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https://www.readbyqxmd.com/read/28542034/dopamine-d2-receptor-affinity-of-antipsychotics-in-relation-to-subjective-well-being-in-patients-with-a-psychotic-disorder
#1
Iris E de Wit, Floor A van Dijk, Carin J Meijer, Mirjam J van Tricht, Lieuwe de Haan
Dopamine D2-receptor blockade by antipsychotic medication reduces psychotic symptoms, but may reduce subjective well-being. The current study aims to further explore the relation between dopamine D2-receptor affinity and subjective well-being within a large sample of patients with psychotic disorders. Patients participated in a longitudinal naturalistic cohort study: the Genetic Risk and Outcome of Psychosis (GROUP) study. Three groups of antipsychotic medication were created on the basis of their affinity for the D2-receptor: (i) loose or partial agonistic binding, (ii) moderate binding, and (iii) tight binding...
May 24, 2017: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28537214/pharmacokinetic-drug-evaluation-of-safinamide-mesylate-for-the-treatment-of-mid-to-late-stage-parkinson-s-disease
#2
Thomas Müller
Patients with Parkinson's disease suffer from a heterogeneous expression of neurotransmitter deficits. They cause an individual variable expression of motor and non-motor symptoms. Thus, drugs with various mechanisms of actions are suitable to counteract these disease related neurotransmitter alterations. Areas covered: This invited review suggests safinamide as an ideal compound for therapy of Parkinson's disease, as its pharmacological profile includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent sodium channels, modulation of calcium channels and abnormal glutamate release...
June 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28536511/aripiprazole-facilitates-extinction-of-conditioned-fear-in-adolescent-rats
#3
Despina E Ganella, Liubov Lee-Kardashyan, Sophia J Luikinga, Danny L D Nguyen, Heather B Madsen, Isabel C Zbukvic, Russell Coulthard, Andrew J Lawrence, Jee Hyun Kim
Anxiety disorders are the most common type of mental disorder during adolescence, which is at least partly due to the resistance to extinction exhibited at this age. The dopaminergic system is known to be dysregulated during adolescence; therefore, we aimed to facilitate extinction in adolescent rats using the dopamine receptor 2 partial agonist aripiprazole (Abilify™), and examine the behavioral and neural outcomes. Adolescent rats were conditioned to fear a tone. The next day, rats received extinction 30 min after a systemic injection of either 5 mg/kg aripiprazole or vehicle, and then were tested the following day...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28533164/a-novel-iron-ii-preferring-dopamine-agonist-chelator-d-607-significantly-suppresses-%C3%AE-syn-and-mptp-induced-toxicities-in-vivo
#4
Banibrata Das, Subramanian Rajagopalan, Gnanada S Joshi, Liping Xu, Dan Luo, Julie K Andersen, Sokol V Todi, Aloke K Dutta
Here, we report the characterization of a novel hybrid D2/D3 agonist and iron (II) specific chelator, D-607, as a multi-target-directed ligand against Parkinson's disease (PD). In our previously published report, we showed that D-607 is a potent agonist of dopamine (DA) D2/D3 receptors, exhibits efficacy in a reserpinized PD animal model and preferentially chelates to iron (II). As further evidence of its potential as a neuroprotective agent in PD, the present study reveals D-607 to be protective in neuronal PC12 cells against 6-OHDA toxicity...
May 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28531297/mechanisms-of-kappa-opioid-receptor-potentiation-of-dopamine-d2-receptor-function-in-quinpirole-induced-locomotor-sensitization-in-rats
#5
Angélica P Escobar, Marcela P González, Rodrigo C Meza, Verónica Noches, Pablo Henny, Katia Gysling, Rodrigo A España, José A Fuentealba, María E Andrés
Background: Increased locomotor activity in response to the same stimulus is an index of behavioral sensitization observed in preclinical models of drug addiction and compulsive behaviors. Repeated administration of Quinpirole (QNP), a D2/D3 dopamine agonist, induces locomotor sensitization. This effect is potentiated and accelerated by co-administration of U69593, a kappa opioid receptor agonist (KOR). The mechanism underlying KOR potentiation of QNP-induced locomotor sensitization remains to be elucidated...
May 22, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28531264/cariprazine-exhibits-anxiolytic-and-dopamine-d3-receptor-dependent-antidepressant-effects-in-the-chronic-stress-model
#6
Vanya Duric, Mounira Banasr, Tina Franklin, Ashley Lepack, Nika Adham, Béla Kiss, István Gyertyán, Ronald S Duman
Background: Cariprazine, a D3-preferring dopamine D2/D3 receptor partial agonist, is a new antipsychotic drug recently approved in the US for the treatment of schizophrenia and bipolar mania. We recently demonstrated that cariprazine also has significant anti-anhedonic-like effects in rats subjected to chronic stress; however, the exact mechanism of action for cariprazine's antidepressant-like properties is not known. Thus, in this study we examined whether the effects of cariprazine are mediated by dopamine D3 receptors...
May 22, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28523537/prolactinoma-management-predictors-of-remission-and-recurrence-after-dopamine-agonists-withdrawal
#7
Margarida Teixeira, Pedro Souteiro, Davide Carvalho
OBJECTIVE: Prolactinomas are the most common functional pituitary tumour. Dopamine agonists (DA) are its principal treatment. The criteria that should guide therapy withdrawal and the factors that influence disease remission or relapse are not yet fully established. Our purpose is to evaluate the proportion of patients who attempted DA withdrawal, and to identify the factors that influence clinicians to try it. In addition, we aim to study the factors that are involved in prolactinoma remission/relapse after therapy withdrawal...
May 18, 2017: Pituitary
https://www.readbyqxmd.com/read/28522313/neurotensin-in-the-nucleus-accumbens-reverses-dopamine-supersensitivity-evoked-by-antipsychotic-treatment
#8
Alice Servonnet, Ellie-Anna Minogianis, Claude Bouchard, Anne-Marie Bédard, Daniel Lévesque, Pierre-Paul Rompré, Anne-Noël Samaha
Long-term exposure to antipsychotics like haloperidol can increase sensitivity to dopamine agonist stimulation. This could contribute to treatment failure and increase relapse to psychosis. Chronic antipsychotic treatment elevates neurotensin levels in the nucleus accumbens (NAc), where the neuropeptide modulates dopamine function by signalling through NTS1 receptors. We hypothesized that increasing neurotensin activity in the NAc attenuates the expression of antipsychotic-induced dopamine supersensitivity, which is indicated by a potentiated psychomotor response to amphetamine...
May 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28521736/clinical-characteristics-of-impulse-control-and-related-disorders-in-chinese-parkinson-s-disease-patients
#9
Yu Zhang, An Qi He, Lin Li, Wei Chen, Zhen Guo Liu
BACKGROUND: Impulse control and related disorders (ICRDs) are clinically complications in Parkinson's disease (PD). However, the clinical characteristics of ICRDs in Chinese PD patients were rarely reported. We aimed to explore the prevalence and the clinical profile of ICRDs in Chinese patients with PD. METHODS: 142 Chinese PD patients were consecutively enrolled. The symptoms of ICRDs were assessed with the Questionnaire for Impulsive-Compulsive Disorders. The clinical characteristics of patients with ICRDs and without ICRDs were compared...
May 18, 2017: BMC Neurology
https://www.readbyqxmd.com/read/28520722/altered-detrusor-contractility-in-mptp-treated-common-marmosets-with-bladder-hyperreflexia
#10
Sara Pritchard, Michael J Jackson, Atsuko Hikima, Lisa Lione, Christopher D Benham, K Ray Chaudhuri, Sarah Rose, Peter Jenner, Mahmoud M Iravani
Bladder hyperreflexia is a common non-motor feature of Parkinson's disease. We now report on the contractility of the isolated primate detrusor strips devoid of nerve input and show that following MPTP, the amplitude and frequency of spontaneous contraction was increased. These responses were unaffected by dopamine D1 and D2 receptor agonists A77636 and ropinirole respectively. Contractions by exogenous carbachol, histamine or ATP were similar and no differences in the magnitude of noradrenaline-induced relaxation were seen in detrusor strip obtained from normal and MPTP-treated common marmosets (Callithrix jacchus)...
2017: PloS One
https://www.readbyqxmd.com/read/28516479/g%C3%AE-s-signalling-of-the-cb1-receptor-and-the-influence-of-receptor-number
#11
David B Finlay, Erin E Cawston, Natasha L Grimsey, Morag R Hunter, Anisha Korde, V Kiran Vemuri, Alexandros Makriyannis, Michelle Glass
BACKGROUND AND PURPOSE: CB1 cannabinoid receptor signalling is canonically mediated through inhibitory Gαi proteins, but signalling through other G proteins occurs under some circumstances; Gαs being the most characterised secondary pathway. Determinants of this signalling switch identified to date include Gαi blockade, CB1 /D2 dopamine receptor co-stimulation, CB1 agonist class, and cell background. The aim of this study was to examine the effects of receptor number and ligand dependence on CB1 signalling...
May 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28516430/ramelteon-improves-post-traumatic-stress-disorder-like-behaviors-exhibited-by-fatty-acid-binding-protein-3-null-mice
#12
Yasushi Yabuki, Ibuki Takahata, Kazuya Matsuo, Yuji Owada, Kohji Fukunaga
We previously reported that fatty acid-binding protein 3 (FABP3) knockout (Fabp3 (-/-)) mice exhibit abnormal dopamine-related behaviors such as enhanced dopamine D2 receptor antagonist-induced catalepsy behaviors. Here, we report that Fabp3 null mice exhibit cognitive deficits, hyperlocomotion and impaired fear extinction, and thus show post-traumatic stress disorder (PTSD)-like behaviors. Notably, chronic administration of ramelteon (1.0 mg/kg, p.o.), a melatonin receptor agonist, improved all PTSD-like behaviors tested in Fabp3 (-/-) mice...
May 17, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28515684/selegiline-ameliorates-depression-like-behavior-in-mice-lacking-the-cd157-bst1-gene-a-risk-factor-for-parkinson-s-disease
#13
Satoka Kasai, Toru Yoshihara, Olga Lopatina, Katsuhiko Ishihara, Haruhiro Higashida
Parkinson's disease (PD), a neurodegenerative disorder, is accompanied by various non-motor symptoms including depression and anxiety, which may precede the onset of motor symptoms. Selegiline is an irreversible monoamine oxidase-B (MAO-B) inhibitor, and is widely used in the treatment of PD and major depression. However, there are few reports about the effects of selegiline on non-motor symptoms in PD. The aim of this study was to explore the antidepressant and anxiolytic effects of selegiline, using CD157/BST1 knockout (CD157 KO) mouse, a PD-related genetic model displaying depression and anxiety, compared with other antiparkinsonian drugs and an antidepressant, and was to investigate the effects of selegiline on biochemical parameters in emotion-related brain regions...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28514338/-a-comparative-chemoreactome-analysis-of-mexidol
#14
I Yu Torshin, O A Gromova, I S Sardaryan, L E Fedotova
AIM: To compare mexidol with control molecules (choline alfoscerate, piracetam, glycine, semax) using chemoreactome analysis. MATERIAL AND METHODS: The chemical structure of mexidol was compared to molecule metabolites extracted from the Human Metabolome Database (HMDB) and a drug database. More than 40 000 of metabolites from HMDB were used as a model of human metabolome. RESULTS AND CONCLUSION: The chemoreactome analysis showed that mexidol may be (1) an agonist of acetylcholine and GABA-A receptors; (2) an anti-inflammatory agent, the effects of which are carried out by inhibiting the synthesis of pro-inflammatory prostaglandins; (3) a neurotrophic agent with neuroprotective properties; (4) a coagulation inhibitor; (5) a diabetes medication and (6) a hypolipidemic agent...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/28514334/-anxiety-and-depressive-disorders-in-parkinson-s-disease
#15
G N Akhmadeeva, R V Magzhanov, G N Tayupova, A R Bajtimerov, I M Hidijatova
This review presents the most recent data of worldwide research on anxiety and depressive disorders in patients with Parkinson's disease. Their characteristics and epidemiology, pathogenetic and clinical features, methods of diagnosis and treatment are presented. Depression occurs in 40-50% of patients with PD, anxiety in 17-43% of patients. Pramipexole, a dopamine agonist, is only one drug recommended for depression treatment. Nortriptyline and desipramine, belonging to the group of tricyclic antidepressants (TCAs), are considered to be possibly effective...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/28513757/-new-drugs-for-horses-and-production-animals-in-2016
#16
Ilka Ute Emmerich
In 2016, only one newly developed active pharmaceutical ingredient for horses and food-producing animals was released on the German market for veterinary drug products. The immunomodulator Pegbovigrastim is now available as an injection solution for cattle (Imrestor(®)). Four established veterinary active pharmaceutical ingredients are available for further species: the ectoparasitic Amitraz (Apitraz(®)) from the triazapentadiene group was additionally authorized for honeybees, the expectorant Bromhexine (Exflow(®) Vet) for chickens, turkeys and ducks and the macrolide antibiotic Gamithromycin (Zactran(®)) for pigs...
May 17, 2017: Tierärztliche Praxis. Ausgabe G, Grosstiere/Nutztiere
https://www.readbyqxmd.com/read/28511976/fertility-pregnancy-and-prolactinoma-a-survey-of-pituitary-surgeons-view-and-review-of-the-literature
#17
Walter C Jean, Daniel R Felbaum
OBJECTIVE: Pituitary surgeons frequently encounter female prolactinoma patients seeking treatment to restore fertility. Current medical guidelines recommend using dopamine agonist (DA) for this, but for fetal safety, DA should stop upon pregnancy confirmation. The probability that prolactinoma may grow during pregnancy makes this last recommendation imperfect. With the advances in endoscopic surgery, we queried the potential role for surgery in these infertile patients, who may be ambivalent about both stopping and continuing DA while pregnant...
May 13, 2017: Journal of Clinical Neuroscience: Official Journal of the Neurosurgical Society of Australasia
https://www.readbyqxmd.com/read/28511259/impulse-control-disorders-and-related-complications-of-parkinson-s-disease-therapy
#18
Alexander M Lopez, Daniel Weintraub, Daniel O Claassen
Impulsive and compulsive behaviors in Parkinson's disease (PD) patients are most often attributed to dopamine agonist therapy; dysregulation of the mesocorticolimbic system accounts for this behavioral phenotype. The clinical presentation is commonly termed impulse control disorder (ICD): Behaviors include hypersexuality, compulsive eating, shopping, pathological gambling, and compulsive hobby participation. However, not all PD individuals taking dopamine agonists develop these behavioral changes. In this review, the authors focus on the similarities between the phenotypic presentation of ICDs with that of other reward-based behavioral disorders, including binge eating disorder, pathological gambling, and substance use disorders...
April 2017: Seminars in Neurology
https://www.readbyqxmd.com/read/28511252/diagnosis-and-management-of-parkinson-s-disease
#19
Arjun Tarakad, Joseph Jankovic
Despite numerous efforts to identify specific and sensitive biomarkers, the diagnosis of Parkinson's disease (PD) is still based on clinical criteria that include the presence of a combination of cardinal motor features (tremor, rigidity, bradykinesia, and postural instability), other motor features (including freezing of gait and abnormal postures), and numerous nonmotor features. In addition, the presence of atypical features may suggest an alternative diagnosis. Levodopa therapy remains the gold standard in the management of motor features of PD...
April 2017: Seminars in Neurology
https://www.readbyqxmd.com/read/28507321/pet-imaging-of-dopamine-d2-receptor-internalization-in-schizophrenia
#20
J J Weinstein, E van de Giessen, R J Rosengard, X Xu, N Ojeil, G Brucato, R B Gil, L S Kegeles, M Laruelle, M Slifstein, A Abi-Dargham
Recent genetic, molecular and post-mortem studies suggest impaired dopamine (DA)-D2 receptor (D2R) trafficking in patients with schizophrenia (SZ). Imaging and preclinical studies have shown agonist-induced D2R internalization can be imaged with positron emission tomography (PET) using D2R radiotracers combined with psychostimulant challenge. This is feasible if radiotracer binding is measured when postchallenge DA levels have returned to baseline, following the initial competition phase between DA and radiotracer for binding to D2R...
May 16, 2017: Molecular Psychiatry
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