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https://www.readbyqxmd.com/read/28839342/efficacy-of-valbenazine-nbi-98854-in-treating-subjects-with-tardive-dyskinesia-and-schizophrenia-or-schizoaffective-disorder
#1
John M Kane, Christoph U Correll, Grace S Liang, Joshua Burke, Christopher F O'Brien
BACKGROUND: Valbenazine (VBZ, NBI-98854) is a novel vesicular monoamine transporter 2 (VMAT2) inhibitor approved for the treatment of tardive dyskinesia (TD). The KINECT 3 study (NCT02274558) evaluated the effects of VBZ on TD in subjects with schizophrenia/schizoaffective disorder (SCHZ) or mood disorder (mood disorder presented separately) who received up to 48 weeks of treatment. METHODS: KINECT 3 included: 6-week, double-blind, placebo (PBO)-controlled (DBPC) period (205 completers); 42-week VBZ extension (VE) period (124 completers): 4-week washout period (121 completers)...
August 1, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/28839340/efficacy-of-valbenazine-nbi-98854-in-treating-subjects-with-tardive-dyskinesia-and-mood-disorder
#2
Christoph U Correll, Richard C Josiassen, Grace S Liang, Joshua Burke, Christopher F O'Brien
BACKGROUND: Valbenazine (VBZ, NBI-98854) is a novel vesicular monoamine transporter 2 (VMAT2) inhibitor approved for the treatment of tardive dyskinesia (TD). The KINECT 3 study (NCT02274558) evaluated the effects of VBZ on TD in subjects with mood disorder or schizophrenia/schizoaffective disorder (SCHZ, presented separately) who received up to 48 weeks of treatment. METHODS: KINECT 3 included: 6-week, double-blind, placebo (PBO)-controlled (DBPC) period (205 completers); 42-week VBZ extension (VE) period (124 completers); 4-week washout period (121 completers)...
August 1, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/28839339/single-dose-and-repeat-once-daily-dose-safety-tolerability-and-pharmacokinetics-of-valbenazine-in-healthy-male-subjects
#3
Rosa Luo, Haig Bozigian, Roland Jimenez, Gordon Loewen, Christopher F O'Brien
Valbenazine (VBZ) is a vesicular monoamine transporter 2 (VMAT2) inhibitor approved for the treatment of tardive dyskinesia. The safety, tolerability and pharmacokinetics of VBZ following single and repeat once-daily (QD) dosing were evaluated in 2 randomized, single-center, double-blind studies in healthy male subjects. In the first study, 2 cohorts of 8 subjects were administered single doses (SD) of placebo (PBO; N = 2/period) or VBZ (N = 6/period; 1, 2, 5, or 12.5 mg for Cohort 1 and 12.5, 25, 50, or 75 mg for Cohort 2) using a sequential escalation scheme...
August 1, 2017: Psychopharmacology Bulletin
https://www.readbyqxmd.com/read/28830769/plasmalogen-precursor-mitigates-striatal-dopamine-loss-in-mptp-mice
#4
Edith Miville-Godbout, Mélanie Bourque, Marc Morissette, Sara Al-Sweidi, Tara Smith, Dushmanthi Jayasinghe, Shawn Ritchie, Thérèse Di Paolo
Ethanolamine plasmalogens (PlsEtn) are a class of glycerophospholipids characterized by a vinyl-ether bond at the sn-1 position that play an important role in the structure and function of membranes. Previous reports have suggested a link between reduced blood and brain PlsEtn levels and Parkinson's disease (PD). We recently reported that the DHA containing plasmalogen precursor PPI-1011 protected striatal dopamine (DA) against MPTP toxicity in mice. In this paper, we further investigate the specificity requirements of the lipid side chains by testing the oleic acid-containing plasmalogen precursor PPI-1025...
August 19, 2017: Brain Research
https://www.readbyqxmd.com/read/28776237/differences-in-dihydrotetrabenazine-isomer-concentrations-following-administration-of-tetrabenazine-and-valbenazine
#5
Heather Skor, Evan B Smith, Gordon Loewen, Christopher F O'Brien, Dimitri E Grigoriadis, Haig Bozigian
BACKGROUND: Tetrabenazine (TBZ) activity is thought to result from four isomeric dihydrotetrabenazine (HTBZ) metabolites ([+]-α-HTBZ, [-]-α-HTBZ, [+]-β-HTBZ, [-]-β-HTBZ). Each isomer has a unique profile of vesicular monoamine transporter 2 (VMAT2) inhibition and off-target binding. Previously published data only report total isomer (α) and (β) concentrations. We developed a method to quantify the individual HTBZ isomers in samples from patients with Huntington's disease receiving TBZ...
August 3, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28743955/early-synaptic-dysfunction-induced-by-%C3%AE-synuclein-in-a-rat-model-of-parkinson-s-disease
#6
Jenny-Ann Phan, Kathrine Stokholm, Justyna Zareba-Paslawska, Steen Jakobsen, Kim Vang, Albert Gjedde, Anne M Landau, Marina Romero-Ramos
Evidence suggests that synapses are affected first in Parkinson's disease (PD). Here, we tested the claim that pathological accumulation of α-synuclein, and subsequent synaptic disruption, occur in absence of dopaminergic neuron loss in PD. We determined early synaptic changes in rats that overexpress human α-synuclein by local injection of viral-vectors in midbrain. We aimed to achieve α-synuclein levels sufficient to induce terminal pathology without significant loss of nigral neurons. We tested synaptic disruption in vivo by analyzing motor defects and binding of a positron emission tomography (PET) radioligand to the vesicular monoamine transporter 2, (VMAT2), [(11)C]dihydrotetrabenazine (DTBZ)...
July 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28699794/valbenazine-for-the-treatment-of-tardive-dyskinesia
#7
Lauren C Seeberger, Robert A Hauser
Tardive dyskinesia (TD) is a hyperkinetic movement disorder that may result from treatment with antipsychotics or other dopamine receptor blocking agents. Underlying pathophysiology is incompletely understood but since the 1970s dopamine depleting agents have been used to reduce involuntary movements. The search for safe, effective treatments for TD is ongoing. Valbenazine, a novel VMAT2 inhibitor, has recently been FDA approved for treatment of TD. Areas covered: An overview of TD, unmet medical needs and current treatment guidelines are presented...
August 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28637871/phosphorylation-at-serine-31-targets-tyrosine-hydroxylase-to-vesicles-for-transport-along-microtubules
#8
Ana Jorge-Finnigan, Rune Kleppe, Kunwar Jung-Kc, Ming Ying, Michael Marie, Ivan Rios-Mondragon, Michael F Salvatore, Jaakko Saraste, Aurora Martinez
Tyrosine hydroxylase (TH) catalyzes the conversion of l-tyrosine into l-DOPA, which is the rate-limiting step in the synthesis of catecholamines, such as dopamine, in dopaminergergic neurons. Low dopamine levels and death of the dopaminergic neurons are hallmarks of Parkinson's disease (PD), where α-synuclein is also a key player. TH is highly regulated, notably by phosphorylation of several Ser/Thr residues in the N-terminal tail. However, the functional role of TH phosphorylation at the Ser-31 site (THSer(P)-31) remains unclear...
August 25, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28627368/photoactivation-of-erk-creb-vmat2-pathway-attenuates-mpp-induced-neuronal-injury-in-a-cellular-model-of-parkinson-s-disease
#9
Xiaotong Gu, Lei Liu, Qi Shen, Da Xing
The vesicular monoamine transporter 2 (VMAT2) pumps dopamine from cytoplasm into synaptic vesicles for subsequent release, and the deficits of VMAT2 has been implicated in the dopaminergic neuronal cell loss which is considered as a typical pathological feature of Parkinson's disease (PD). Low-power laser irradiation (LPLI), a potent noninvasive physiotherapy approach, is capable of penetrating into nerve tissue to exert beneficial effects such as promoting nerve regeneration and ATP production. In the present study, we demonstrated that LPLI protects against MPP(+)-induced neurotoxicity via upregulation of VMAT2 in SH-SY5Y human dopaminergic neuroblastoma cells...
June 13, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28623006/a-longevity-study-with-enhancer-substances-selegiline-bpap-detected-an-unknown-tumor-manifestation-suppressing-regulation-in-rat-brain
#10
J Knoll, K Baghy, S Eckhardt, P Ferdinandy, M Garami, L G Harsing, P Hauser, Z Mervai, T Pocza, Z Schaff, D Schuler, I Miklya
AIMS: First proof to show that (-)-deprenyl/selegiline (DEP), the first selective inhibitor of MAO-B, later identified as the first β-phenylethylamine (PEA)-derived synthetic catecholaminergic activity enhancer (CAE) substance and (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP), the tryptamine-derived presently known most potent, selective, synthetic enhancer substance, are specific markers of unknown enhancer-sensitive brain regulations. MAIN METHODS: Longevity study disclosing the operation of tumor-manifestation-suppressing (TMS) regulation in rat brain...
August 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/28596586/storage-of-neural-histamine-and-histaminergic-neurotransmission-is-vmat2-dependent-in-the-zebrafish
#11
Henri A J Puttonen, Svetlana Semenova, Maria Sundvik, Pertti Panula
Monoaminergic neurotransmission is greatly dependent on the function of the vesicular monoamine transporter VMAT2, which is responsible for loading monoamines into secretory vesicles. The role of VMAT2 in histaminergic neurotransmission is poorly understood. We studied the structure and function of the histaminergic system in larval zebrafish following inhibition of VMAT2 function by reserpine. We found that reserpine treatment greatly reduced histamine immunoreactivity in neurons and an almost total disappearance of histamine-containing nerve fibers in the dorsal telencephalon and habenula, the most densely innervated targets of the hypothalamic histamine neurons...
June 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28578484/valbenazine-first-global-approval
#12
REVIEW
Esther S Kim
Valbenazine (Ingrezza™) is an orally bioavailable, selective, vesicular monoamine transporter 2 (VMAT2) inhibitor being developed by Neurocrine Biosciences for the treatment of various central nervous system disorders. Valbenazine has been approved in the USA for the treatment of adults with tardive dyskinesia (TD), is at various stages of development in other countries for TD and is in phase 2 development in the USA for Tourette syndrome. This article summarizes the milestones in the development of valbenazine leading to its first global approval in the USA for the treatment of adults with TD...
July 2017: Drugs
https://www.readbyqxmd.com/read/28560316/vmat2-mediated-neurotransmission-from-midbrain-leptin-receptor-neurons-in-feeding-regulation
#13
Yuanzhong Xu, Yungang Lu, Pingwen Xu, Leandra R Mangieri, Elsa Isingrini, Yong Xu, Bruno Giros, Qingchun Tong
Leptin receptors (LepRs) expressed in the midbrain contribute to the action of leptin on feeding regulation. The midbrain neurons release a variety of neurotransmitters including dopamine (DA), glutamate and GABA. However, which neurotransmitter mediates midbrain leptin action on feeding remains unclear. Here, we showed that midbrain LepR neurons overlap with a subset of dopaminergic, GABAergic and glutamatergic neurons. Specific removal of vesicular monoamine transporter 2 (VMAT2) in midbrain LepR neurons (KO mice) disrupted DA accumulation in vesicles, but failed to cause a significant change in the evoked release of either glutamate or GABA to downstream neurons...
May 2017: ENeuro
https://www.readbyqxmd.com/read/28497864/valbenazine-for-tardive-dyskinesia-a-systematic-review-of-the-efficacy-and-safety-profile-for-this-newly-approved-novel-medication-what-is-the-number-needed-to-treat-number-needed-to-harm-and-likelihood-to-be-helped-or-harmed
#14
REVIEW
Leslie Citrome
OBJECTIVE: The objective of this systematic review was to describe the efficacy, tolerability, and safety of valbenazine for the treatment of tardive dyskinesia (TD). DATA SOURCES: The pivotal registration trials were accessed by querying http://www.ncbi.nlm.nih.gov/pubmed/ and http://www.clinicaltrials.gov, for the search terms 'valbenazine' OR 'NBI-98854', and by also querying the EMBASE (Elsevier) commercial database for clinical poster abstracts, and by asking the manufacturer for copies of posters presented at congresses...
May 12, 2017: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/28495607/prenatal-exposure-to-lambda-cyhalothrin-alters-brain-dopaminergic-signaling-in-developing-rats
#15
Yogesh K Dhuriya, Pranay Srivastava, Rajendra K Shukla, Richa Gupta, Dhirendra Singh, Devendra Parmar, Aditya B Pant, Vinay K Khanna
The present study is focused to decipher the molecular mechanisms associated with dopaminergic alterations in corpus striatum of developing rats exposed prenatally to lambda-cyhalothrin (LCT), a new generation type II synthetic pyrethroid. There was no significant change in the mRNA and protein expression of DA-D1 receptors at any of the doses of LCT (0.5, 1 and 3mg/kg body weight) in corpus striatum of developing rats exposed prenatally to LCT on PD22 and PD45. Prenatal exposure to LCT (1 and 3mg/kg body weight) resulted to decrease the levels of mRNA and protein of DA-D2 receptors in corpus stratum of developing rats on PD22 as compared to controls...
July 1, 2017: Toxicology
https://www.readbyqxmd.com/read/28490469/management-impact-of-imaging-brain-vesicular-monoamine-transporter-type-2-vmat2-in-clinically-uncertain-parkinsonian-syndrome-cups-with-18-f-av133-and-pet
#16
Paschal Kevin Alexander, Yennie Lie, Gareth Jones, Chomalaven Sivaratnam, Svetlana Bozinovski, Rachel S Mulligan, Kenneth Young, Victor Luis Villemagne, Christopher C Rowe
Objectives: Idiopathic Parkinson's disease (iPD) is a common neurodegenerative disorder where misdiagnosis occurs in up to 30% of patients after initial assessment and in 10-15% even after long-term follow-up. Vesicular monoamine transporter type II (VMAT2) imaging with Positron Emission Tomography (PET) allows assessment of the integrity of the presynaptic dopaminergic pathway. We investigated the management impact of VMAT2 imaging in patients with Clinically Uncertain Parkinsonian Syndromes (CUPS). Methods: Forty-seven patients with CUPS (56...
May 10, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28464229/functional-characterization-of-the-neuron-restrictive-silencer-element-in-the-human-tryptophan-hydroxylase-2-gene-expression
#17
Yukino Nawa, Hanae Kaneko, Masayuki Oda, Masaaki Tsubonoya, Tomoko Hiroi, Maria Teresa Gentile, Luca Colucci-D'Amato, Ryoya Takahashi, Hiroaki Matsui
Tryptophan hydroxylase 2 (TPH2) is the key enzyme in the synthesis of neuronal serotonin. Although previous studies suggest that TPH2 NRSE (neuron-restrictive silencer element) functions as a negative regulator dependent on NRSF (neuron-restrictive silencer factor) activity, the underlying mechanisms are yet to be fully elucidated. Here, we show a detailed analysis of the NRSE-mediated repression of the human TPH2 (hTPH2) promoter activity in RN46A cells, a cell line derived from rat raphe neurons. Quantitative real-time RT-PCR analysis revealed the expression of serotonergic marker genes (Mash1, Nkx2...
May 2, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28456940/mptp-mouse-model-of-preclinical-and-clinical-parkinson-s-disease-as-an-instrument-for-translational-medicine
#18
Eduard R Mingazov, Gulnara R Khakimova, Elena A Kozina, Alexei E Medvedev, Olga A Buneeva, Ara S Bazyan, Michael V Ugrumov
Parkinson's disease (PD) is characterized by the appearance of motor symptoms many years after the onset of neurodegeneration, which explains low efficiency of therapy. Therefore, one of the priorities in neurology is to develop an early diagnosis and preventive treatment of PD, based on knowledge of molecular mechanisms of neurodegeneration and neuroplasticity in the nigrostriatal system. However, due to inability to diagnose PD at preclinical stage, research and development must be performed in animal models by comparing the nigrostriatal system in the models of asymptomatic and early symptomatic stages of PD...
April 29, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28454718/effects-of-co-administration-of-ketamine-and-ethanol-on-the-dopamine-system-via-the-cortex-striatum-circuitry
#19
Qing Liu, Tian-Yong Xu, Zhi-Bi Zhang, Chi-Kwan Leung, Ding-Yun You, Shang-Wen Wang, Shuai Yi, Qiang Jing, Run-Fang Xie, Huifang-Jie Li, Xiao-Feng Zeng
AIM: Ketamine and ethanol are increasingly being used together as recreational drugs in rave parties. Their effects on the dopamine (DA) system remain largely unknown. This study aimed to investigate the effects of consuming two different concentrations of ketamine with and without alcohol on the DA system. MATERIALS AND METHODS: We employed the conditioned place preference (CPP) paradigm to evaluate the rewarding effects of the combined administration of two different doses of ketamine (30mg/kg and 60mg/kg) with ethanol (0...
June 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28451991/-18-f-fp-dtbz-pet-study-in-a-lactacystin-treated-rat-model-of-parkinson-disease
#20
Chi-Chang Weng, Siao-Lan Huang, Zi-An Chen, Kun-Ju Lin, Ing-Tsung Hsiao, Tzu-Chen Yen, Mei-Ping Kung, Shiaw-Pyng Wey, Ching-Han Hsu
OBJECTIVE: Lactacystin has been used to establish rodent models of Parkinson disease (PD), with cerebral α-synuclein inclusions. This study evaluated the uptake of [(18)F]9-fluoropropyl-(+)-dihydrotetrabenazine ([(18)F]FP-(+)-DTBZ), a vesicular monoamine transporter type 2 (VMAT2)-targeting radiotracer, through positron emission tomography (PET) in lactacystin-treated rat brains. METHODS: Adult male Sprague-Dawley rats were randomly treated with a single intracranial dose of lactacystin (2 or 5 μg) or saline (served as the sham control) into the left medial forebrain bundle...
April 27, 2017: Annals of Nuclear Medicine
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