A Survey of Molecular Imaging of Opioid Receptors.

Cumming, Paul; Marton, János; Lilius, Tuomas O.; Olberg, Dag Erlend; Rominger, Axel. (2019). A Survey of Molecular Imaging of Opioid Receptors. Molecules, 24(22) Molecular Diversity Preservation International MDPI 10.3390/molecules24224190

RomA_Cumming_A Survey of Molecular Imaging of Opioid Receptors.pdf - Published Version
Available under License Creative Commons: Attribution (CC-BY).

Download (4MB) | Preview

The discovery of endogenous peptide ligands for morphine binding sites occurred in parallel with the identification of three subclasses of opioid receptor (OR), traditionally designated as μ, δ, and κ, along with the more recently defined opioid-receptor-like (ORL1) receptor. Early efforts in opioid receptor radiochemistry focused on the structure of the prototype agonist ligand, morphine, although N-[methyl-11C]morphine, -codeine and -heroin did not show significant binding in vivo. [11C]Diprenorphine ([11C]DPN), an orvinol type, non-selective OR antagonist ligand, was among the first successful PET tracers for molecular brain imaging, but has been largely supplanted in research studies by the μ-preferring agonist [11C]carfentanil ([11C]Caf). These two tracers have the property of being displaceable by endogenous opioid peptides in living brain, thus potentially serving in a competition-binding model. Indeed, many clinical PET studies with [11C]DPN or [11C]Caf affirm the release of endogenous opioids in response to painful stimuli. Numerous other PET studies implicate μ-OR signaling in aspects of human personality and vulnerability to drug dependence, but there have been very few clinical PET studies of μORs in neurological disorders. Tracers based on naltrindole, a non-peptide antagonist of the δ-preferring endogenous opioid enkephalin, have been used in PET studies of δORs, and [11C]GR103545 is validated for studies of κORs. Structures such as [11C]NOP-1A show selective binding at ORL-1 receptors in living brain. However, there is scant documentation of δ-, κ-, or ORL1 receptors in healthy human brain or in neurological and psychiatric disorders; here, clinical PET research must catch up with recent progress in radiopharmaceutical chemistry.

Item Type:

Journal Article (Review Article)


04 Faculty of Medicine > Department of Radiology, Neuroradiology and Nuclear Medicine (DRNN) > Clinic of Nuclear Medicine

UniBE Contributor:

Cumming, Paul and Rominger, Axel Oliver


600 Technology > 610 Medicine & health




Molecular Diversity Preservation International MDPI




Sabine Lanz

Date Deposited:

23 Jan 2020 15:00

Last Modified:

23 Jan 2020 15:00

Publisher DOI:


PubMed ID:


Uncontrolled Keywords:

drug dependence epilepsy movement disorders opioid receptors pain positron emission tomography radiotracers μOR-, δOR-, κOR- and ORL1-ligands





Actions (login required)

Edit item Edit item
Provide Feedback