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https://www.readbyqxmd.com/read/29217539/inhibition-of-cocaine-and-3-4-methylenedioxypyrovalerone-mdpv-self-administration-by-lorcaserin-is-mediated-by-5-ht2c-receptors-in-rats
#1
Brenda M Gannon, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
Lorcaserin is a serotonin (5-HT)2C receptor-preferring agonist approved by the US Food and Drug Administration to treat obesity. Lorcaserin has been shown to decrease cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB 242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. The goals of this study were to determine: (1) the potency and effectiveness of lorcaserin to decrease self-administration of cocaine and 3,4-methylenedioxypyrovalerone (MDPV), a common "bath salts" constituent; and (2) the receptor(s) mediating the effects of lorcaserin on cocaine and MDPV self-administration...
December 7, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29213077/allosteric-nanobodies-uncover-a-role-of-hippocampal-mglu2-receptor-homodimers-in-contextual-fear-consolidation
#2
Pauline Scholler, Damien Nevoltris, Dimitri de Bundel, Simon Bossi, David Moreno-Delgado, Xavier Rovira, Thor C Møller, Driss El Moustaine, Michaël Mathieu, Emilie Blanc, Heather McLean, Elodie Dupuis, Gérard Mathis, Eric Trinquet, Hervé Daniel, Emmanuel Valjent, Daniel Baty, Patrick Chames, Philippe Rondard, Jean-Philippe Pin
Antibodies have enormous therapeutic and biotechnology potential. G protein-coupled receptors (GPCRs), the main targets in drug development, are of major interest in antibody development programs. Metabotropic glutamate receptors are dimeric GPCRs that can control synaptic activity in a multitude of ways. Here we identify llama nanobodies that specifically recognize mGlu2 receptors, among the eight subtypes of mGluR subunits. Among these nanobodies, DN10 and 13 are positive allosteric modulators (PAM) on homodimeric mGlu2, while DN10 displays also a significant partial agonist activity...
December 6, 2017: Nature Communications
https://www.readbyqxmd.com/read/29209406/serum-prolactin-levels-and-sexual-dysfunction-in-patients-with-schizophrenia-treated-with-antipsychotics-comparison-between-aripiprazole-and-other-atypical-antipsychotics
#3
Eiji Kirino
Objectives: Antipsychotics, even atypical ones, can induce hyperprolactinemia. Aripiprazole (APZ), a dopamine D2 partial agonist, has a unique pharmacological profile and few side effects. We investigated the incidence of hyperprolactinemia in patients with schizophrenia treated with APZ and other antipsychotics. Methods: Serum prolactin levels were measured by ELISA (enzyme-linked immunosorbent assay). A questionnaire survey was used to evaluate subjective sexual dysfunction...
2017: Annals of General Psychiatry
https://www.readbyqxmd.com/read/29208933/the-anthelmintic-praziquantel-is-a-human-serotoninergic-g-protein-coupled-receptor-ligand
#4
John D Chan, Pauline M Cupit, Gihan S Gunaratne, John D McCorvy, Yang Yang, Kristen Stoltz, Thomas R Webb, Peter I Dosa, Bryan L Roth, Ruben Abagyan, Charles Cunningham, Jonathan S Marchant
Schistosomiasis is a debilitating tropical disease caused by infection with parasitic blood flukes. Approximately 260 million people are infected worldwide, underscoring the clinical and socioeconomic impact of this chronic infection. Schistosomiasis is treated with the drug praziquantel (PZQ), which has proved the therapeutic mainstay for over three decades of clinical use. However, the molecular target(s) of PZQ remain undefined. Here we identify a molecular target for the antischistosomal eutomer - (R)-PZQ - which functions as a partial agonist of the human serotoninergic 5HT2B receptor...
December 5, 2017: Nature Communications
https://www.readbyqxmd.com/read/29203848/bdnf-release-and-signaling-are-required-for-the-antidepressant-actions-of-glyx-13
#5
T Kato, M V Fogaça, S Deyama, X-Y Li, K Fukumoto, R S Duman
Conventional antidepressant medications, which act on monoaminergic systems, display significant limitations, including a time lag of weeks to months and low rates of therapeutic efficacy. GLYX-13 is a novel glutamatergic compound that acts as an N-methyl-d-aspartate (NMDA) modulator with glycine-like partial agonist properties; like the NMDA receptor antagonist ketamine GLYX-13 produces rapid antidepressant actions in depressed patients and in preclinical rodent models. However, the mechanisms underlying the antidepressant actions of GLYX-13 have not been characterized...
December 5, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/29202114/dihydrosanguinarine-enhances-glucose-uptake-in-mouse-3t3-l1-cells
#6
Yit-Lai Chow, Yuko Iwata, Fumihiko Sato
Recently, more studies have aimed at identifying selective peroxisome proliferator-activated receptor gamma (PPARγ) modulators that transactivate the expression of PPARγ-dependent genes as partial agonists to improve diabetic symptoms with fewer side effects compared to classic PPARγ agonists such as thiazolidinediones. We found that dihydrosanguinarine (DHS) treatment induced preadipocyte differentiation and lipid droplet accumulation in 3T3-L1 cells, but this effect is weaker than that elicited by the full PPARγ agonist troglitazone...
October 31, 2017: ACS Omega
https://www.readbyqxmd.com/read/29200912/biphasic-augmentation-of-alpha-adrenergic-contraction-by-plumbagin-in-rat-systemic-arteries
#7
Hae Jin Kim, Hae Young Yoo, Yin Hua Zhang, Woo Kyung Kim, Sung Joon Kim
Plumbagin, a hydroxy 1,4-naphthoquinone compound from plant metabolites, exhibits anticancer, antibacterial, and antifungal activities via modulating various signaling molecules. However, its effects on vascular functions are rarely studied except in pulmonary and coronary arteries where NADPH oxidase (NOX) inhibition was suggested as a mechanism. Here we investigate the effects of plumbagin on the contractility of skeletal artery (deep femoral artery, DFA), mesenteric artery (MA) and renal artery (RA) in rats...
November 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29199269/dendrogenin-a-drives-lxr-to-trigger-lethal-autophagy-in-cancers
#8
Gregory Segala, Marion David, Philippe de Medina, Mathias C Poirot, Nizar Serhan, François Vergez, Aurelie Mougel, Estelle Saland, Kevin Carayon, Julie Leignadier, Nicolas Caron, Maud Voisin, Julia Cherier, Laetitia Ligat, Frederic Lopez, Emmanuel Noguer, Arnaud Rives, Bruno Payré, Talal Al Saati, Antonin Lamaziere, Gaëtan Despres, Jean-Marc Lobaccaro, Silvere Baron, Cecile Demur, Fabienne de Toni, Clément Larrue, Helena Boutzen, Fabienne Thomas, Jean-Emmanuel Sarry, Marie Tosolini, Didier Picard, Michel Record, Christian Récher, Marc Poirot, Sandrine Silvente-Poirot
Dendrogenin A (DDA) is a newly discovered cholesterol metabolite with tumor suppressor properties. Here, we explored its efficacy and mechanism of cell death in melanoma and acute myeloid leukemia (AML). We found that DDA induced lethal autophagy in vitro and in vivo, including primary AML patient samples, independently of melanoma Braf status or AML molecular and cytogenetic classifications. DDA is a partial agonist on liver-X-receptor (LXR) increasing Nur77, Nor1, and LC3 expression leading to autolysosome formation...
December 4, 2017: Nature Communications
https://www.readbyqxmd.com/read/29198647/isolation-functional-characterization-of-allatotropin-receptor-from-the-cotton-bollworm-helicoverpa-armigera
#9
Fang Zhang, Jun Wang, Kiran Thakur, Fei Hu, Jian-Guo Zhang, Xing-Fu Jiang, Shi-Hen An, Hongbo Jiang, Li Jiang, Zhao-Jun Wei
Insect allatotropin (AT) plays multi-functions including regulation of juvenile hormone synthesis, growth, development and reproduction. In the present study, the full-length cDNA encoding the AT receptor was cloned from the brain of Helicoverpa armigera (Helar-ATR). The ORF of Helar-ATR exhibited the characteristic seven transmembrane domains of the G protein-coupled receptor (GPCR) and was close to the ATR of Manduca sexta in the phylogenetic tree. The Helar-ATR expressed in vertebrate cell lines can be activated by Helar-AT and each Helar-ATL in a dose-responsive manner, in the following order: Helar-ATLI>Helar-ATLII>Helar-AT>Helar-ATLIII...
November 30, 2017: Peptides
https://www.readbyqxmd.com/read/29197607/inflammatory-response-modulation-through-a-ppar%C3%AE-agonist-during-surgically-induced-visceral-ischemia-in-an-animal-model
#10
Bianca Pane, Valerio Gazzola, Giovanni Spinella, Paola Bagnato, Federica Grillo, Valerio Gaetano Vellone, Domenico Palombo
BACKGROUND: Ischemia / reperfusion (I/R) injury represents one of the most severe complications in vascular surgery where cross-clamping of the aorta and subsequent visceral ischemia are a recurrent issue. The literature describes a family of nuclear receptors, i.e., peroxisome-proliferator activated receptors (PPARs), in particular PPARγ isoform, which are important modulators of vascular inflammation resulting from I/R injury. The aim of our study is to evaluate how PPARγ agonist administration could reduce local and systemic inflammatory response after I/R injury during aortic supraceliac clamping in animal model...
November 29, 2017: Annals of Vascular Surgery
https://www.readbyqxmd.com/read/29195167/effects-of-short-and-long-term-aripiprazole-treatment-on-group-i-mglurs-in-the-nucleus-accumbens-comparison-with-haloperidol
#11
Jeremy S Lum, Bo Pan, Chao Deng, Xu-Feng Huang, Lezanne Ooi, Kelly A Newell
The D2 receptor partial agonist, aripiprazole, has shown increased therapeutic efficacy for schizophrenia, autism and Tourette's syndrome compared to traditional antipsychotics such as the D2 receptor antagonist, haloperidol. Recent evidence suggests this superior profile may be associated with downstream effects on glutamatergic synapses. Group 1 metabotropic glutamate receptors (mGluRs) and their endogenous modulators, Norbin and Homer1, are regulated by D2 receptor activity, particularly within the nucleus accumbens (NAc), a target region of aripiprazole and haloperidol...
November 21, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/29194351/identification-of-a-raloxifene-analog-that-promotes-ahr-mediated-apoptosis-in-cancer-cells
#12
Hyo Sang Jang, Martin Pearce, Edmond F O'Donnell, Bach Duc Nguyen, Lisa Truong, Monica J Mueller, William H Bisson, Nancy I Kerkvliet, Robert L Tanguay, Siva Kumar Kolluri
We previously reported that raloxifene, an estrogen receptor modulator, is also a ligand for the aryl hydrocarbon receptor (AhR). Raloxifene induces apoptosis in estrogen receptor-negative human cancer cells through the AhR. We performed structure-activity studies with seven raloxifene analogs to better understand the structural requirements of raloxifene for induction of AhR-mediated transcriptional activity and apoptosis. We identified Y134 as a raloxifene analog that activates AhR-mediated transcriptional activity and induces apoptosis in MDA-MB-231 human triple negative breast cancer cells...
December 1, 2017: Biology
https://www.readbyqxmd.com/read/29191726/essential-oils-of-culinary-herbs-and-spices-display-agonist-and-antagonist-activities-at-human-aryl-hydrocarbon-receptor-ahr
#13
Iveta Bartoňková, Zdeněk Dvořák
Essential oils (EOs) of culinary herbs and spices are used to flavor, color and preserve foods and drinks. Dietary intake of EOs is significant, deserving an attention of toxicologists. We examined the effects of 31 EOs of culinary herbs and spices on the transcriptional activity of human aryl hydrocarbon receptor (AhR), which is a pivotal xenobiotic sensor, having also multiple roles in human physiology. Tested EOs were sorted out into AhR-inactive ones (14 EOs) and AhR-active ones, including full agonists (cumin, jasmine, vanilla, bay leaf), partial agonists (cloves, dill, thyme, nutmeg, oregano) and antagonists (tarragon, caraway, turmeric, lovage, fennel, spearmint, star anise, anise)...
November 27, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29188556/current-and-future-challenges-in-gpcr-drug-discovery
#14
Sid Topiol
GPCRs play a pervasive physiological role and, in turn, are the leading target class for pharmaceuticals. Beginning with the determination of the structure of rhodopsin, and dramatically accelerating since the reporting of the first ligand-mediated GPCR X-ray structures, our understanding of the structural and functional characteristics of these proteins has grown dramatically. Deploying this now rapidly emerging information for drug discovery has already been extensively demonstrated through a watershed of studies appearing in numerous scientific reports...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29187337/prr-signaling-during-in-vitro-macrophage-differentiation-from-progenitors-modulates-their-subsequent-response-to-inflammatory-stimuli
#15
Alba Martínez, Cristina Bono, Javier Megías, Alberto Yáñez, Daniel Gozalbo, M Luisa Gil
Toll-like receptor (TLR) agonists drive hematopoietic stem and progenitor cells (HSPCs) to differentiate along the myeloid lineage in vitro and also in vivo following infection. In this study, we used an in vitro model of HSPC differentiation to investigate the functional consequences (cytokine production) that exposing HSPCs to various pathogen-associated molecular patterns (PAMPs) and Candida albicans cells have on the subsequently derived macrophages. Mouse HSPCs (Lin- cells) were cultured with GM-CSF to induce macrophage differentiation in the presence or absence of the following pattern recognition receptor (PRR) agonists: Pam3CSK4 (TLR2 ligand), LPS (TLR4 ligand), depleted zymosan (which only activates Dectin-1), or inactivated C...
September 1, 2017: European Cytokine Network
https://www.readbyqxmd.com/read/29184207/lateral-geniculate-neurons-projecting-to-primary-visual-cortex-show-ocular-dominance-plasticity-in-adult-mice
#16
Juliane Jaepel, Mark Hübener, Tobias Bonhoeffer, Tobias Rose
Experience-dependent plasticity in the mature visual system is widely considered to be cortical. Using chronic two-photon Ca2+ imaging of thalamic afferents in layer 1 of binocular visual cortex, we provide evidence against this tenet: the respective dorsal lateral geniculate nucleus (dLGN) cells showed pronounced ocular dominance (OD) shifts after monocular deprivation in adult mice. Most (86%), but not all, of dLGN cell boutons were monocular during normal visual experience. Following deprivation, initially deprived-eye-dominated boutons reduced or lost their visual responsiveness to that eye and frequently became responsive to the non-deprived eye...
December 2017: Nature Neuroscience
https://www.readbyqxmd.com/read/29183806/the-antagonist-properties-of-bazedoxifene-after-acute-treatment-are-shifted-to-stimulatory-action-after-chronic-exposure-in-the-liver-but-not-in-the-uterus
#17
Mélissa Buscato, Coralie Fontaine, Aurélie Fabre, Alexia Vinel, Marie-Cécile Valera, Emmanuelle Noirrit, Maeva Guillaume, Bernard Payrastre, Raphaël Métivier, Jean-François Arnal
A promising alternative to conventional hormone therapy for postmenopausal symptoms is treatment combining Bazedoxifene (BZA), a third-generation selective estrogen receptor modulator (SERM), and conjugated equine estrogen (CE). This combination is also known as a tissue-selective estrogen complex (TSEC). Understanding the tissue-specific actions of SERMs and the TSEC remains a major challenge to try to predict their clinical effects. The aim of this study was to compare acute versus chronic treatment with BZA, CE or CE + BZA in two major targets of estrogens, the uterus and the liver...
November 25, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29183588/heterologous-formation-of-neonicotinoid-sensitive-nachrs-containing-unc-38-and-unc-29-subunits-from-bursaphelenchus-xylophilus
#18
Na Yu, Yang Liu, Xuan Wang, Jian Li, Haibo Bao, Zewen Liu
Nicotinic acetylcholine receptor (nAChR) subunits are encoded by a large multigene family and generate a large number of pentameric receptors with various properties. At present, nematode species, such as Caenorhabditis elegans, have the largest number of nAChR subunits. In this study, two nAChR subunits (Bxy-Unc-38 and Bxy-Unc-29) were cloned from Bursaphelenchus xylophilus, a fatal nematode pest on pine trees causing pine wilt disease. When Bxy-Unc-38 and Bxy-Unc-29 were co-expressed in Xenopus oocytes, constructed functional nAChRs showed agonist responses to acetylcholine and imidacloprid, a neonicotinoid insecticide...
November 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/29183321/effects-of-controlled-hypoxemia-or-hypovolemia-on-global-and-intestinal-oxygenation-and-perfusion-in-isoflurane-anesthetized-horses-receiving-an-alpha-2-agonist-infusion
#19
Klaus Hopster, Liza Wittenberg-Voges, Florian Geburek, Charlotte Hopster-Iversen, Sabine B R Kästner
BACKGROUND: Aim of this prospective experimental study was to assess effects of systemic hypoxemia and hypovolemia on global and gastrointestinal oxygenation and perfusion in anesthetized horses. Therefore, we anesthetized twelve systemically healthy warmblood horses using either xylazine or dexmedetomidine for premedication and midazolam and ketamine for induction. Anesthesia was maintained using isoflurane in oxygen with either xylazine or dexmedetomidine and horses were ventilated to normocapnia...
November 28, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/29177442/increased-27-hydroxycholesterol-production-during-luteolysis-may-mediate-the-progressive-decline-in-progesterone-secretion
#20
Yafei Xu, Scot M Hutchison, José J Hernández-Ledezma, Randy L Bogan
STUDY QUESTION: Does 27-hydroxycholesterol (27OH) actively facilitate the progression of luteolysis? SUMMARY ANSWER: There is increased mRNA expression of the enzyme that produces 27OH during luteolysis in vivo in rhesus macaques and sheep, and 27OH reduces progesterone secretion from human luteinized granulosa cells. WHAT IS KNOWN ALREADY: There is an increase in mRNA expression of liver x receptor (LXR) and a decrease in sterol regulatory element binding protein 2 (SREBP2) target genes during spontaneous luteolysis in primates, which could result in reduced cholesterol availability for steroidogenesis...
November 21, 2017: Molecular Human Reproduction
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