Download or read book Ex Vivo Binding of the Agonist PET Radiotracer 11C PHNO to Dopamine D2 D3 Receptors in Rat Brain written by Patrick N. McCormick and published by . This book was released on 2010 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Ex Vivo Binding of the Agonist PET Radiotracer carbon 11 PHNO to Dopamine D2 D3 Receptors in Rat Brain Lack of Correspondence to the D2 Receptor Two affinity state Model written by Patrick Neil McCormick and published by . This book was released on 2010 with total page 444 pages. Available in PDF, EPUB and Kindle. Book excerpt: The dopamine D2 receptor exists in vitro in two states of agonist affinity: a high-affinity state mediating dopamine's physiological effects, and a physiologically-inert low-affinity state. Our primary goal was to determine the in vivo relevance of this two-affinity-state model for the agonist PET radiotracer [11C]-(+)-PHNO, developed for measurement of the D2 high-affinity state. Our second goal was to characterize the regional D2 versus D3 pharmacology of [3H]-(+)-PHNO binding and assess its utility for measuring drug occupancy at both receptor subtypes.Using ex vivo dual-radiotracer experiments in conscious rats, we showed that, contrary to the two-affinity-state model, the binding of [11C]-(+)-PHNO and the antagonist [3H]-raclopride were indistinguishably inhibited by D2 partial agonist (aripiprazole), indirect agonist (amphetamine) and full agonist ((-)-NPA) pretreatment. Furthermore, ex vivo [11C]-(+)-PHNO binding was unaffected by treatments that increase in vitro high-affinity state density (chronic amphetamine, ethanol-withdrawal), whereas unilateral 6-OHDA lesion, which increases total D2 receptor expression, similarly increased the ex vivo binding of [11C]-(+)-PHNO and [3H]- raclopride. These results do not support the in vivo validity of the two-affinity-state model, suggesting instead a single receptor state for [11C]-(+)-PHNO and [3H]-raclopride in conscious rat. Importantly, we also demonstrated that the increased amphetamine-sensitivity of the agonist radiotracers [11C]-(+)-PHNO and [11C]-(-)-NPA, commonly seen in isoflurane-anaesthetized animals and cited as evidence for the two-affinity-state model, is due to the confounding effects of anaesthesia.Using in vitro and ex vivo autoradiography in rat and the D3 receptor-selective drug SB277011, we found that [ 3H]-(+)-PHNO binding in striatum and cerebellum lobes 9 and 10 was due exclusively to D2 and D3 receptor binding, respectively, but in other extra-striatal regions to a mix of the two receptor subtypes. Surprisingly, the D3 contribution to [3H]-(+)-PHNO binding was greater ex vivo than in vitro. Also surprising, several antipsychotic drugs, at doses producing 80% D2 occupancy, produced insignificant (olanzapine, risperidone, haloperidol) or small (clozapine, ∼35%) D3 occupancy, despite similarly occupying both receptor subtypes in vitro. These data reveal a significant discrepancy between in vitro and ex vivo measures of dopamine receptor binding and suggest that the D3 occupancy is not necessary for the therapeutic effect of antipsychotic drugs.
Download or read book Pre clinical Evaluation of carbon 11 PHNO as an Agonist Positron Emission Tomography PET Radiotracer for Imaging of the High affinity State of the Dopamine D2 Receptor written by Patrick Neil McCormick and published by . This book was released on 2006 with total page 150 pages. Available in PDF, EPUB and Kindle. Book excerpt: In vivo imaging of the D2 receptor with agonist radiotracers could provide important information on the high-affinity, functional state of the D2 receptor in schizophrenia and Parkinson's disease. Here the D2 agonist [11C]-(+)-PHNO was evaluated for use as an agonist PET radiotracer. In vitro, (+)-PHNO was shown, through competitive binding experiments and functional assays for D2 agonism, to be a potent full agonist at the D2 receptor. Ex vivo in rats, [11C]-(+)-PHNO readily crossed the blood-brain barrier and accumulated preferentially in the D2-rich striatum. [11C]-(+)-PHNO pharmacokinetics were rapid, with peak accumulation 5 min after tail-vein injection. The striatal binding of [11C]-(+)-PHNO was highly stereo selective, saturable, had pharmacology appropriate for D2 receptor binding and was sensitive to both increases and decreases in the concentration of endogenous dopamine. These characteristics make [11C]-(+)-PHNO a promising candidate for in vivo imaging of the high-affinity, functional state of the D2 receptor in humans using PET.
Download or read book Estimating Endogenous Dopamine at D2 and D3 Receptors in the Human Brain Using the Agonist Radiotracer 11C PHNO written by Fernando Caravaggio and published by . This book was released on 2015 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Localization and Differential Regulation of Dopamine D2 and D3 Receptors in the Rat Brain written by Gregg D. Stanwood and published by . This book was released on 1998 with total page 176 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Small Animal Imaging written by Fabian Kiessling and published by Springer Science & Business Media. This book was released on 2010-11-29 with total page 589 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small animal imaging has been recognized as an important tool in preclinical research. Nevertheless, the results of non-invasive imaging are often disappointing owing to choice of a suboptimal imaging modality and/or shortcomings in study design, experimental setup, and data evaluation. This textbook is a practical guide to the use of non-invasive imaging in preclinical research. Each of the available imaging modalities is discussed in detail, with the assistance of numerous informative illustrations. In addition, many useful hints are provided on the installation of a small animal unit, study planning, animal handling, and the cost-effective performance of small animal imaging. Cross-calibration methods, data postprocessing, and special imaging applications are also considered in depth. This is the first book to cover all the practical basics in small animal imaging, and it will prove an invaluable aid for researchers, students, and technicians.
Download or read book Novel Antischizophrenia Treatments written by Mark A. Geyer and published by Springer Science & Business Media. This book was released on 2012-08-31 with total page 456 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume will try to put current therapy - achievements, shortcomings, remaining medical needs - and emerging new targets into the context of increasing knowledge regarding the genetic and neurodevelopmental contributions to the pathophysiology of schizophrenia. Some of the chapters will also deal with respective experimental and clinical methodology, biomarkers, and translational aspects of drug development. The volume will concentrate on reviewing the ongoing research attempting to identify novel treatments for the cognitive deficits and negative symptoms of schizophrenia, which are not treated adequately by current antipsychotic medications.
Download or read book Novel Antischizophrenia Treatments written by Mark A. Geyer and published by Springer Science & Business Media. This book was released on 2012-10-01 with total page 456 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume tries to put current therapy - achievements, shortcomings, remaining medical needs - and emerging new targets into the context of increasing knowledge regarding the genetic and neurodevelopmental contributions to the pathophysiology of schizophrenia. Some of the chapters also deal with respective experimental and clinical methodology, biomarkers, and translational aspects of drug development. The volume concentrates on reviewing the ongoing research attempting to identify novel treatments for the cognitive deficits and negative symptoms of schizophrenia, which are not treated adequately by current antipsychotic medications.
Download or read book Handbook of Radiopharmaceuticals written by Michael R. Kilbourn and published by John Wiley & Sons. This book was released on 2021-04-12 with total page 768 pages. Available in PDF, EPUB and Kindle. Book excerpt: The thoroughly updated new edition of the authoritative reference in Radiopharmaceutical Sciences The second edition of Handbook of Radiopharmaceuticals is a comprehensive review of the field, presenting up-to-date coverage of central topics such as radionuclide production, synthetic methodology, radiopharmaceutical development and regulations, and a wide range of practical applications. A valuable reference work for those new to the Radiopharmaceutical Sciences and experienced professionals alike, this volume explores the latest concepts and issues involving both targeted diagnostic and therapeutic radiopharmaceuticals. Contributions from a team of experts from across sub-disciplines provide readers with an immersive examination of radiochemistry, nuclear medicine, molecular imaging, and more. Since the first edition of the Handbook was published, Nuclear Medicine and Radiopharmaceutical Sciences have undergone major changes. New radiopharmaceuticals for diagnosis and therapy have been approved by the FDA, the number of clinical PET and SPECT scans have increased significantly, and advances in Artificial Intelligence have dramatically improved research techniques. This fully revised edition reflects the current state of the field and features substantially updated and expanded content. New chapters cover topics including current Good Manufacturing Practice (cGMP), regulatory oversight, novel approaches to quality control—ensuring that readers are informed of the exciting developments of recent years. This important resource: Features extensive new and revised content throughout Covers key areas of application for diagnosis and therapy in oncology, neurology, and cardiology Emphasizes the multidisciplinary nature of Radiopharmaceutical Sciences Discusses how drug companies are using modern radiopharmaceutical imaging techniques to support drug discovery Examines current and emerging applications of Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) Edited by recognized experts in radiochemistry and PET imaging, Handbook of Radiopharmaceuticals: Radiochemistry and Applications, 2 nd Edition is an indispensable reference for post-doctoral fellows, research scientists, and professionals in the pharmaceutical industry, and for academics, graduate students, and newcomers in the field of radiopharmaceuticals.
Download or read book Cyclin Dependent Kinase 5 Cdk5 written by Nancy Y. Ip and published by Springer Science & Business Media. This book was released on 2009-02-28 with total page 326 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cyclin Dependent Kinase 5 provides a comprehensive and up-to-date collection of reviews on the discovery, signaling mechanisms and functions of Cdk5, as well as the potential implication of Cdk5 in the treatment of neurodegenerative diseases. Since the identification of this unique member of the Cdk family, Cdk5 has emerged as one of the most important signal transduction mediators in the development, maintenance and fine-tuning of neuronal functions and networking. Further studies have revealed that Cdk5 is also associated with the regulation of neuronal survival during both developmental stages and in neurodegenerative diseases. These observations indicate that precise control of Cdk5 is essential for the regulation of neuronal survival. The pivotal role Cdk5 appears to play in both the regulation of neuronal survival and synaptic functions thus raises the interesting possibility that Cdk5 inhibitors may serve as therapeutic treatment for a number of neurodegenerative diseases.
Download or read book Imaging of the Human Brain in Health and Disease written by Philip Seeman and published by Elsevier. This book was released on 2013-11-15 with total page 534 pages. Available in PDF, EPUB and Kindle. Book excerpt: Brain imaging technology remains at the forefront of advances in both our understanding of the brain and our ability to diagnose and treat brain disease and disorders. Imaging of the Human Brain in Health and Disease examines the localization of neurotransmitter receptors in the nervous system of normal, healthy humans and compares that with humans who are suffering from various neurologic diseases. Opening chapters introduce the basic science of imaging neurotransmitters, including sigma, acetylcholine, opioid, and dopamine receptors. Imaging the healthy and diseased brain includes brain imaging of anger, pain, autism, the release of dopamine, the impact of cannabinoids, and Alzheimer's disease. This book is a valuable companion to a wide range of scholars, students, and researchers in neuroscience, clinical neurology, and psychiatry, and provides a detailed introduction to the application of advanced imaging to the treatment of brain disorders and disease. A focused introduction to imaging healthy and diseased brains Focuses on the primary neurotransmitter release Includes sigma, acetylcholine, opioid, and dopamine receptors Presents the imaging of healthy and diseased brains via anger, pain, autism, and Alzheimer's disease
Download or read book Methods in Neurotransmitter Receptor Analysis written by Henry I. Yamamura and published by Raven Press (ID). This book was released on 1990 with total page 298 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book PET and SPECT in Psychiatry written by Rudi A.J.O. Dierckx and published by Springer Science & Business Media. This book was released on 2014-03-28 with total page 851 pages. Available in PDF, EPUB and Kindle. Book excerpt: PET and SPECT in Psychiatry showcases the combined expertise of renowned authors whose dedication to the investigation of psychiatric disease through nuclear medicine technology has achieved international recognition. The classical psychiatric disorders as well as other subjects – such as suicide, sleep, eating disorders, and autism – are discussed and the latest results in functional neuroimaging are detailed. Most chapters are written jointly by a clinical psychiatrist and a nuclear medicine expert to ensure a multidisciplinary approach. This state of the art compendium will be valuable to all who have an interest in the field of neuroscience, from the psychiatrist and the radiologist/nuclear medicine specialist to the interested general practitioner and cognitive psychologist. It is the first volume of a trilogy on PET and SPECT imaging in the neurosciences; other volumes will focus on PET and SPECT in neurology and PET and SPECT of neurobiological systems.
Download or read book Ketamine written by David T. Yew and published by CRC Press. This book was released on 2015-03-16 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: Increasing use of ketamine as a recreational drug in Asia, Europe, and America is a great burden on society at large, leading to aspirational strain, unemployment, and crime. These societal effects have led to growing interest among researchers and clinicians in ketamine's effects on various systems of the body. Ketamine: Use and Abuse reviews the
Download or read book Quality in Nuclear Medicine written by Andor W.J.M. Glaudemans and published by Springer. This book was released on 2016-11-14 with total page 455 pages. Available in PDF, EPUB and Kindle. Book excerpt: This comprehensive textbook provides a state of the art overview of the means by which quality in patient care is ensured within the field of nuclear medicine. Acknowledged experts in the field cover both management aspects, such as laws, standards, guidelines, patient safety, management instruments, and organisations, and specific issues, including radiation safety and equipment. Quality in Nuclear Medicine not only presents detailed information on the topics discussed but should also stimulate further discussion and offer an important tool to all professionals in the field of nuclear medicine and their stakeholders. Readers will find that the book provides a wealth of excellent guidance and reflects the pioneering role of nuclear medicine in advancing different aspects of quality within medicine.
Download or read book Clinical Nuclear Medicine written by Hans-Jürgen Biersack and published by Springer Science & Business Media. This book was released on 2008-01-03 with total page 573 pages. Available in PDF, EPUB and Kindle. Book excerpt: This work has true international scope, being a unique European/American joint venture that focuses on the state of the art in both diagnostic and therapeutic radionuclide methodology. Pertinent clinical applications are emphasized rather than attempting to cover everything included in the several large comprehensive texts available in our field. This "practical" approach should make it an essential guide to nuclear medicine physicians, technologists, students and interested clinicians alike.
Download or read book Trends on the Role of PET in Drug Development written by Philip H. Elsinga and published by World Scientific. This book was released on 2012 with total page 799 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug development is very expensive and a fight against time. PET offers possibilities to speed up this process by adding unique in vivo information on pharmacokinetics/dynamics of a drug at an early stage. This information can help decision makers to move the drug in the drug development process or to decide to stop further developments. This unique and complete book highlights the different ways PET can be used and describes the latest trends in the various disciplines within nuclear medicine to further improve methodologies and increase the number of tools to accelerate drug development. Various topics within tracer development, instrumentation, data analysis and many clinical and preclinical topics are described by leading scientists from industry and academia.
