART). METHODS: We did a multicentre, randomised, parallel, open-label, superiority, trial in the HIV services of five hospitals in sub-Saharan Africa (Yaoundé, Cameroon; Dakar, Senegal; and Bobo Dioulasso, Burkina Faso)...
September 2017: Lancet HIV
E Kowalczyk, E Patyra, A Grelik, K Kwiatek
A high performance liquid chromatography combined with fluorescence detection (HPLC-FLD) method was developed for determination of five ergot alkaloids (EA): ergometrine, ergotamine, ergocornine, ergocrypine and ergocristine in animal feedingstuffs. The method was based on the application of QuEChERS salts for extraction and modified QuEChERS dispersive SPE for the cleanup step. Alkaloids separation was performed on a C18, 250 mm x 4.6 mm, 5 μm column with the mobile phase containing ammonium carbonate and acetonitrile...
September 1, 2016: Polish Journal of Veterinary Sciences
James L Klotz, Glen E Aiken, Jessica R Bussard, Andrew P Foote, David L Harmon, Ben M Goff, F Neal Schrick, James R Strickland
Previous research has indicated that serotonergic and α-adrenergic receptors in peripheral vasculature are affected by exposure of cattle grazing toxic endophyte-infected (E+; Epichlöe coenophialia) tall fescue (Lolium arundinaceum). The objective of this experiment was to determine the period of time necessary for the vascular effects of ergot alkaloids to subside. Two experiments were conducted to investigate changes in vascular contractile response and vasoconstriction over time relative to removal from an ergot alkaloid-containing E+ tall fescue pasture...
September 22, 2016: Toxins
Shinji Kishimoto, Michio Sato, Yuta Tsunematsu, Kenji Watanabe
Varieties of alkaloids are known to be produced by various organisms, including bacteria, fungi and plants, as secondary metabolites that exhibit useful bioactivities. However, understanding of how those metabolites are biosynthesized still remains limited, because most of these compounds are isolated from plants and at a trace level of production. In this review, we focus on recent efforts in identifying the genes responsible for the biosynthesis of those nitrogen-containing natural products and elucidating the mechanisms involved in the biosynthetic processes...
August 18, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jordi Navarro, Adrian Curran, Joaquin Burgos, Ariadna Torrella, Inma Ocaña, Vicenç Falcó, Manuel Crespo, Esteban Ribera
An HIV-infected patient treated with tenofovir disoproxil fumarate/emtricitabine/elvitegravir/cobicistat developed severe acute ischaemia of both legs during a migraine episode. After being interrogated he admitted taking an ergotamine-containing preparation. Ergotism due to interaction between ergotics and cobicistat was diagnosed. We describe the first reported case of this interaction.
2017: Antiviral Therapy
Anelize Bauermeister, Fernando Armani Aguiar, Lucas Maciel Mauriz Marques, Jose Dos Santos Malta, Fábio Barros, Daniel Roberto Callejon, Anderson Rodrigo Moraes de Oliveira, Norberto Peporine Lopes
Dihydroergotamine is a semisynthetic natural product derived from ergotamine, an ergot alkaloid. It is used to treat migraines, a neurological disease characterized by recurrent moderate to severe headaches. In this work, the in vitro metabolism of dihydroergotamine was evaluated in a biomimetic phase I reaction, aiming to verify all possible formed metabolites. Dihydroergotamine was submitted to an in vitro metabolism assay using rat liver microsomes, and the metabolites were analyzed by HPLC-MS/MS. The biomimetic reactions were performed with Jacobsen catalyst for scaling up production of oxidized metabolites...
October 2016: Planta Medica
Thomas A White, Anton Barty, Wei Liu, Andrii Ishchenko, Haitao Zhang, Cornelius Gati, Nadia A Zatsepin, Shibom Basu, Dominik Oberthür, Markus Metz, Kenneth R Beyerlein, Chun Hong Yoon, Oleksandr M Yefanov, Daniel James, Dingjie Wang, Marc Messerschmidt, Jason E Koglin, Sébastien Boutet, Uwe Weierstall, Vadim Cherezov
We describe the deposition of four datasets consisting of X-ray diffraction images acquired using serial femtosecond crystallography experiments on microcrystals of human G protein-coupled receptors, grown and delivered in lipidic cubic phase, at the Linac Coherent Light Source. The receptors are: the human serotonin receptor 2B in complex with an agonist ergotamine, the human δ-opioid receptor in complex with a bi-functional peptide ligand DIPP-NH2, the human smoothened receptor in complex with an antagonist cyclopamine, and finally the human angiotensin II type 1 receptor in complex with the selective antagonist ZD7155...
August 1, 2016: Scientific Data
Guadalupe C Vidal-Cantú, Mildred Jiménez-Hernández, Héctor I Rocha-González, Carlos M Villalón, Vinicio Granados-Soto, Enriqueta Muñoz-Islas
Sumatriptan, dihydroergotamine and methysergide inhibit 1% formalin-induced nociception by activation of peripheral 5-HT1B/1D receptors. This study set out to investigate the pharmacological profile of the antinociception produced by intrathecal and intraplantar administration of ergotamine (a 5-HT1B/1D and 5-HT5A/5B receptor agonist) and valerenic acid (a partial agonist at 5-HT5A receptors). Intraplantar injection of 1% formalin in the right hind paw resulted in spontaneous flinching behavior of the injected hindpaw of female Wistar rats...
June 15, 2016: European Journal of Pharmacology
A Donnet, D Braunstein, V Pradel, V Sciortino, V Allaria-Lapierre, J Micallef, M Lanteri-Minet
OBJECTIVE: The objective of this study was to estimate and to characterize the actual patterns of ergot use and overuse in France using a drug reimbursement database. METHODS: We included all people covered by the French General Health Insurance System (GHIS) from the Provence-Alpes-Côte-d'Azur (PACA) and Corsica administrative areas who had at least one prescription of ergot between May 2010 and December 2011. All prescriptions of ergots, migraine prophylactic treatment, and psychotropic medications were extracted from the GHIS database...
March 2016: Headache
Dorota Latek, Marek Bajda, Sławomir Filipek
The recent GPCR Dock 2013 assessment of serotonin receptor 5-HT1B and 5-HT2B, and smoothened receptor SMO targets, exposed the strengths and weaknesses of the currently used computational approaches. The test cases of 5-HT1B and 5-HT2B demonstrated that both the receptor structure and the ligand binding mode can be predicted with the atomic-detail accuracy, as long as the target-template sequence similarity is relatively high. On the other hand, the observation of a low target-template sequence similarity, e...
April 25, 2016: Journal of Chemical Information and Modeling
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