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Dopamine receptor 2

Alessio Soggiu, Cristian Piras, Viviana Greco, Paola Devoto, Andrea Urbani, Luigino Calzetta, Marco Bortolato, Paola Roncada
The enzyme 5α-reductase (5αR) catalyzes the conversion of progesterone and testosterone into neuroactive steroids implicated in a wide array of behavioral functions. The prototypical 5αR inhibitor, finasteride (FIN), is clinically approved for the treatment of androgenic alopecia and benign prostatic hyperplasia. Recent evidence has shown that FIN, albeit generally well tolerated, can induce untoward psychological effects in a subset of patients; furthermore, this drug may have therapeutic efficacy for a number of different neuropsychiatric conditions, ranging from Tourette syndrome to schizophrenia...
October 6, 2016: Psychoneuroendocrinology
Adele Bahar, Zahra Kashi, Ezzatossadat Daneshpour, Ozra Akha, Shahram Ala
BACKGROUND: Cabergoline is a long-acting agonist of dopamine, which has a high affinity to dopamine receptors (type 2). Treatment using a dopaminergic agonist reduces hypothalamic stimulation that increases during liver gluconeogenesis, lipids synthesis, and insulin resistance. Our aim was to evaluate the effects of cabergoline on blood glucose levels in patients with type 2 diabetes mellitus (DM). METHODS: This study was a double-blind, controlled clinical trial in patients with type 2 DM...
October 2016: Medicine (Baltimore)
Amrita A Gugale, Pradnya Milind Bhalerao
BACKGROUND: Postoperative nausea and vomiting (PONV) is a common occurrence after laparoscopic surgeries. A number of pharmacological agents (antihistamines, butyrophenones, dopamine receptor antagonists) have been tried of which the 5-hydroxytryptamine type 3 receptor antagonists are devoid of most side effects and highly effective in prevention and treatment of PONV. Thus, we evaluated the effectiveness of granisetron and palonosetron in prevention of PONV after laparoscopic surgeries under general anesthesia...
September 2016: Anesthesia, Essays and Researches
Gregory N Ruegsegger, Jacob D Brown, M Cathleen Kovarik, Dennis K Miller, Frank W Booth
The mesolimbic dopamine and opioid systems are postulated to influence the central control of physical activity motivation. We utilized selectively bred rats for high (HVR) or low (LVR) voluntary running behavior to examine 1) inherent differences in mu-opioid receptor (Oprm1) expression and function in the nucleus accumbens (NAc), 2) if dopamine-related mRNAs, wheel-running, and food intake are differently influenced by intraperitoneal (i.p.) naltrexone injection in HVR and LVR rats, and 3) if dopamine is required for naltrexone-induced changes in running and feeding behavior in HVR rats...
October 12, 2016: Neuroscience
Meg Waraczynski, Samantha Abbott, Alex V Schultz
Previous work in our laboratory has shown that stimulating D2 dopamine receptors in the central sublenticular extended amygdala (SLEAc) can render medial forebrain bundle (MFB) stimulation less rewarding. One of the many ways in which D2 stimulation could affect the activity status of SLEAc neurons is by indirectly blocking calcium ion (Ca(2+)) influx through CaV1.3 channels. He we directly investigate the effects of blocking CaV1.3 channels on the rewarding effect of MFB stimulation. In experiment one, CaV1...
October 12, 2016: Behavioural Brain Research
Astra S Bryant, Anna K Greenwood, Scott A Juntti, Allie E Byrne, Russell D Fernald
Dopamine regulates reproduction in part by modulating neuronal activity within the hypothalamic-pituitary-gonadal (HPG) axis. Previous studies suggested numerous mechanisms by which dopamine exerts inhibitory control over the HPG axis, ultimately changing the levels of sex steroids that regulate reproductive behaviors. However, it is not known whether these mechanisms are conserved across vertebrate species. In particular, it is unknown whether mechanisms underlying dopaminergic control of reproduction are shared between mammals and teleost fish...
October 14, 2016: Journal of Experimental Biology
Chrislean Jun Botanas, Seong Shoon Yoon, June Bryan de la Peña, Irene Joy Dela Peña, Mikyung Kim, Taeseon Woo, Joung-Wook Seo, Choon-Gon Jang, Kyung-Tae Park, Young Hun Lee, Yong Sup Lee, Hee Jin Kim, Jae Hoon Cheong
The recreational use of synthetic cathinones has grown rapidly which prompted concerns from legal authorities and health care providers. However, in response to legislative regulations, synthesis of novel synthetic cathinones by introducing substituents in cathinone molecule has dramatically increased the diversity of these substances. Based on current trends, the aromatic ring is one of the popular sites in cathinone molecule being explored by designer-type modifications. In this study, we designed and synthesized a novel synthetic cathinone, 2-(methylamino)-1-(naphthalen-2-yl) propan-1-one (BMAPN), which has a naphthalene substituent on the aromatic ring...
October 10, 2016: Behavioural Brain Research
Nathaniel B Bone, Zhongyu Liu, Jean-Francois Pittet, Jaroslaw W Zmijewski
Catecholamines, including β-adrenergic and dopaminergic neurotransmitters, have an essential role in regulating the "fight or flight" reflex and also affects immune cell proinflammatory action. However, little is known about whether catecholamines prevent dysfunction of metabolic pathways associated with inflammatory organ injury, including development of acute lung injury (ALI). We hypothesize that selected catecholamines may reduce metabolic alterations in LPS-stimulated macrophages and in the lungs of mice subjected to endotoxin-induced ALI, a situation characterized by diminished activity of AMP-activated protein kinase (AMPK)...
October 12, 2016: Journal of Leukocyte Biology
Hannah Twarkowski, Denise Manahan-Vaughan
Neuromodulation by means of the catecholaminergic system is a key component of motivation-driven learning and behaviorally modulated hippocampal synaptic plasticity. In particular, dopamine acting on D1/D5 receptors and noradrenaline acting on beta-adrenergic receptors exert a very potent regulation of forms of hippocampal synaptic plasticity that last for very long-periods of time (>24 h), and occur in conjunction with novel spatial learning. Antagonism of these receptors not only prevents long-term potentiation (LTP) and long-term depression (LTD), but prevents the memory of the spatial event that, under normal circumstances, leads to the perpetuation of these plasticity forms...
2016: Frontiers in Synaptic Neuroscience
Ken Ikeda, Takehisa Hirayama, Takanori Takazawa, Kiyokazu Kawabe, Yasuo Iwasaki
Objective Parkinson's disease (PD) is characterized by the progressive degeneration of the nigrostriatal dopaminergic neurons. Rotigotine is a non-ergot dopamine receptor agonist (DA). Its transdermal patch maintains the effective concentrations for 24 hours. Freezing of gait (FOG) is a common and devastating symptom in PD patients. Little is known about therapeutic effects of rotigotine on FOG in PD patients. Herein we compared how three non-ergot DAs of rotigotine, pramipexole LA and ropinirole CR influence FOG, besides classical motor deficits in PD patients...
2016: Internal Medicine
Anna Niewiarowska-Sendo, Andrzej Kozik, Ibeth Guevara-Lora
Kinin peptides ubiquitously occur in nervous tissue and participate in inflammatory processes associated with distinct neurological disorders. These substances have also been demonstrated to promote the oxidative stress. On the other hand, the importance of oxidative stress and inflammation has been emphasized in disorders that involve the neurodegenerative processes such as Parkinson's disease (PD). A growing number of reports have demonstrated the increased expression of kinin receptors in neurodegenerative diseases...
2016: Mediators of Inflammation
A Acharjee, R Chaube, K P Joy
The commercial fish spawning inducer Ovaprim (OVP) containing a salmon gonadotropin-releasing hormone analogue and domperidone (a dopamine receptor-2 antagonist) has been widely used as an effective spawning inducer in artificial breeding of fishes. It induces a preovulatory LH surge resulting in final oocyte maturation (FOM) and ovulation through a mechanism involving a steroidogenic shift to secrete a maturation-inducing steroid (MIS). In the present study, a 0.5μL/g body weight dose of OVP each injected at 0h and 24h intraperitoneally into gravid female catfish, Heteropneustes fossilis resulted in periovulatory changes in gonadotropin (GtH) subunit gene expression and steroid hormone levels...
October 5, 2016: General and Comparative Endocrinology
Ting Ting Zhao, Keon Sung Shin, Hyun Jin Park, Kyung Sook Kim, Kung Eun Lee, Yoon Jeong Cho, Myung Koo Lee
This study investigated the effects of (-)-sesamin on memory deficits induced by chronic electric footshock (EF)-induced stress in mice. Mice were treated with (-)-sesamin (25 and 50mg/kg, p.o., daily for 21day) prior to chronic EF stress (0.6mA, 1s every 5s for 3min, daily for 21day). Transfer retention latencies in the elevated plus maze test and N-methyl-D-aspartate (NMDA) receptor (type 1) phosphorylation in the hippocampus increased with chronic EF stress, and they were reduced by treatment with (-)-sesamin at both doses...
October 4, 2016: Neuroscience Letters
Pelle L Ishøy, Filip K Knop, Brian V Broberg, Nikolaj Bak, Ulrik B Andersen, Niklas R Jørgensen, Jens J Holst, Birte Y Glenthøj, Bjørn H Ebdrup
AIMS: Schizophrenia is associated with cardiovascular co-morbidity and a reduced life-expectancy of up to 20 years. Antipsychotics are dopamine D2 receptor antagonists and the standard of medical care in schizophrenia, but the drugs are associated with severe metabolic side effects like obesity and diabetes. Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are registered for treatment of both obesity and type 2 diabetes. We investigated metabolic effects of the GLP-1RA, exenatide once-weekly, in non-diabetic, antipsychotic-treated, obese patients with schizophrenia...
September 26, 2016: Diabetes, Obesity & Metabolism
Travis T Wager, Thomas A Chappie, David Horton, Ramalakshmi Y Chandrasekaran, Brian M Samas, Elizabeth Dunn-Sims, Cathleen Hsu, Nawshaba Nawreen, Michelle A Vanase-Frawley, Rebecca E O'Connor, Christopher Schmidt, Keith Dlugolenski, Nancy C Stratman, Mark J Majchrzak, Bethany L Kormos, David Nguyen, Aarti Sawant-Basak, Andy N Mead
Dopamine receptor antagonism is a compelling molecular target for the treatment of a range of psychiatric disorders, including substance use disorders. From our corporate compound file we identified a structurally unique D3 receptor (D3R) antagonist scaffold, 1. Through a hybrid approach, we merged key pharmacophore elements from 1 and D3 agonist 2 to yield the novel D3R/D2R antagonist PF-4363467 (3). Compound 3 was designed to possess CNS drug-like properties as defined by its CNS MPO desirability score (≥4/6)...
October 7, 2016: ACS Chemical Neuroscience
Seon Joo Park, Seung Hwan Lee, Heehong Yang, Chul Soon Park, Chang-Soo Lee, Oh Seok Kwon, Tai Hyun Park, Jyongsik Jang
In the brain and central nervous system, dopamine plays a crucial function as a neurotransmitter or a local chemical messenger for interneuronal communication. Dopamine is associated with renal, hormonal, and cardiovascular systems. Additionally, dopamine dysfunction is known to cause serious illnesses, such as Parkinson's disease and Alzheimer's disease. Therefore, dopamine detection is essential for medical diagnosis and disease prevention, which require a novel strategy with high sensitivity and selectivity, and with a rapid response...
October 7, 2016: ACS Applied Materials & Interfaces
Robert E Chapin, Douglas J Ball, Zaher A Radi, Steven W Kumpf, Petra H Koza-Taylor, David M Potter, W Mark Vogel
Tofacitinib is an oral Janus kinase (JAK) inhibitor for the treatment of rheumatoid arthritis. Tofacitinib preferentially inhibits receptor signaling through JAK3 and JAK1, relative to JAK2. In the 2-year rat carcinogenicity study, there were tofacitinib, dose-related increases in the incidences of testicular Leydig cell hyperplasia and benign adenomas in male rats, and decreased incidences of mammary tumors and duct dilatation/galactocele in female rats. Such findings in rats are typical of agents, such as dopamine agonists, which decrease prolactin (PRL) activity...
October 5, 2016: Toxicological Sciences: An Official Journal of the Society of Toxicology
X G Zhang, H Zhang, X L Liang, Q Liu, H Y Wang, B Cao, J Cao, S Liu, Y J Long, W Y Xie, D Z Peng
Maternal post-traumatic stress disorder (PTSD) increases the risk of adverse neurodevelopmental outcomes in the child. Epigenetic alternations may play an essential role in the negative effects of PTSD. This study was aimed to investigate the possible epigenetic alterations of maternal PTSD, which underpins the developmental and behavioral impact. 24 pregnant Sprague-Dawley (SD) rats were randomly grouped into PTSD and control groups. Open-field tests (OFTs), elevated pull maze (EPM) assays, gene expression profile chip tests, and methylated DNA immunoprecipitation sequencing (MeDIP-Seq) were performed on the offsprings 30 days after birth...
August 19, 2016: Genetics and Molecular Research: GMR
D Peleg-Raibstein, G Sarker, K Litwan, S D Krämer, S M Ametamey, R Schibli, C Wolfrum
Epidemiological studies have shown an association between maternal overnutrition and increased risk of the progeny for the development of obesity as well as psychiatric disorders. Animal studies have shown results regarding maternal high-fat diet (HFD) and a greater risk of the offspring to develop obesity. However, it still remains unknown whether maternal HFD can program the central reward system in such a way that it will imprint long-term changes that will predispose the offspring to addictive-like behaviors that may lead to obesity...
October 4, 2016: Translational Psychiatry
Daniela Elgueta, María S Aymerich, Francisco Contreras, Andro Montoya, Marta Celorrio, Estefanía Rojo-Bustamante, Eduardo Riquelme, Hugo González, Mónica Vásquez, Rafael Franco, Rodrigo Pacheco
Neuroinflammation involves the activation of glial cells, which is associated to the progression of neurodegeneration in Parkinson's disease. Recently, we and other researchers demonstrated that dopamine receptor D3 (D3R)-deficient mice are completely refractory to neuroinflammation and consequent neurodegeneration associated to the acute intoxication with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). In this study we examined the therapeutic potential and underlying mechanism of a D3R-selective antagonist, PG01037, in mice intoxicated with a chronic regime of administration of MPTP and probenecid (MPTPp)...
September 28, 2016: Neuropharmacology
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