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https://www.readbyqxmd.com/read/28196430/first-in-human-trial-of-a-type-i-positive-allosteric-modulator-of-alpha7-nicotinic-acetylcholine-receptors-pharmacokinetics-safety-and-evidence-for-neurocognitive-effect-of-avl-3288
#1
Kelvin W Gee, Ann Olincy, Richard Kanner, Lynn Johnson, Derk Hogenkamp, Josette Harris, Minhtam Tran, Stephen A Edmonds, William Sauer, Ryan Yoshimura, Timothy Johnstone, Robert Freedman
Type I positive allosteric modulators (PAMs) of the alpha7-nicotinic receptor enhance its cholinergic activation while preserving the spatiotemporal features of synaptic transmission and the receptor's characteristic rapid desensitization kinetics. Alpha7-nicotinic receptor agonists have shown promise for improving cognition in schizophrenia, but longer-term trials have been disappointing. Therefore, the type I PAM AVL-3288 was evaluated for safety and preliminary evidence of neurocognitive effect in healthy human subjects...
February 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28168926/stimulation-of-nicotinic-acetylcholine-alpha7-receptors-rescue-schizophrenia-like-cognitive-impairments-in-rats
#2
Agnieszka Potasiewicz, Agnieszka Nikiforuk, Małgorzata Hołuj, Piotr Popik
Alpha7 nicotinic acetylcholine receptor (α7 nAChR) dysfunction plays an important role in schizophrenia. Positive allosteric modulators of α7 nAChR have emerged as a promising therapeutic approach to manage cognitive deficits that are inadequately treated in schizophrenic patients. The aim of the present study was to evaluate the ability of type I (CCMI) and type II (PNU120596) α7 nAChR positive allosteric modulators to counteract MK-801-induced cognitive and sensorimotor gating deficits. The activity of these compounds was compared with the action of the α7 nAChR agonist A582941...
February 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28147247/evidence-of-brdu-positive-retinal-neurons-after-application-of-an-alpha7-nicotinic-acetylcholine-receptor-agonist
#3
Mark K Webster, Cynthia A Cooley-Themm, Joseph D Barnett, Harrison B Bach, Jessica M Vainner, Sarah E Webster, Cindy L Linn
Irreversible vision loss due to disease or age is responsible for a reduced quality of life. The experiments in this study test the hypothesis that the α7 nicotinic acetylcholine receptor agonist, PNU-282987, leads to the generation of retinal neurons in an adult mammalian retina in the absence of retinal injury or exogenous growth factors. Using antibodies against BrdU, retinal ganglion cells, progenitor cells and Müller glia, the results of this study demonstrate that multiple types of retinal cells and neurons are generated after eye drop application of PNU-282987 in adult Long Evans rats in a dose-dependent manner...
January 29, 2017: Neuroscience
https://www.readbyqxmd.com/read/28132910/b-973-a-novel-piperazine-positive-allosteric-modulator-of-the-%C3%AE-7-nicotinic-acetylcholine-receptor
#4
Debra J Post-Munson, Rick L Pieschl, Thaddeus F Molski, John D Graef, Adam W Hendricson, Ronald J Knox, Ivar M McDonald, Richard E Olson, John E Macor, Michael R Weed, Linda J Bristow, Laszlo Kiss, Michael K Ahlijanian, James Herrington
The alpha7 (α7) nicotinic acetylcholine receptor is a therapeutic target for cognitive disorders. Here we describe 3-(3,4-difluorophenyl)-N-(1-(6-(4-(pyridin-2-yl)piperazin-1-yl)pyrazin-2-yl)ethyl)propanamide (B-973), a novel piperazine-containing molecule that acts as a positive allosteric modulator of the α7 receptor. We characterize the action of B-973 on the α7 receptor using electrophysiology and radioligand binding. At 0.1mM acetylcholine, 1μM B-973 potentiated peak acetylcholine-induced currents 6-fold relative to maximal acetylcholine (3mM) and slowed channel desensitization, resulting in a 6900-fold increase in charge transfer...
January 26, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28131621/talkin-about-my-re-generation-the-who-of-intrinsic-retinal-stem-cells
#5
Deborah C Otteson
World-wide, two degenerative retinal diseases, glaucoma and age-related macular degeneration, are estimated to affect more than 12% of individuals over the age of 40 (Tham et al., 2014; Wong et al., 2014). Current therapies can slow progression, but cannot restore lost neurons or vision. Thus, there is increasing interest in developing strategies for therapeutic retinal regeneration. Nearly 50years of research on retinal neurogenesis and regeneration has identified Müller glia as intrinsic retinal stem cells in teleost fish...
January 25, 2017: Neuroscience
https://www.readbyqxmd.com/read/28078612/ameliorative-effect-of-ginsenoside-rg1-on-lipopolysaccharide-induced-cognitive-impairment-role-of-cholinergic-system
#6
Yang Jin, Jian Peng, Xiaona Wang, Dong Zhang, Tianyin Wang
Bacterial endotoxin lipopolysaccharide (LPS) can induce systemic inflammation, and therefore disrupt learning and memory processes. Ginsenoside Rg1, a major bioactive component of ginseng, is shown to greatly improve cognitive function. The present study was designed to further investigate whether administration of ginsenoside Rg1 can ameliorate LPS-induced cognitive impairment in the Y-maze and Morris water maze (MWM) task, and to explore the underlying mechanisms. Results showed that exposure to LPS (500 μg/kg) significantly impaired working and spatial memory and that repeated treatment with ginsenoside Rg1 (200 mg/kg/day, for 30 days) could effectively alleviate the LPS-induced cognitive decline as indicated by increased working and spatial memory in the Y-maze and MWM tests...
January 11, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28074940/alpha7-nicotinic-acetylcholine-receptor-is-required-for-amyloid-pathology-in-brain-endothelial-cells-induced-by-glycoprotein-120-methamphetamine-and-nicotine
#7
Liqun Liu, Jingyi Yu, Li Li, Bao Zhang, Lingjuan Liu, Chun-Hua Wu, Ambrose Jong, Ding-An Mao, Sheng-He Huang
One of the most challenging issues in HIV-associated neurocognitive disorders (HAND) caused by HIV-1 virotoxins and drug abuse is the lack of understanding the underlying mechanisms that are commonly associated with disorders of the blood-brain barrier (BBB), which mainly consists of brain microvascular endothelial cells (BMEC). Here, we hypothesized that Glycoprotein 120 (gp120), methamphetamine (METH) and nicotine (NT) can enhance amyloid-beta (Aβ) accumulation in BMEC through Alpha7 nicotinic acetylcholine receptor (α7 nAChR)...
January 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28045139/chrna7-deficient-mice-manifest-no-consistent-neuropsychiatric-and-behavioral-phenotypes
#8
Jiani Yin, Wu Chen, Hongxing Yang, Mingshan Xue, Christian P Schaaf
The alpha7 nicotinic acetylcholine receptor, encoded by the CHRNA7 gene, has been implicated in various psychiatric and behavioral disorders, including schizophrenia, bipolar disorder, epilepsy, autism, Alzheimer's disease, and Parkinson's disease, and is considered a potential target for therapeutic intervention. 15q13.3 microdeletion syndrome is a rare genetic disorder, caused by submicroscopic deletions on chromosome 15q. CHRNA7 is the only gene in this locus that has been deleted entirely in cases involving the smallest microdeletions...
January 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28039041/spinal-activation-of-alpha7-nicotinic-acetylcholine-receptor-attenuates-posttraumatic-stress-disorder-related-chronic-pain-via-suppression-of-glial-activation
#9
Rao Sun, Wei Zhang, Jinhua Bo, Zuoxia Zhang, Yishan Lei, Wenwen Huo, Yue Liu, Zhengliang Ma, Xiaoping Gu
The high prevalence of chronic pain in posttraumatic stress disorder (PTSD) individuals has been widely reported by clinical studies, which emphasized an urgent need to uncover the underlying mechanisms and identify potential therapeutic targets. Recent studies suggested that targeting activated glia and their pro-inflammatory products may provide a novel and effective therapy for the stress-related pain. In this study, we investigated whether activation of alpha-7 nicotinic acetylcholine receptor (α7 nAChR), a novel anti-inflammatory target, could attenuate PTSD-related chronic pain...
March 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/27717880/3-furan-2-yl-n-p-tolyl-acrylamide-a-positive-allosteric-modulator-of-the-%C3%AE-7-nicotinic-receptor-reverses-schizophrenia-like-cognitive-and-social-deficits-in-rats
#10
Agnieszka Potasiewicz, Małgorzata Hołuj, Tomasz Kos, Piotr Popik, Hugo R Arias, Agnieszka Nikiforuk
The cognitive impairments and negative symptoms experienced by schizophrenia patients still await effective treatment. Alpha7 nicotinic acetylcholine receptors (α7 nAChRs) have gain considerable attention in this regard. It has been recently proposed that positive allosteric modulators (PAMs) of α7 nAChRs may represent an alternative strategy to that based on orthosteric agonists. The aim of the present study is to evaluate the efficacy of PAM-2 (3-furan-2-yl-N-p-tolyl-acrylamide) against cognitive deficits and negative-like symptoms in a rat model of schizophrenia based on administration of ketamine, a NMDAR antagonist...
February 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27681882/immunomodulatory-effects-of-nicotine-on-interleukin-1%C3%AE-activated-human-astrocytes-and-the-role-of-cyclooxygenase-2-in-the-underlying-mechanism
#11
Priya Revathikumar, Filip Bergqvist, Srividya Gopalakrishnan, Marina Korotkova, Per-Johan Jakobsson, Jon Lampa, Erwan Le Maître
BACKGROUND: The cholinergic anti-inflammatory pathway (CAP) primarily functions through acetylcholine (ACh)-alpha7 nicotinic acetylcholine receptor (α7nAChR) interaction on macrophages to control peripheral inflammation. Interestingly, ACh can also bind α7nAChRs on microglia resulting in neuroprotective effects. However, ACh effects on astrocytes remain elusive. Here, we investigated the effects of nicotine, an ACh receptor agonist, on the cytokine and cholinesterase production of immunocompetent human astrocytes stimulated with interleukin 1β (IL-1β) in vitro...
September 29, 2016: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/27661000/alpha7-nicotine-acetylcholine-receptor-agonist-pnu-282987-attenuates-acute-lung-injury-in-a-cardiopulmonary-bypass-model-in-rats
#12
Jiaxi Ge, Jie Tian, Hao Yang, Lei Hou, Zhankui Wang, Zhengyu He, Xiangrui Wang
OBJECTIVE: Cardiopulmonary bypass (CPB) carries a risk of lung ischemia- reperfusion, leading to acute lung injury (ALI). Alpha7 nicotinic acetylcholine receptor (alpha7nAChR) has been implicated in the release of high mobility group box1 (HMGB1), which promotes systemic inflammation in response to ischemia-reperfusion injury. However, the specific role of alpha7nAChR in CPB is poorly understood. This study employed the alpha7nAChR agonist PNU-282987 and a rat model of CPB to determine whether alpha7nAChR was associated with CPB-induced lung damage...
September 22, 2016: Shock
https://www.readbyqxmd.com/read/27565651/brief-report-initial-trial-of-alpha7-nicotinic-receptor-stimulation-in-two-adult-patients-with-autism-spectrum-disorder
#13
Ann Olincy, Audrey Blakeley-Smith, Lynn Johnson, William R Kem, Robert Freedman
Abnormalities in CHRNA7, the alpha7-nicotinic receptor gene, have been reported in autism spectrum disorder. These genetic abnormalities potentially decrease the receptor's expression and diminish its functional role. This double-blind, placebo-controlled crossover study in two adult patients investigated whether an investigational receptor-specific partial agonist drug would increase the inhibitory functions of the gene and thereby increase patients' attention. An electrophysiological biomarker, P50 inhibition, verified the intended neurobiological effect of the agonist, and neuropsychological testing verified a primary cognitive effect...
December 2016: Journal of Autism and Developmental Disorders
https://www.readbyqxmd.com/read/27554853/heme-oxygenase-i-and-pcg-1%C3%AE-regulate-mitochondrial-biogenesis-via-microglial-activation-of-alpha7-nicotinic-acetylcholine-receptors-using-pnu282987
#14
Elisa Navarro, Laura Gonzalez-Lafuente, Irene Perez-Liebana, Izaskun Buendia, Elia López-Bernardo, Cristina Sanchez-Ramos, Ignacio Prieto, Antonio Cuadrado, Jorgina Satrustegui, Susana Cadenas, Maria Monsalve, Manuela Garcia Lopez
AIMS: A loss in brain acetylcholine and cholinergic markers, subchronic inflammation, and impaired mitochondrial function, which leads to low energy production and high oxidative stress, are common pathological factors in several neurodegenerative diseases. Glial cells are important for brain homeostasis and microglia controls the central immune response, where α7 acetylcholine nicotinic receptors (nAChR) seem to play a pivotal role; however, little is known about the effects of this receptor in metabolism...
August 23, 2016: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/27474687/alpha7-nicotinic-acetylcholine-receptor-agonists-and-pams-as-adjunctive-treatment-in-schizophrenia-an-experimental-study
#15
Monica M Marcus, Carl Björkholm, Anna Malmerfelt, Annie Möller, Ninni Påhlsson, Åsa Konradsson-Geuken, Kristin Feltmann, Kent Jardemark, Björn Schilström, Torgny H Svensson
Nicotine has been found to improve cognition and reduce negative symptoms in schizophrenia and a genetic and pathophysiological link between the α7 nicotinic acetylcholine receptors (nAChRs) and schizophrenia has been demonstrated. Therefore, there has been a large interest in developing drugs affecting the α7 nAChRs for schizophrenia. In the present study we investigated, in rats, the effects of a selective α7 agonist (PNU282987) and a α7 positive allosteric modulator (PAM; NS1738) alone and in combination with the atypical antipsychotic drug risperidone for their utility as adjunct treatment in schizophrenia...
September 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27467081/the-novel-nicotinic-alpha7-receptor-partial-agonist-bms-933043-improves-cognition-and-sensory-processing-in-preclinical-models-of-schizophrenia
#16
Linda J Bristow, Amy E Easton, Yu-Wen Li, Digavalli V Sivarao, Regina Lidge, Kelli M Jones, Debra Post-Munson, Christopher Daly, Nicholas J Lodge, Lizbeth Gallagher, Thaddeus Molski, Richard Pieschl, Ping Chen, Adam Hendricson, Ryan Westphal, James Cook, Christiana Iwuagwu, Daniel Morgan, Yulia Benitex, Dalton King, John E Macor, Robert Zaczek, Richard Olson
The development of alpha7 nicotinic acetylcholine receptor agonists is considered a promising approach for the treatment of cognitive symptoms in schizophrenia patients. In the present studies we characterized the novel agent, (2R)-N-(6-(1H-imidazol-1-yl)-4-pyrimidinyl)-4'H-spiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxazol]-2'-amine (BMS-933043), in vitro and in rodent models of schizophrenia-like deficits in cognition and sensory processing. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8...
2016: PloS One
https://www.readbyqxmd.com/read/27434535/carotid-and-aortic-stiffness-in-patients-with-heterozygous-familial-hypercholesterolemia
#17
Alexandra I Ershova, Alexey N Meshkov, Tatyana A Rozhkova, Maria V Kalinina, Alexander D Deev, Anatoliy N Rogoza, Tatyana V Balakhonova, Sergey A Boytsov
BACKGROUND: The role of plasma cholesterol in impairing arterial function and elasticity remains unclear. We evaluated arterial stiffness, measured locally in the common carotid artery by high-resolution echo-tracking, and aortic stiffness, using carotid-femoral pulse wave velocity (PWV) (the "gold-standard" measurement of arterial stiffness), in treatment-naive patients with heterozygous familial hypercholesterolemia (FH). METHODS: The study included 66 patients with FH (10-66 years old) and 57 first-degree relatives without FH (11-61 years old)...
2016: PloS One
https://www.readbyqxmd.com/read/27323436/-effects-of-electroaupuncture-stimulation-of-xiajuxu-st-39-etc-on-duodenal-mucosal-injury-serum-pro-inflammatory-factors-levels-and-duodenal-nicotinic-acetylcholine-receptor-alpha-7-expression-in-duodenal-ulcer-rats
#18
Xi Ling, Hong Zhang, Xi-qin Yi, Jin-feng Wu
OBJECTIVE: To observe the relatively specific effect of electroacupuncture (EA) of "Xiajuxu" (ST 39, the lower hesea paint of the small intestine), etc. on the level of serum TNF-alpha, lnterleukin-1 P (IL-1 P) and high mobility group protein B 1 (HMGB 1) contents, and duodenum a7 nicotinic acetyicholine receptor (nAchR) expression in duodenal ulcer rats, so as to explore its mechanisms underlying improving duodenal ulcer. METHODS: Sixty SD rats were randomly divided into 6 groups: normal control, model, Xiajuxu (ST 39), Zusanli (ST 36), Shangjuxu (ST 37) and Yanglingquan (GB 34)...
April 2016: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/27245499/the-kynurenine-pathway-in-schizophrenia-and-bipolar-disorder
#19
REVIEW
Sophie Erhardt, Lilly Schwieler, Sophie Imbeault, Göran Engberg
The kynurenine pathway of tryptophan degradation generates several neuroactive compounds. Of those, kynurenic acid is an N-methyl-d-aspartate (NMDA) and alpha7 nicotinic receptor antagonist. The kynurenic acid hypothesis of schizophrenia is built upon the fact that kynurenic acid blocks glutamate receptors and is elevated in schizophrenia. Kynurenic acid tightly controls glutamatergic and dopaminergic neurotransmission and elevated brain levels appear related to psychotic symptoms and cognitive impairments...
January 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27183376/tos-nos-mos-synthesis-of-different-aryl-sulfonate-precursors-for-the-radiosynthesis-of-the-alpha7-nicotinic-acetylcholine-receptor-radioligand-18-f-ns14490
#20
Sven Rötering, Matthias Scheunemann, Robert Günther, Reik Löser, Achim Hiller, Dan Peters, Peter Brust, Steffen Fischer, Jörg Steinbach
Radiopharmacological investigations of [(18)F]NS14490 have proven that this radiotracer could be a potential PET radiotracer for imaging of alpha7 nicotinic acetylcholine receptor particularly with regard to vulnerable plaques of diseased vessels. For further optimisation of the previously automated one-pot radiosynthesis of [(18)F]NS14490 using a tosylate precursor, precursors with other leaving groups (nosylate and mosylate) were synthesized and compared with the tosylate with respect to their reactivities towards [(18)F]fluoride...
August 2016: Applied Radiation and Isotopes
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