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dopamine 5 receptor

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https://www.readbyqxmd.com/read/27922607/endocytosis-following-dopamine-d2-receptor-activation-is-critical-for-neuronal-activity-and-dendritic-spine-formation-via-rabex-5-pdgfr%C3%AE-signaling-in-striatopallidal-medium-spiny-neurons
#1
N Shioda, Y Yabuki, Y Wang, M Uchigashima, T Hikida, T Sasaoka, H Mori, M Watanabe, M Sasahara, K Fukunaga
Aberrant dopamine D2 receptor (D2R) activity is associated with neuropsychiatric disorders, making those receptors targets for antipsychotic drugs. Here, we report that novel signaling through the intracellularly localized D2R long isoform (D2LR) elicits extracellular signal-regulated kinase (ERK) activation and dendritic spine formation through Rabex-5/platelet-derived growth factor receptor-β (PDGFRβ)-mediated endocytosis in mouse striatum. We found that D2LR directly binds to and activates Rabex-5, promoting early-endosome formation...
December 6, 2016: Molecular Psychiatry
https://www.readbyqxmd.com/read/27903793/the-serotonin-5-ht2c-receptor-and-the-non-addictive-nature-of-classic-hallucinogens
#2
REVIEW
Clinton E Canal, Kevin S Murnane
Classic hallucinogens share pharmacology as serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptor agonists. Unique among most other Schedule 1 drugs, they are generally non-addictive and can be effective tools in the treatment of addiction. Mechanisms underlying these attributes are largely unknown. However, many preclinical studies show that 5-HT2C agonists counteract the addictive effects of drugs from several classes, suggesting this pharmacological property of classic hallucinogens may be significant. Drawing from a comprehensive analysis of preclinical behavior, neuroanatomy, and neurochemistry studies, this review builds rationale for this hypothesis, and also proposes a testable, neurobiological framework...
November 15, 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/27902847/food-deprivation-facilitates-reinstatement-of-morphine-induced-conditioned-place-preference-role-of-intra-accumbal-dopamine-d2-like-receptors-in-associating-reinstatement-of-morphine-cpp-with-stress
#3
Fatemeh Sadeghzadeh, Vahab Babapour, Abbas Haghparast
The high rate of relapse to drug use is one of the main problems in the treatment of addiction. Stress plays the essential role in drug abuse and relapse; nevertheless, little is known about the mechanisms underlying stress and relapse. Accordingly, the effects of intra-accumbal administration of Sulpiride, as a dopamine D2-like receptor antagonist, on an ineffective morphine dose+food deprivation(FD)- and morphine priming-induced reinstatement of conditioned place preference (CPP). 104 adult male albino Wistar rats weighing 200-280g were bilaterally implanted by cannula into the nucleus accumbens (NAc)...
November 30, 2016: Synapse
https://www.readbyqxmd.com/read/27901187/interactions-between-prolactin-and-kisspeptin-to-control-reproduction
#4
Jose Donato, Renata Frazão
Prolactin is best known for its effects of stimulating mammary gland development and lactogenesis. However, prolactin is a pleiotropic hormone that is able to affect several physiological functions, including fertility. Prolactin receptors (PRLRs) are widely expressed in several tissues, including several brain regions and reproductive tract organs. Upon activation, PRLRs may exert prolactin's functions through several signaling pathways, although the recruitment of the signal transducer and activator of transcription 5 causes most of the known effects of prolactin...
November 24, 2016: Archives of Endocrinology and Metabolism
https://www.readbyqxmd.com/read/27901065/pharmacological-characterization-of-a-high-affinity-p-tyramine-transporter-in-rat-brain-synaptosomes
#5
Mark D Berry, Shannon Hart, Anthony R Pryor, Samantha Hunter, Danielle Gardiner
p-Tyramine is an archetypal member of the endogenous family of monoamines known as trace amines, and is one of the endogenous agonists for trace amine-associated receptor (TAAR)1. While much work has focused on the function of TAAR1, very little is known about the regulation of the endogenous agonists. We have previously reported that p-tyramine readily crosses lipid bilayers and that its release from synaptosomes is non-exocytotic. Such release, however, showed characteristics of modification by one or more transporters...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27900635/somatostatin-and-dopamine-receptor-regulation-of-pituitary-somatotroph-adenomas
#6
REVIEW
Anat Ben-Shlomo, Ning-Ai Liu, Shlomo Melmed
Somatostatin and dopamine receptors are expressed in normal and tumoral somatotroph cells. Upon receptor stimulation, somatostatin and the somatostatin receptor ligands octreotide, lanreotide, and pasireotide, and to a lesser extent, dopamine and the dopamine analogs bromocriptine and cabergoline, suppress growth hormone (GH) secretion from a GH-secreting pituitary somatotroph adenoma. Somatostatin and dopamine receptors are Gαi-protein coupled that inhibit adenylate cyclase activity and cAMP production and reduce intracellular calcium concentration and calcium flux oscillations...
November 29, 2016: Pituitary
https://www.readbyqxmd.com/read/27886063/d-lysergic-acid-diethylamide-lsd-as-a-model-of-psychosis-mechanism-of-action-and-pharmacology
#7
REVIEW
Danilo De Gregorio, Stefano Comai, Luca Posa, Gabriella Gobbi
d-Lysergic Acid Diethylamide (LSD) is known for its hallucinogenic properties and psychotic-like symptoms, especially at high doses. It is indeed used as a pharmacological model of psychosis in preclinical research. The goal of this review was to understand the mechanism of action of psychotic-like effects of LSD. We searched Pubmed, Web of Science, Scopus, Google Scholar and articles' reference lists for preclinical studies regarding the mechanism of action involved in the psychotic-like effects induced by LSD...
November 23, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27882999/activation-of-ventral-tegmental-area-5-ht2c-receptors-reduces-incentive-motivation
#8
Lourdes Valencia-Torres, Cristian M Olarte-Sánchez, David J Lyons, Teodora Georgescu, Megan Greenwald-Yarnell, Martin G Myers, Christopher M Bradshaw, Lora K Heisler
Obesity is primarily due to food intake in excess of the body's energetic requirements, intake that is not only associated with hunger but also the incentive value of food. The 5-hydroxytryptamine 2C receptor (5-HT2CR) is a target for the treatment of human obesity. Mechanistically, 5-HT2CRs are positioned to influence both homeostatic feeding circuits within the hypothalamus and reward circuits within the ventral tegmental area (VTA). Here we investigated the role of 5-HT2CRs in incentive motivation using a mathematical model of progressive ratio (PR) responding in mice...
November 24, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27882537/neurochemical-and-behavioral-effects-of-hypidone-hydrochloride-yl-0919-a-novel-combined-selective-serotonin-reuptake-inhibitor-and-partial-5-ht1a-agonist
#9
Li-Ming Zhang, Xiao-Yun Wang, Nan Zhao, Yu-Lu Wang, Xiao-Xu Hu, Yu-Hua Ran, Yan-Qin Liu, You-Zhi Zhang, Ri-Fang Yang, Yun-Feng Li
The purpose of the present study was to investigate the pharmacology of hypidone hydrochloride (YL-0919), a novel selective serotonin reuptake inhibitor (SSRI) and 5-hydroxytryptamine (5-HT)1A receptor agonist with high affinity for serotonin transporter (SERT) and 5-HT1A receptors. YL-0919 promoted [(35) S]GTPγ S binding at 85% of the magnitude of the full 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), suggesting that YL-0919 is a high-efficacy partial agonist of 5-HT1A receptors...
November 24, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27872695/reduction-of-the-morphine-maintenance-by-blockade-of-the-nmda-receptors-during-extinction-period-in-conditioned-place-preference-paradigm-of-rats
#10
Ali Siahposht-Khachaki, Zahra Fatahi, Abbas Haghparast
INTRODUCTION: Activation of N-methyl-d-aspartate (NMDA) glutamate receptors in the nucleus accumbens is a component of drug-induced reward mechanism. In addition, NMDA receptors play a major role in brain reward system and activation of these receptors can change firing pattern of dopamine neurons. Blockade of glutamatergic neurotransmission reduces the expression of conditioned place preference (CPP) induced by morphine. Therefore, in this study, by using an NMDA receptor antagonist, DL-2-Amino-5-phosphonopentanoic acid sodium salt (AP5), the role of NMDA receptors on the maintenance and reinstatement of morphine-CPP was investigated...
October 2016: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/27870780/the-activation-of-metabotropic-glutamate-5-receptors-in-the-rat-ventral-tegmental-area-increases-dopamine-extracellular-levels
#11
Carla Ferrada, Ramón Sotomayor-Zárate, Jorge Abarca, Katia Gysling
The mesocorticolimbic circuit projects to the prefrontal cortex, hippocampus, amygdala, and nucleus accumbens, among others, and it originates in the dopaminergic neurons of the ventral tegmental area (VTA). The VTA receives glutamatergic inputs from the prefrontal cortex and several subcortical regions. The glutamate released activates dopaminergic neurons and its action depends on the activation of ionotropic and metabotropic glutamate receptors. VTA dopaminergic neurons release dopamine (DA) from axon terminals in the innervated regions and somatodendritically in the VTA itself...
January 1, 2017: Neuroreport
https://www.readbyqxmd.com/read/27866999/the-5-ht1a-1b-receptor-agonist-eltoprazine-increases-both-catecholamine-release-in-the-prefrontal-cortex-and-dopamine-release-in-the-nucleus-accumbens-and-decreases-motivation-for-reward-and-waiting-impulsivity-but-increases-stopping-impulsivity
#12
S Mechiel Korte, Jolanda Prins, Filip S Van den Bergh, Ronald S Oosting, Rudy Dupree, Gerdien A H Korte-Bouws, Koen G C Westphal, Berend Olivier, Damiaan A Denys, Alexis Garland, Onur Güntürkün
The 5-HT1A/1B-receptor agonist eltoprazine has a behavioral drug signature that resembles that of a variety of psychostimulant drugs, despite the differences in receptor binding profile. These psychostimulants are effective in treating impulsivity disorders, most likely because they increase norepinephrine (NE) and dopamine (DA) levels in the prefrontal cortex. Both amphetamine and methylphenidate, however, also increase dopamine levels in the nucleus accumbens (NAc), which has a significant role in motivation, pleasure, and reward...
November 17, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27864853/pet-radiotracer-development-for-imaging-high-affinity-state-of-dopamine-d2-and-d3-receptors-binding-studies-of-fluorine-18-labeled-aminotetralins-in-rodents
#13
Jogeshwar Mukherjee, Divya Majji, Jasmeet Kaur, Cristian C Constantinescu, Tanjore K Narayanan, Bingzhi Shi, Mohamed T Nour, Min-Liang Pan
Imaging the high-affinity, functional state (HA) of dopamine D2 and D3 receptors has been pursued in PET imaging studies of various brain functions. We report further evaluation of (18) F-5-OH-FPPAT, and the newer (18) F-5-OH-FHXPAT and (18) F-7-OH-FHXPAT. Syntheses of (18) F-5-OH-FHXPAT and (18) F-7-OH-FHXPAT were improved by modifications of our previously reported procedures. Brain slices and brain homogenates from male Sprague-Dawley rats were used with the 3 radiotracers (74-111 kBq/cc). Competition with dopamine (1-100 nM) and Gpp(NH)p (10-50 µM) were carried out to demonstrate binding to dopamine D2 and D3 HA-states and binding kinetics of (18) F-5-OH-FPPAT measured...
November 19, 2016: Synapse
https://www.readbyqxmd.com/read/27856625/longitudinal-micropet-imaging-of-the-zq175-mouse-model-of-huntington-s-disease-shows-in-vivo-changes-of-molecular-targets-in-the-striatum-and-the-cerebral-cortex
#14
Jenny Häggkvist, Miklós Tóth, Lenke Tari, Katarina Varnäs, Marie Svedberg, Anton Forsberg, Sangram Nag, Celia Dominguez, Ignacio Munoz-Sanjuan, Jonathan Bard, John Wityak, Andrea Varrone, Christer Halldin, Ladislav Mrzljak
RATIONALE: Since the discovery of the HTT gene in 1993, numerous animal models have been developed to study the progression of Huntington's disease, as well as to evaluate potential new therapeutics. In the present study we used small animal positron emission tomography (PET) to characterize the expression of molecular targets in the recently reported HD animal model, the zQ175 mouse model. METHODS: Male heterozygous zQ175 (Htttm1Mfc/190JChdi, CHDI-81003003) and wild type (WT, C57BL/6J) animals were imaged with the dopamine D2-receptor radioligand [(11)C]raclopride, the PDE10A radioligand [(18)F]MNI-659, the dopamine D1-receptor radioligand [(11)C]NNC 112 and the 5-HT2A radioligand [(11)C]MDL 100907 at 6 and 9 months of age...
November 10, 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/27853928/d1-and-d2-specific-dopamine-antagonist-modulate-the-caudate-nucleus-neuronal-responses-to-chronic-methylphenidate-exposure
#15
Sidish Venkataraman, Catherine Claussen, Nachum Dafny
The psychostimulant, methylphenidate (MPD), is the first line treatment as a pharmacotherapy to treat behavioral disorders such as attention deficit hyperactivity disorder (ADHD). MPD is commonly misused in non-ADHD (normal) youth and young adults both as a recreational drug and for cognitive enhancing effects to improve their grades. MPD is known to act on the reward circuit; including the caudate nucleus (CN). The CN is comprised of medium spiny neurons containing largely dopamine (DA) D1 and D2 receptors...
November 16, 2016: Journal of Neural Transmission
https://www.readbyqxmd.com/read/27851959/identification-of-serotonergic-neuronal-modules-that-affect-aggressive-behavior
#16
Vera Niederkofler, Tedi E Asher, Benjamin W Okaty, Benjamin D Rood, Ankita Narayan, Lara S Hwa, Sheryl G Beck, Klaus A Miczek, Susan M Dymecki
Escalated aggression can have devastating societal consequences, yet underlying neurobiological mechanisms are poorly understood. Here, we show significantly increased inter-male mouse aggression when neurotransmission is constitutively blocked from either of two subsets of serotonergic, Pet1(+) neurons: one identified by dopamine receptor D1(Drd1a)::cre-driven activity perinatally, and the other by Drd2::cre from pre-adolescence onward. Blocking neurotransmission from other Pet1(+) neuron subsets of similar size and/or overlapping anatomical domains had no effect on aggression compared with controls, suggesting subtype-specific serotonergic neuron influences on aggression...
November 15, 2016: Cell Reports
https://www.readbyqxmd.com/read/27847973/metabotropic-glutamate-receptor-5-as-a-potential-target-for-smoking-cessation
#17
REVIEW
Cristiano Chiamulera, Claudio Marcello Marzo, David J K Balfour
RATIONALE: Most habitual smokers find it difficult to quit smoking because they are dependent upon the nicotine present in tobacco smoke. Tobacco dependence is commonly treated pharmacologically using nicotine replacement therapy or drugs, such as varenicline, that target the nicotinic receptor. Relapse rates, however, remain high, and there remains a need to develop novel non-nicotinic pharmacotherapies for the dependence that are more effective than existing treatments. OBJECTIVE: The purpose of this paper is to review the evidence from preclinical and clinical studies that drugs that antagonise the metabotropic glutamate receptor 5 (mGluR5) in the brain are likely to be efficacious as treatments for tobacco dependence...
November 16, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#18
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27829813/olanzapine-induced-biochemical-and-histopathological-changes-after-its-chronic-administration-in-rats
#19
Rehmat Shah, Fazal Subhan, Gowhar Ali, Ihsan Ullah, Sami Ullah, Muhammad Shahid, Nisar Ahmad, Khwaja Fawad
Objective: Olanzapine is a second generation antipsychotic acting mainly as a dopamine D2 and serotonine 5-HT2 receptors antagonist prescribed in the treatment of schizophrenia and various other psychiatric illnesses. Even though olanzapine is widely used in psychiatry, its effects on the architecture of pancreas, liver and kidneys are little known. The histology of pancreas especially has never been studied. For these reasons, the current study was designed to elucidate the toxic effects of chronic administration of olanzapine on pancreas, liver and kidneys and the enzymes released by these tissues in an escalating dose manner...
November 2016: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/27826691/drd2-c957t-polymorphism-is-associated-with-improved-6-month-verbal-learning-following-traumatic-brain-injury
#20
John K Yue, Ethan A Winkler, Jonathan W Rick, John F Burke, Thomas W McAllister, Sam S Oh, Esteban G Burchard, Donglei Hu, Jonathan Rosand, Nancy R Temkin, Frederick K Korley, Marco D Sorani, Adam R Ferguson, Hester F Lingsma, Sourabh Sharma, Caitlin K Robinson, Esther L Yuh, Phiroz E Tarapore, Kevin K W Wang, Ava M Puccio, Pratik Mukherjee, Ramon Diaz-Arrastia, Wayne A Gordon, Alex B Valadka, David O Okonkwo, Geoffrey T Manley
Traumatic brain injury (TBI) often leads to heterogeneous clinical outcomes, which may be influenced by genetic variation. A single-nucleotide polymorphism (SNP) in the dopamine D2 receptor (DRD2) may influence cognitive deficits following TBI. However, part of the association with DRD2 has been attributed to genetic variability within the adjacent ankyrin repeat and kinase domain containing 1 protein (ANKK1). Here, we utilize the Transforming Research and Clinical Knowledge in Traumatic Brain Injury Pilot (TRACK-TBI Pilot) study to investigate whether a novel DRD2 C957T polymorphism (rs6277) influences outcome on a cognitive battery at 6 months following TBI-California Verbal Learning Test (CVLT-II), Wechsler Adult Intelligence Test Processing Speed Index Composite Score (WAIS-PSI), and Trail Making Test (TMT)...
November 8, 2016: Neurogenetics
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