PET for Drug Development and Evaluation

1. Front Matter

   Pages i-viii

   PDF

2. Introduction

   1. Drug Development and Positron Emission Tomography

      • Bruce Campbell

      Pages 1-24

   2. Positron Emission Tomography: Basic Principles and Potential Interest for Pharmacological Studies

      • Bernard Mazoyer

      Pages 25-35

   3. Is PET a Tool for Drug Evaluation?

      • Bengt Långström, Mats Bergström, Per Hartvig, Sven Valind, Yasuyoshi Watanabe

      Pages 37-50

3. Psychiatry

   1. PET in Neuropsychiatric Drug Development

      • Lars Farde

      Pages 51-53

   2. Radioligand Disposition and Metabolism — Key Information in Early Drug Development

      • Christer Halldin, Carl-Gunnar Swahn, Lars Farde, Göran Sedvall

      Pages 55-65

   3. PET Studies in the Early Clinical Development of a New Antipsychotic

      • J. M. Ad Sitsen, L. Farde

      Pages 67-71

   4. PET in the Development of Dopamine D1 Antagonists as New Potential Antipsychotic Drugs

      • Christian Foged, Per Karlsson, Birte K. Skrumsager, Lars Ynddal, Erik B. Nielsen, Christer Halldin et al.

      Pages 73-81

   5. Is the 5-HT2-Receptor a Target for Antipsychotic Drug Action? PET Studies on Dopamine (D2 and Serotonin (5-HT2) Receptor Occupancy in Patients and Healthy Subjects

      • Svante Nyberg, Anna-Lena Nordström, Christer Halldin, Lars Farde

      Pages 83-92

   6. Preclinical Development of a Radioligand for the Study of Central 5-HT1A Receptors with PET — [11C]Way-100635

      • Victor W. Pike, Ian A. Cliffe, Allan Fletcher, Susan P. Hume, Julie A. McCarron, Sharon Ashworth et al.

      Pages 93-108

   7. Comparative In vivo and In vitro Selectivity of Zolpidem for ω (Benzodiazepine) Modulatory Site Subtypes

      • Jesús Benavides, Pascale Abadie, Jean Claude Baron, Bernard Scatton

      Pages 109-122

   8. Do the Effects of Muscarinic Receptor Blockade on Brain Glucose Consumption Mimic the Cortical and Subcortical Metabolic Pattern of Alzheimer’s Disease in Normal Volunteers ?

      • J. Blin, T. N. Chase, M. F. Piercey

      Pages 123-132

4. Neurology

   1. PET Evaluation of Drug Treatment in Ischemic Stroke and Alzheimer’s Disease

      • Wolf-Dieter Heiss

      Pages 133-146

   2. PET Imaging of Cerebral Perfusion and Oxygen Metabolism in Acute Ischemic Stroke: Implications for Management and Therapy

      • J. C. Baron

      Pages 147-154

   3. Pharmacokinetics: Kinetic Modelling of MAO Inhibitors and D2 Antagonists

      • Adriaan A. Lammertsma, Christopher J. Bench

      Pages 155-165

   4. Brain Activation Under Drug Treatment

      • Paul M. Grasby, Karl J. Friston

      Pages 167-177

   5. Modifying the Progression of Parkinson’s Disease

      • Paul Morrish, James Rakshi, David J. Brooks

      Pages 179-188

   6. COMT Inhibition: Pharmacology of Tolcapone and 6-[18F]-Fluoro-L-DOPA (FDOPA) PET Results

      • Jorga Karin, Leenders Klaus Leonhard, Günther Ilonka, Psylla Maria

      Pages 189-195

   7. Interaction of Lisuride with dopaminergic receptors

      • B. Mazière, R. Horowski

      Pages 197-203

   8. Lisuride and [C-11]-Raclopride Interaction at the D2 Receptor Site

      • Klaus Leonhard Leenders, Angelo Antonini

      Pages 205-214

Can drug development and evaluation be improved by the use of positron emission tomography (PET)? PET is now well established and many PET centres participate in networks that warrant the quality of their research. PET allows one to follow the effect of a drug on a variety of patients' metabolic parameters. In addition, PET may be used to follow the fate in vivo of a compound, allowing visualisation of its binding to specific receptors and a direct study of the mechanism of drug action in normal and pathological situations.
The book shows the fields in which PET offers new and unique information for the development of drugs (conception, toxicity, pharmacokinetics and metabolism, clinical research, and relations between clinical and biological effects) and evaluates fields in which PET may shorten the development time of drugs.
Audience: Professionals in the pharmaceutical industry in all areas of drug discovery and pharmacology, pre-clinical testing, pharmacokinetics and metabolism, clinical evaluation, registration and regulatory affairs. Government health authority representatives who assess data and documentation on new drug development and radiopharmaceuticals. Academic experts concerned with any of these areas.

• brain
• clinical research
• diagnosis
• dopamine
• drug
• drug development
• drug discovery
• kinetics
• metabolism
• pharmacokinetics
• pharmacology
• positron emission tomography (PET)
• research
• tomography
• toxicity

• Hôpital Neuro-cardiologique, Lyon, France

  D. Comar

Policies and ethics