Development of [18F]ASEM, a specific radiotracer for quantification of the α7-nAChR with positron-emission tomography

Research output: Contribution to journalArticle

Abstract

The alpha-7 subtype of the nicotinic acetylcholine receptor (α7-nAChR) is fundamental to physiology; it mediates various brain functions and represents an important target for drug discovery. Exploration of the brain nicotinic acetylcholine receptors (nAChRs) using positron-emission tomography (PET) will make it possible to better understand the important role of this receptor and to study its involvement in schizophrenia, bipolar disorder, Alzheimer's and Parkinson's diseases, drug dependence, inflammation and many other disorders and simplify the development of nicotinic drugs for treatment of these disorders. Until recently, PET imaging of α7-nAChRs has been impeded by the absence of good radiotracers. This review describes various endeavors to develop α7-nAChR PET tracers by several research groups including the author's group. Most initial PET tracers for imaging α7-nAChRs did not exhibit suitable imaging properties due to their low specific binding. Newly discovered [18F]ASEM is the first highly specific α7-nAChR radioligand and in 2014 it was translated to human PET imaging.

Original languageEnglish (US)
Pages (from-to)566-575
Number of pages10
JournalBiochemical Pharmacology
Volume97
Issue number4
DOIs
StatePublished - Oct 15 2015

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Positron emission tomography
Nicotinic Receptors
Positron-Emission Tomography
Imaging techniques
Brain
Physiology
Drug Discovery
Bipolar Disorder
Pharmaceutical Preparations
Substance-Related Disorders
Parkinson Disease
3-(1,4-diazabicyclo(3.2.2)nonan-4-yl)-6-fluorodibenzo(b,d)thiophene 5,5-dioxide
Schizophrenia
Alzheimer Disease
Inflammation
Research

Keywords

  • Alpha 7
  • Nicotinic receptor
  • PET
  • Positron emission tomography
  • [F]ASEM
  • α7-nAChR

ASJC Scopus subject areas

  • Pharmacology
  • Biochemistry

Cite this

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abstract = "The alpha-7 subtype of the nicotinic acetylcholine receptor (α7-nAChR) is fundamental to physiology; it mediates various brain functions and represents an important target for drug discovery. Exploration of the brain nicotinic acetylcholine receptors (nAChRs) using positron-emission tomography (PET) will make it possible to better understand the important role of this receptor and to study its involvement in schizophrenia, bipolar disorder, Alzheimer's and Parkinson's diseases, drug dependence, inflammation and many other disorders and simplify the development of nicotinic drugs for treatment of these disorders. Until recently, PET imaging of α7-nAChRs has been impeded by the absence of good radiotracers. This review describes various endeavors to develop α7-nAChR PET tracers by several research groups including the author's group. Most initial PET tracers for imaging α7-nAChRs did not exhibit suitable imaging properties due to their low specific binding. Newly discovered [18F]ASEM is the first highly specific α7-nAChR radioligand and in 2014 it was translated to human PET imaging.",
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