Update on PET Tracer Development for Muscarinic Acetylcholine Receptors
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Radiosynthesis and in Vivo Evaluation of a 18F-Labelled Styryl-Benzoxazole Derivative for Β-Amyloid Targeting
Author's Accepted Manuscript Radiosynthesis and in vivo Evaluation of a 18F- Labelled Styryl-Benzoxazole Derivative for β- Amyloid Targeting G.Ribeiro Morais, L. Gano, T. Kniess, R. Berg- mann, A. Abrunhosa, I. Santos, A. Paulo www.elsevier.com/locate/apradiso PII: S0969-8043(13)00292-3 DOI: http://dx.doi.org/10.1016/j.apradiso.2013.07.003 Reference: ARI6294 To appear in: Applied Radiation and Isotopes Received date: 9 January 2013 Revised date: 15 April 2013 Accepted date: 1 July 2013 Cite this article as: G.Ribeiro Morais, L. Gano, T. Kniess, R. Bergmann, A. Abrunhosa, I. Santos, A. Paulo, Radiosynthesis and in vivo Evaluation of a 18F- Labelled Styryl-Benzoxazole Derivative for β-Amyloid Targeting, Applied Radiation and Isotopes, http://dx.doi.org/10.1016/j.apradiso.2013.07.003 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting galley proof before it is published in its final citable form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. Radiosynthesis and in vivo Evaluation of a 18F-Labelled Styryl-Benzoxazole Derivative for β-Amyloid Targeting G. Ribeiro Morais,1 L. Gano,1 T. Kniess,2 R. Bergmann,2 A. Abrunhosa,3 I. Santos,1 and A. Paulo1* 1Radiopharmaceutical Sciences Group, IST/ITN, Instituto Superior Técnico, Universidade Técnica de Lisboa, EN 10, 2686-953 Sacavem; 2Institute of Radiopharmacy, Helmholtz-Zentrum Dresden-Rossendorf e.V., POB 510119, D-01314 Dresden, Germany; 3Universidade Coimbra, ICNAS, Inst Nucl Sci Appl Saúde, P-3000 Coimbra, Portugal Corresponding e-mail: [email protected] Keywords: Alzheimer´s Disease/ β-Amyloid aggregation/ Molecular Imaging / Fluorine-18 Abstract The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer´s disease (AD). -
Myocardial Perfusion Imaging in Coronary Artery Disease
Cor et Vasa Available online at www.sciencedirect.com journal homepage: www.elsevier.com/locate/crvasa Přehledový článek | Review article Myocardial perfusion imaging in coronary artery disease Magdalena Kostkiewicza,b a Department of Cardiovascular Diseases, Jagiellonian University, Collegium Medicum, Hospital John Paul II, Krakow, Poland b Department of Nuclear Medicine, Hospital John Paul II, Jagiellonian University, Collegium Medicum, Krakow, Poland ARTICLE INFO SOUHRN Article history: Radionuklidové zobrazování perfuze myokardu (myocardial perfusion imaging, MPI) lze použít k prokázání Received: 22. 8. 2015 přítomnosti ischemické choroby srdeční (ICHS), stratifi kaci rizika i k vedení léčby pacientů s již potvrzeným Received in revised form: 26. 9. 2015 onemocněním. Uvedená metoda je schopna lokalizovat hemodynamicky významné stenózy koronárních Accepted: 28. 9. 2015 tepen i zhodnotit rozsah a závažnost jejich obstrukce podle přítomnosti a rozsahu defektů perfuze. Nor- Available online: 31. 10. 2015 mální výsledek MPI znamená nepřítomnost koronární obstrukce, a tedy i klinicky významného onemocnění. Předností vyšetření srdce metodou PET je oproti SPECT její vyšší prostorové a časové rozlišení i nižší radiační zátěž pacienta. Zdá se, že hybridní vyšetření srdce kombinací SPECT nebo PET s údaji z CT nabízí přesnější Klíčová slova: a spolehlivější diagnostické a prognostické informace o pacientech se středně vysokým rizikem rozvoje ICHS. Ischemická choroba srdeční V poslední době byl zaznamenán významný pokrok ve smyslu přesnější kvantifi kace průtoku krve myokar- PET dem a koronární průtokové rezervy. Několik studií rovněž prokázalo, že kombinace zobrazení apoptózy Radionuklidové zobrazování perfuze a tvorby matrixových metaloproteináz může být prospěšná při zobrazování nestabilních plátů a vyhledání myokardu skupin asymptomatických pacientů s vysokým rizikem, pro něž znamená vyšetření zobrazovací metodou SPECT největší přínos. -
Classification of Medicinal Drugs and Driving: Co-Ordination and Synthesis Report
Project No. TREN-05-FP6TR-S07.61320-518404-DRUID DRUID Driving under the Influence of Drugs, Alcohol and Medicines Integrated Project 1.6. Sustainable Development, Global Change and Ecosystem 1.6.2: Sustainable Surface Transport 6th Framework Programme Deliverable 4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Due date of deliverable: 21.07.2011 Actual submission date: 21.07.2011 Revision date: 21.07.2011 Start date of project: 15.10.2006 Duration: 48 months Organisation name of lead contractor for this deliverable: UVA Revision 0.0 Project co-funded by the European Commission within the Sixth Framework Programme (2002-2006) Dissemination Level PU Public PP Restricted to other programme participants (including the Commission x Services) RE Restricted to a group specified by the consortium (including the Commission Services) CO Confidential, only for members of the consortium (including the Commission Services) DRUID 6th Framework Programme Deliverable D.4.4.1 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Page 1 of 243 Classification of medicinal drugs and driving: Co-ordination and synthesis report. Authors Trinidad Gómez-Talegón, Inmaculada Fierro, M. Carmen Del Río, F. Javier Álvarez (UVa, University of Valladolid, Spain) Partners - Silvia Ravera, Susana Monteiro, Han de Gier (RUGPha, University of Groningen, the Netherlands) - Gertrude Van der Linden, Sara-Ann Legrand, Kristof Pil, Alain Verstraete (UGent, Ghent University, Belgium) - Michel Mallaret, Charles Mercier-Guyon, Isabelle Mercier-Guyon (UGren, University of Grenoble, Centre Regional de Pharmacovigilance, France) - Katerina Touliou (CERT-HIT, Centre for Research and Technology Hellas, Greece) - Michael Hei βing (BASt, Bundesanstalt für Straßenwesen, Germany). -
Test–Retest Variability of Serotonin 5-HT2A Receptor Binding Measured with Positron Emission Tomography and [18F]Altanserin in the Human Brain
SYNAPSE 30:380–392 (1998) Test–Retest Variability of Serotonin 5-HT2A Receptor Binding Measured With Positron Emission Tomography and [18F]Altanserin in the Human Brain GWENN S. SMITH,1,2* JULIE C. PRICE,2 BRIAN J. LOPRESTI,2 YIYUN HUANG,2 NORMAN SIMPSON,2 DANIEL HOLT,2 N. SCOTT MASON,2 CAROLYN CIDIS MELTZER,1,2 ROBERT A. SWEET,1 THOMAS NICHOLS,2 DONALD SASHIN,2 AND CHESTER A. MATHIS2 1Department of Psychiatry, Western Psychiatric Institute and Clinic, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania 2Department of Radiology, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania KEY WORDS positron emission tomography (PET); serotonin receptor; 5-HT2A; imaging ABSTRACT The role of serotonin in CNS function and in many neuropsychiatric diseases (e.g., schizophrenia, affective disorders, degenerative dementias) support the development of a reliable measure of serotonin receptor binding in vivo in human subjects. To this end, the regional distribution and intrasubject test–retest variability of the binding of [18F]altanserin were measured as important steps in the further development of [18F]altanserin as a radiotracer for positron emission tomography (PET) 18 studies of the serotonin 5-HT2A receptor. Two high specific activity [ F]altanserin PET studies were performed in normal control subjects (n ϭ 8) on two separate days (2–16 days apart). Regional specific binding was assessed by distribution volume (DV), estimates that were derived using a conventional four compartment (4C) model, and the Logan graphical analysis method. For both analysis methods, levels of [18F]altanserin binding were highest in cortical areas, lower in the striatum and thalamus, and lowest in the cerebellum. -
Current Status and Growth of Nuclear Theranostics in Singapore
Nuclear Medicine and Molecular Imaging (2019) 53:96–101 https://doi.org/10.1007/s13139-019-00580-3 PERSPECTIVE ISSN (print) 1869-3482 ISSN (online) 1869-3474 Current Status and Growth of Nuclear Theranostics in Singapore Hian Liang Huang1,2 & Aaron Kian Ti Tong1,2 & Sue Ping Thang1,2 & Sean Xuexian Yan1,2 & Winnie Wing Chuen Lam1,2 & Kelvin Siu Hoong Loke1,2 & Charlene Yu Lin Tang1 & Lenith Tai Jit Cheng1 & Gideon Su Kai Ooi1 & Han Chung Low1 & Butch Maulion Magsombol1 & Wei Ying Tham1,2 & Charles Xian Yang Goh 1,2 & Colin Jingxian Tan 1 & Yiu Ming Khor1,2 & Sumbul Zaheer1,2 & Pushan Bharadwaj1,2 & Wanying Xie1,2 & David Chee Eng Ng1,2 Received: 3 January 2019 /Revised: 13 January 2019 /Accepted: 14 January 2019 /Published online: 25 January 2019 # Korean Society of Nuclear Medicine 2019 Abstract The concept of theranostics, where individual patient-level biological information is used to choose the optimal therapy for that individual, has become more popular in the modern era of ‘personalised’ medicine. With the growth of theranostics, nuclear medicine as a specialty is uniquely poised to grow along with the ever-increasing number of concepts combining imaging and therapy. This special report summarises the status and growth of Theranostic Nuclear Medicine in Singapore. We will cover our experience with the use of radioiodine, radioiodinated metaiodobenzylguanidine, peptide receptor radionuclide therapy, prostate specific membrane antigen radioligand therapy, radium-223 and yttrium-90 selective internal radiation therapy. We also include a section on our radiopharmacy laboratory, crucial to our implementation of theranostic principles. Radionuclide theranostics has seen tremendous growth and we hope to be able to grow alongside to continue to serve the patients in Singapore and in the region. -
A Systematic Review of Combination and High-Dose Atypical
APPENDIX 12: STUDY CHARACTERISTICS OF INCLUDED STUDIES Number of Interventions/ Adjunctive Treatment APDs Failed Sample Author, Year Country Sponsor Comparators Medications Duration Prior to Size (Mean Dose) Allowed (Weeks) Study Grant from Stanley Medical research Institute, RIS+CLZ Benzodiazepines Janssen 515.6±138.7 mg/d CLZ for anxiety and/or AKDEDE et al. Pharmaceutica, and 42 Turkey biperiden for 6 weeks ≥3 30 (2005) THE Ritter 5.1±1.3 mg/day RIS EPS allowed if Foundation, the PLC+CLZ necessary William K. 414.3±96.9 mg/d CLZ Warren Medical Research Foundation ANIL YAGCIOGLU et 45 See Akdede 2006 al. (2005) AMI400+CLZ 400mg/d AMI and 300 Occasional mg/d CLZ intake of 49 Sanofi- AMI600+CLZ benzodiazepines, ASSION et al. (2008) Germany 6 weeks ≥1 16 Synthelabo 600 mg/d AMI and sedatives, or 300mg/d CLZ antidepressants PLC+CLZ allowed 300 mg/d CLZ 60 France and Novartis Phama RIS (H): median 9 mg/d AZORIN et al. (2001) Not reported 12 weeks ≥1 273 Canada S.A. CLZ: median: 600 mg/d Lorazepam or Janssen oxazepam for BONDOLFI et al. France and RIS (H): 6.4 mg/d 66 Research sleep induction 8 weeks ≥2 86 (1998) Switzerland CLZ: 291.2 mg/d Foundation or daytime sedation; 156 Systematic Review of Combination and High-Dose AAPs for Schizophrenia Number of Interventions/ Adjunctive Treatment APDs Failed Sample Author, Year Country Sponsor Comparators Medications Duration Prior to Size (Mean Dose) Allowed (Weeks) Study biperiden and procyclidine for EPS Supported by grants from Brain Research center, funded by the ARI+CLZ Antidepressants, Ministry of 15.5±7.1 mg/d ARI and 38 anticholinergics CHANG et al. -
Partial Agreement in the Social and Public Health Field
COUNCIL OF EUROPE COMMITTEE OF MINISTERS (PARTIAL AGREEMENT IN THE SOCIAL AND PUBLIC HEALTH FIELD) RESOLUTION AP (88) 2 ON THE CLASSIFICATION OF MEDICINES WHICH ARE OBTAINABLE ONLY ON MEDICAL PRESCRIPTION (Adopted by the Committee of Ministers on 22 September 1988 at the 419th meeting of the Ministers' Deputies, and superseding Resolution AP (82) 2) AND APPENDIX I Alphabetical list of medicines adopted by the Public Health Committee (Partial Agreement) updated to 1 July 1988 APPENDIX II Pharmaco-therapeutic classification of medicines appearing in the alphabetical list in Appendix I updated to 1 July 1988 RESOLUTION AP (88) 2 ON THE CLASSIFICATION OF MEDICINES WHICH ARE OBTAINABLE ONLY ON MEDICAL PRESCRIPTION (superseding Resolution AP (82) 2) (Adopted by the Committee of Ministers on 22 September 1988 at the 419th meeting of the Ministers' Deputies) The Representatives on the Committee of Ministers of Belgium, France, the Federal Republic of Germany, Italy, Luxembourg, the Netherlands and the United Kingdom of Great Britain and Northern Ireland, these states being parties to the Partial Agreement in the social and public health field, and the Representatives of Austria, Denmark, Ireland, Spain and Switzerland, states which have participated in the public health activities carried out within the above-mentioned Partial Agreement since 1 October 1974, 2 April 1968, 23 September 1969, 21 April 1988 and 5 May 1964, respectively, Considering that the aim of the Council of Europe is to achieve greater unity between its members and that this -
In Vivo Molecular Imaging: Ligand Development and Research Applications
31 IN VIVO MOLECULAR IMAGING: LIGAND DEVELOPMENT AND RESEARCH APPLICATIONS MASAHIRO FUMITA AND ROBERT B. INNIS In positron emission tomography (PET) and single-photon ders must be addressed. Physical barriers include limited emission computed tomography (SPECT), tracers labeled anatomic resolution and the need for even higher sensitivity. with radioactive isotopes are used to measure protein mole- However, recent developments with improved detector cules (e.g., receptors, transporters, and enzymes). A major crystals (e.g., lutetium oxyorthosilicate) and three-dimen- advantage of these two radiotracer techniques is extraordi- sional image acquisition have markedly enhanced both sen- -M), many orders sitivity and resolution. (5). Commercially available PET de 12מto 10 9מnarily high sensitivity (ϳ 10 of magnitude greater than the sensitivities available with vices provide resolution of 2 to 2.5 mm (6,7). Furthermore, -M) or mag- the relatively high cost of imaging with SPECT, and espe 4מmagnetic resonance imaging (MRI) (ϳ 10 M). cially PET, can be partially subsidized by clinical use of the 5מto 10 3מnetic resonance spectroscopy (MRS) (ϳ 10 For example, MRI detection of gadolinium occurs at con- devices. Recent approval of U.S. government (i.e., Medi- מ centrations of approximately 10 4 M (1), and MRS mea- care) reimbursement of selected PET studies for patients sures brain levels of ␥-aminobutyric acid (GABA) and gluta- with tumors, epilepsy, and cardiac disease has significantly מ mine at concentrations of approximately 10 3 M (2,3). enhanced the sales of PET cameras and their availability for In contrast, PET studies with [11C]NNC 756 in which a partial use in research studies. -
Anew Drug Design Strategy in the Liht of Molecular Hybridization Concept
www.ijcrt.org © 2020 IJCRT | Volume 8, Issue 12 December 2020 | ISSN: 2320-2882 “Drug Design strategy and chemical process maximization in the light of Molecular Hybridization Concept.” Subhasis Basu, Ph D Registration No: VB 1198 of 2018-2019. Department Of Chemistry, Visva-Bharati University A Draft Thesis is submitted for the partial fulfilment of PhD in Chemistry Thesis/Degree proceeding. DECLARATION I Certify that a. The Work contained in this thesis is original and has been done by me under the guidance of my supervisor. b. The work has not been submitted to any other Institute for any degree or diploma. c. I have followed the guidelines provided by the Institute in preparing the thesis. d. I have conformed to the norms and guidelines given in the Ethical Code of Conduct of the Institute. e. Whenever I have used materials (data, theoretical analysis, figures and text) from other sources, I have given due credit to them by citing them in the text of the thesis and giving their details in the references. Further, I have taken permission from the copyright owners of the sources, whenever necessary. IJCRT2012039 International Journal of Creative Research Thoughts (IJCRT) www.ijcrt.org 284 www.ijcrt.org © 2020 IJCRT | Volume 8, Issue 12 December 2020 | ISSN: 2320-2882 f. Whenever I have quoted written materials from other sources I have put them under quotation marks and given due credit to the sources by citing them and giving required details in the references. (Subhasis Basu) ACKNOWLEDGEMENT This preface is to extend an appreciation to all those individuals who with their generous co- operation guided us in every aspect to make this design and drawing successful. -
[18F] Altanserin Bolus Injection in the Canine Brain Using PET Imaging
Pauwelyn et al. BMC Veterinary Research (2019) 15:415 https://doi.org/10.1186/s12917-019-2165-5 RESEARCH ARTICLE Open Access Kinetic analysis of [18F] altanserin bolus injection in the canine brain using PET imaging Glenn Pauwelyn1*† , Lise Vlerick2†, Robrecht Dockx2,3, Jeroen Verhoeven1, Andre Dobbeleir2,5, Tim Bosmans2, Kathelijne Peremans2, Christian Vanhove4, Ingeborgh Polis2 and Filip De Vos1 Abstract 18 Background: Currently, [ F] altanserin is the most frequently used PET-radioligand for serotonin2A (5-HT2A) receptor imaging in the human brain but has never been validated in dogs. In vivo imaging of this receptor in the canine brain could improve diagnosis and therapy of several behavioural disorders in dogs. Furthermore, since dogs are considered as a valuable animal model for human psychiatric disorders, the ability to image this receptor in dogs could help to increase our understanding of the pathophysiology of these diseases. Therefore, five healthy laboratory beagles underwent a 90-min dynamic PET scan with arterial blood sampling after [18F] altanserin bolus injection. Compartmental modelling using metabolite corrected arterial input functions was compared with reference tissue modelling with the cerebellum as reference region. 18 Results: The distribution of [ F] altanserin in the canine brain corresponded well to the distribution of 5-HT2A receptors in human and rodent studies. The kinetics could be best described by a 2-Tissue compartment (2-TC) model. All reference tissue models were highly correlated with the 2-TC model, indicating compartmental modelling can be replaced by reference tissue models to avoid arterial blood sampling. Conclusions: This study demonstrates that [18F] altanserin PET is a reliable tool to visualize and quantify the 5- HT2A receptor in the canine brain. -
Fluorine-18-Labeled Fluorescent Dyes for Dual-Mode Molecular Imaging
molecules Review Fluorine-18-Labeled Fluorescent Dyes for Dual-Mode Molecular Imaging Maxime Munch 1,2,*, Benjamin H. Rotstein 1,2 and Gilles Ulrich 3 1 University of Ottawa Heart Institute, Ottawa, ON K1Y 4W7, Canada; [email protected] 2 Department of Biochemistry, Microbiology and Immunology, University of Ottawa, Ottawa, ON K1H 8M5, Canada 3 Institut de Chimie et Procédés pour l’Énergie, l’Environnement et la Santé (ICPEES), UMR CNRS 7515, École Européenne de Chimie, Polymères et Matériaux (ECPM), 25 rue Becquerel, CEDEX 02, 67087 Strasbourg, France; [email protected] * Correspondence: [email protected]; Tel.: +1-613-696-7000 Academic Editor: Emmanuel Gras Received: 30 November 2020; Accepted: 16 December 2020; Published: 21 December 2020 Abstract: Recent progress realized in the development of optical imaging (OPI) probes and devices has made this technique more and more affordable for imaging studies and fluorescence-guided surgery procedures. However, this imaging modality still suffers from a low depth of penetration, thus limiting its use to shallow tissues or endoscopy-based procedures. In contrast, positron emission tomography (PET) presents a high depth of penetration and the resulting signal is less attenuated, allowing for imaging in-depth tissues. Thus, association of these imaging techniques has the potential to push back the limits of each single modality. Recently, several research groups have been involved in the development of radiolabeled fluorophores with the aim of affording dual-mode PET/OPI probes used in preclinical imaging studies of diverse pathological conditions such as cancer, Alzheimer’s disease, or cardiovascular diseases. Among all the available PET-active radionuclides, 18F stands out as the most widely used for clinical imaging thanks to its advantageous characteristics (t1/2 = 109.77 min; 97% β+ emitter). -
The Who, When, Why, and How of PET Amyloid Imaging in Management of Alzheimer’S Disease—Review of Literature and Interesting Images
diagnostics Review The Who, When, Why, and How of PET Amyloid Imaging in Management of Alzheimer’s Disease—Review of Literature and Interesting Images Subapriya Suppiah 1,2 , Mellanie-Anne Didier 3,4 and Sobhan Vinjamuri 3,* 1 Centre for Diagnostic Nuclear Imaging, University Putra Malaysia, Serdang 43400, Selangor, Malaysia; [email protected] 2 Department of Imaging, Faculty of Medicine and Health Sciences, University Putra Malaysia, Serdang 43400, Selangor, Malaysia 3 The Royal Liverpool and Broadgreen University Hospitals NHS Trusts, Prescot St, Liverpool L7 8XP, UK; [email protected] 4 Section of Nuclear Medicine, Department of Surgery, Radiology, Anaesthesia & Intensive Care, The University Hospital of The West Indies, The University of The West Indies, Mona Campus, Kingston 7, Jamaica * Correspondence: [email protected] Received: 23 May 2019; Accepted: 21 June 2019; Published: 25 June 2019 Abstract: Amyloid imaging using positron emission tomography (PET) has an emerging role in the management of Alzheimer’s disease (AD). The basis of this imaging is grounded on the fact that the hallmark of AD is the histological detection of beta amyloid plaques (Aβ) at post mortem autopsy. Currently, there are three FDA approved amyloid radiotracers used in clinical practice. This review aims to take the readers through the array of various indications for performing amyloid PET imaging in the management of AD, particularly using 18F-labelled radiopharmaceuticals. We elaborate on PET amyloid scan interpretation techniques, their limitations and potential improved specificity provided by interpretation done in tandem with genetic data such as apolipiprotein E (APO) 4 carrier status in sporadic cases and molecular information (e.g., cerebral spinal fluid (CSF) amyloid levels).