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Dopamine antagonists

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https://www.readbyqxmd.com/read/28431434/bright-light-suppresses-form-deprivation-myopia-development-with-activation-of-dopamine-d1-receptor-signaling-in-the-on-pathway-in-retina
#1
Si Chen, Zhina Zhi, Qingqing Ruan, Qingxia Liu, Fen Li, Fen Wan, Peter S Reinach, Jiangfan Chen, Jia Qu, Xiangtian Zhou
Purpose: To determine whether dopamine receptor D1 (D1R) signaling pathway activation by bright light (BL) in specific retinal neuronal cell types contributes to inhibiting form-deprivation myopia (FDM) in mice. Methods: Mice (3-weeks old) were raised under either normal light (NL: 100-200 lux) or BL (2500-5000 lux) conditions with or without form deprivation. Refraction changes were evaluated with an eccentric infrared photorefractor, and ocular axial components with optical coherence tomography...
April 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28430979/effect-of-physical-exercise-and-acute-escitalopram-on-the-excitability-of-brain-monoamine-neurons-in-vivo-electrophysiological-study-in-rats
#2
Eliyahu Dremencov, Kristína Csatlósová, Barbora Durišová, Lucia Lapínová, Lubica Lacinová, Daniela Ježová
Background: The antidepressant effect of physical exercise has been reported in several clinical and animal studies. Since serotonin (5-HT), norepinephrine and dopamine play a central role in depression, it is possible that the beneficial effects of physical exercise are mediated via monoamine pathways. This study investigates the effects of voluntary wheel running (VWR) on the excitability of monoamine neurons. Material and methods: Male Sprague-Dawley rats were used in the study...
April 18, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28430805/effect-of-the-glucocorticoid-receptor-antagonist-ru486-on-mk-801-induced-behavioural-sensitisation
#3
Emilia M Lefevre, Gregory A Medley, Timothy Reeks, Suzy Alexander, Thomas H J Burne, Darryl W Eyles
Stress is known to modulate sensitisation to repeated psychostimulant exposure. However, there is no direct evidence linking glucocorticoids and sensitisation achieved by repeated administration of the NMDA receptor antagonist MK-801. We tested the hypothesis that co-administration of RU486, a glucocorticoid receptor (GR) antagonist, prior to repeated daily MK-801 injections would block the expression of locomotor sensitisation due to its dual effects on corticosterone and dopamine. We employed a repeated MK-801 administration locomotor sensitisation paradigm in male Sprague Dawley rats...
2017: PloS One
https://www.readbyqxmd.com/read/28428755/pharmacological-analysis-of-the-anti-epileptic-mechanisms-of-fenfluramine-in-scn1a-mutant-zebrafish
#4
Jo Sourbron, Ilse Smolders, Peter de Witte, Lieven Lagae
Dravet syndrome (DS) is a genetic encephalopathy that is characterized by severe seizures and prominent co-morbidities (e.g., physical, intellectual disabilities). More than 85% of the DS patients carry an SCN1A mutation (sodium channel, voltage gated, type I alpha subunit). Although numerous anti-epileptic drugs have entered the market since 1990, these drugs often fail to adequately control seizures in DS patients. Nonetheless, current clinical data shows significant seizure reduction in DS patients treated with the serotonergic (5-hydroxytryptamine, 5-HT) drug fenfluramine (FA)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28426179/novel-selective-and-developable-dopamine-d3-antagonists-with-modified-amino-region
#5
Fabrizio Micheli
This minireview describes the presentation made at the XXIV National Meeting in Medicinal Chemistry held in Perugia (Italy) in 2016, September 11-14. It relates to the discovery of novel templates of the so called "amino" region of the Dopamine D3 antagonists. Moving from the early scaffolds which were modified in the amine portion, the review describes the variations which led to the discovery of new systems which were published in 2016 allowing the identification of molecules endowed of great selectivity over DA D2 receptor and hERG channel...
April 20, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28424758/redox-related-epigenetic-mechanisms-in-glioblastoma-nuclear-factor-erythroid-derived-2-like-2-cobalamin-and-dopamine-receptor-subtype-4
#6
Matthew Scott Schrier, Malav Suchin Trivedi, Richard Carlton Deth
Glioblastoma is an exceptionally difficult cancer to treat. Cancer is universally marked by epigenetic changes, which play key roles in sustaining a malignant phenotype, in addition to disease progression and patient survival. Studies have shown strong links between the cellular redox state and epigenetics. Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a redox-sensitive transcription factor that upregulates endogenous antioxidant production, and is aberrantly expressed in many cancers, including glioblastoma...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28421623/a-preliminary-investigation-of-the-effect-of-acute-alcohol-on-dopamine-transmission-as-assessed-by-11-c-phno
#7
Thulasi Thiruchselvam, Alan A Wilson, Isabelle Boileau, Bernard Le Foll
BACKGROUND: Previous positron emission tomography (PET) studies exploring the effect of acute alcohol on dopamine (DA) levels have yielded inconsistent results, with only some studies suggesting increased synaptic DA levels after an alcohol challenge. The D2 /D3 agonist radiotracer, [(11) C]-(+)-propyl-hexahydro-naphtho-oxazin ([(11) C]-(+)-PHNO), has greater sensitivity to synaptic DA fluctuation than previously used antagonist radiotracers and is in principle more suitable for imaging alcohol-induced changes in DA...
April 19, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28421257/histone-deacetylase-inhibitors-reverse-age-related-increases-in-side-effects-of-haloperidol-in-mice
#8
Janitza L Montalvo-Ortiz, Daniel W Fisher, Guadalupe Rodríguez, Deyu Fang, John G Csernansky, Hongxin Dong
BACKGROUND: Older patients can be especially susceptible to antipsychotic-induced side effects, and the pharmacodynamic mechanism underlying this phenomenon remains unclear. We hypothesized that age-related epigenetic alterations lead to decreased expression and functionality of the dopamine D2 receptor (D2R), contributing to this susceptibility. METHODS: In this study, we treated young (2-3 months old) and aged (22-24 months old) C57BL/6 mice with the D2R antagonist haloperidol (HAL) once a day for 14 days to evaluate HAL-induced motor side effects...
April 18, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28419646/suvorexant-an-orexin-hypocretin-receptor-antagonist-attenuates-motivational-and-hedonic-properties-of-cocaine
#9
Taylor A Gentile, Steven J Simmons, David J Barker, Jessica K Shaw, Rodrigo A España, John W Muschamp
Orexins ('hypocretins') are peptides produced by neurons of the hypothalamus that project to structures implicated in reward and emotion processing. Converging evidence demonstrates functional roles of orexin signaling in arousal, sleep/wakefulness and motivated behaviors for natural and drug rewards. Suvorexant, a dual orexin receptor antagonist, recently received approval from the US Food and Drug Administration to treat insomnia. In Experiment 1, rats self-administered cocaine under a progressive-ratio schedule of reinforcement and the effects of suvorexant on motivation to self-administer cocaine were measured...
April 17, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28419642/nicotine-induced-molecular-alterations-are-modulated-by-gabab-receptor-activity
#10
Andres P Varani, Valeria T Pedrón, Amira J Aon, Christian Höcht, Gabriela B Acosta, Bernhard Bettler, Graciela N Balerio
It has been demonstrated that GABAB receptors modulate nicotine (NIC) reward effect; nevertheless, the mechanism implicated is not well known. In this regard, we evaluated the involvement of GABAB receptors on the behavioral, neurochemical, biochemical and molecular alterations associated with the rewarding effects induced by NIC in mice, from a pharmacological and genetic approach. NIC-induced rewarding properties (0.5 mg/kg, subcutaneously, sc) were evaluated by conditioned place preference (CPP) paradigm...
April 17, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28414989/role-of-cortical-alpha-2-adrenoceptors-in-alcohol-withdrawal-induced-depression-and-tricyclic-antidepressants
#11
Bruk Getachew, Sheketha R Hauser, Antonei B Csoka, Robert E Taylor, Yousef Tizabi
INTRODUCTION: Although a role for alpha-2 adrenoceptors (alpha-2 ARs) in alcohol use disorder (AUD) and depression is suggested, very little information on a direct interaction between alcohol and these receptors is available. METHODS: In this study adult female Wistar and Wistar-Kyoto (WKY) rats, a putative animal model of depression, were exposed to alcohol vapor 3h daily for 10days (blood alcohol concentration ∼150mg%) followed by daily injection of 10mg/kg of imipramine (IMP, a selective norepinephrine NE/serotonin reuptake inhibitor) or nomifensine (NOMI, a selective NE/dopamine reuptake inhibitor)...
April 4, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28411257/relief-of-pain-depressed-behavior-in-rats-by-activation-of-d1-like-dopamine-receptors
#12
Matthew F Lazenka, Kelen C Freitas, Sydney Henck, S Stevens Negus
Clinically significant pain often includes depression of both behavior and mesolimbic dopamine signaling. Indirect and/or direct dopamine receptor agonists may alleviate pain-related behavioral depression. To test this hypothesis, the present study compared effects of indirect and direct dopamine agonists in a preclinical assay of pain-depressed operant responding. Male Sprague-Dawley rats with chronic indwelling microelectrodes in the medial forebrain bundle were trained in an intracranial self-stimulation (ICSS) procedure to press a lever for pulses of electrical brain stimulation...
April 14, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28408289/dopaminergic-control-of-anxiety-in-young-and-aged-zebrafish
#13
Victoria Kacprzak, Neil A Patel, Elizabeth Riley, Lili Yu, Jing-Ruey J Yeh, Irina V Zhdanova
Changes in the expression of the dopamine transporter (DAT), or the sensitivity of dopamine receptors, are associated with aging and substance abuse and may underlie some of the symptoms common to both conditions. In this study, we explored the role of the dopaminergic system in the anxiogenic effects of aging and acute cocaine exposure by comparing the behavioral phenotypes of wildtype (WT) and DAT knockout zebrafish (DAT-KO) of different ages. To determine the involvement of specific dopamine receptors in anxiety states, antagonists to D1 (SCH23390) and D2/D3 (sulpiride) were employed...
April 10, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28407578/a-peek-into-the-drug-development-scenario-of-endometriosis-a-systematic-review
#14
REVIEW
Luxitaa Goenka, Melvin George, Maitrayee Sen
PURPOSE AND OBJECTIVE: Endometriosis is a gynaecological disease that is characterised by the presence of endometrium like tissue-epithelium and stroma that develops outside the uterine cavity, which is responsible for pelvic pain and infertility. Even though several medical therapies exist for the treatment of endometriosis, each of the drug class has its own limitations such as cost of treatment, side-effects and its short-term effect on the symptoms of endometriosis. In this review, we have attempted to summarize the current status and challenges of drug development for endometriosis...
April 10, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28406051/antidepressant-like-deliverables-from-the-sea-evidence-on-the-efficacy-of-three-different-brown-seaweeds-via-involvement-of-monoaminergic-system
#15
Pirzada Jamal Ahmed Siddiqui, Adnan Khan, Nizam Uddin, Saima Khaliq, Munawwer Rasheed, Shazia Nawaz, Muhammad Hanif, Ahsana Dar
Brown seaweeds exhibit several health benefits in treating and managing wide array of ailments. In this study, the antidepressant-like effect of methaolic extracts from Sargassum swartzii (SS), Stoechospermum marginatum (SM), and Nizamuddinia zanardinii (NZ) was examined in forced swimming test (FST), in rats. Oral administration of SS, SM, and NZ extract (30-60 mg/kg) exhibited antidepressant-like activity in FST by reducing immobility time as compared to control group, without inducing significant change in ambulatory behavior in open field test...
April 13, 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/28404742/autonomic-nervous-system-activation-mediates-the-increase-in-whole-body-glucose-uptake-in-response-to-electroacupuncture
#16
Anna Benrick, Milana Kokosar, Min Hu, Martin Larsson, Manuel Maliqueo, Rodrigo Rodrigues Marcondes, Marzia Soligo, Virginia Protto, Elisabet Jerlhag, Antonina Sazonova, Carl Johan Behre, Kurt Højlund, Peter Thorén, Elisabet Stener-Victorin
A single bout of low-frequency electroacupuncture (EA) causing muscle contractions increases whole-body glucose uptake in insulin-resistant rats. We explored the underlying mechanism of this finding and whether it can be translated into clinical settings. Changes in glucose infusion rate (GIR) were measured by euglycemic-hyperinsulinemic clamp during and after 45 min of low-frequency EA in 21 overweight/obese women with polycystic ovary syndrome (PCOS) and 21 controls matched for age, weight, and body mass index (experiment 1) and in rats receiving autonomic receptor blockers (experiment 2)...
April 12, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28403913/brilliant-blue-g-but-not-fenofibrate-treatment-reverts-hemiparkinsonian-behavior-and-restores-dopamine-levels-in-an-animal-model-of-parkinson-s-disease
#17
Enéas G Ferrazoli, Héllio D N de Souza, Isis C Nascimento, Ágatha Oliveira-Giacomelli, Telma T Schwindt, Luiz R Britto, Henning Ulrich
Parkinson's disease (PD) is a neurodegenerative disorder, characterized by the loss of dopaminergic neurons in the substantia nigra and their projections to the striatum. Several processes have been described as potential inducers of the dopaminergic neuron death, such as inflammation, oxidative stress, and mitochondrial dysfunction. However, the death of dopaminergic neurons seems to be multifactorial, and its cause remains unclear. ATP-activating purinergic receptors influence various physiological functions in the CNS, including neurotransmission...
April 13, 2017: Cell Transplantation
https://www.readbyqxmd.com/read/28400256/n-oleoyldopamine-modulates-activity-of-midbrain-dopaminergic-neurons-through-multiple-mechanisms
#18
Olga A Sergeeva, Roberto De Luca, Karolina Mazur, Aissa N Chepkova, Helmut L Haas, Andreas Bauer
N-oleoyl-dopamine (OLDA) is an amide of dopamine and oleic acid, synthesized in catecholaminergic neurons. The present study investigates OLDA targets in midbrain dopaminergic (DA) neurons. Substantia Nigra compacta (SNc) DA neurons recorded in brain slices were excited by OLDA in wild type mice. In transient receptor potential vanilloid 1 (TRPV1) knockout (KO) mice, however, SNc DA neurons displayed sustained inhibition of firing. In the presence of the dopamine type 2 receptor (D2R) antagonist sulpiride or the dopamine transporter blocker nomifensine no such inhibition was observed...
April 9, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28398653/the-noble-gas-xenon-provides-protection-and-trophic-stimulation-to-midbrain-dopamine-neurons
#19
Jérémie Lavaur, Déborah Le Nogue, Marc Lemaire, Jan Pype, Géraldine Farjot, Etienne C Hirsch, Patrick P Michel
Despite its low chemical reactivity, the noble gas xenon possesses a remarkable spectrum of biological effects. In particular, xenon is a strong neuroprotectant in preclinical models of hypoxic-ischemic brain injury. In the present study, we wished to determine whether xenon retained its neuroprotective potential in experimental settings that model the progressive loss of midbrain dopamine (DA) neurons in Parkinson's disease (PD). Using rat midbrain cultures, we established that xenon was partially protective for DA neurons through either direct or indirect effects on these neurons...
April 11, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28396142/atypical-binding-at-dopamine-and-serotonin-transporters-contribute-to-the-discriminative-stimulus-effects-of-mephedrone
#20
Alyssa F DeLarge, Laura L Erwin, Peter J Winsauer
Mephedrone (4-methylmethcathinone), a constituent of the recreational substances known as "bath salts", is a synthetic cathinone that can produce auditory and visual hallucinations, as well as problematic cardiovascular effects. This study compared the discriminative stimulus effects of mephedrone (0.32-10 mg/kg) with other prototypical drugs of abuse: cocaine (0.56-32 mg/kg), d-amphetamine (0.18-3.2 mg/kg), ketamine (1.8-18 mg/kg), phencyclidine (PCP, 1-5.6 mg/kg), heroin (1-10 mg/kg), 2,5-dimethoxy-4-iodoamphetamine (R-DOI, 0...
April 7, 2017: Neuropharmacology
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