Development of radioligands for in vivo imaging of type 1 cannbinoid receptors (CB1) in human brain

Andrew Horti, Koen Van Laere

Research output: Contribution to journalArticle

Abstract

Cerebral cannabinoid receptor (CB1) and cannabinoid drugs constitute a vibrant field in modern medicine and pharmacology. However, the physiological and pharmacological roles played by the cannabinoid receptor in the central nervous system are still not fully understood. Positron-emission tomography (PET) is the most advanced technique for non-invasive research of cerebral receptors. Quantitative PET imaging of CB1 in animal and human brains has been limited by drawbacks of the available CB1 radioligands that manifested low specific binding, high non-specific binding and/or low brain uptake. The latest research revealed three CB1 PET radioligands ([11C]JHU75528, [18F]MK9470 and [11C]MePPEP) with improved imaging properties. These compounds are now being employed for the quantitative evaluation of CB1 in human subjects with PET. Molecular imaging of the CB1 receptor with these radioligands has now become possible and their application in healthy humans and in patients is underway. Despite the substantial progress in development of CB1 PET radioligands even the latest radioligands manifest certain disadvantages. Current research efforts on the development of CB1 radioligands with higher binding potential, greater brain uptake and more optimal brain kinetics.

Original languageEnglish (US)
Pages (from-to)3363-3383
Number of pages21
JournalCurrent Pharmaceutical Design
Volume14
Issue number31
DOIs
StatePublished - Nov 2008

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Cannabinoid Receptor CB1
Positron-Emission Tomography
Brain
Research
Pharmacology
Cannabinoid Receptors
Modern 1601-history
Molecular Imaging
Cannabinoids
Central Nervous System
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

Development of radioligands for in vivo imaging of type 1 cannbinoid receptors (CB1) in human brain. / Horti, Andrew; Van Laere, Koen.

In: Current Pharmaceutical Design, Vol. 14, No. 31, 11.2008, p. 3363-3383.

Research output: Contribution to journalArticle

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