Imaging of Brain Receptors Using (11C)mGlu1

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT01420952
Recruitment Status : Terminated
First Posted : August 22, 2011
Last Update Posted : May 21, 2018
Information provided by:
National Institutes of Health Clinical Center (CC)

Brief Summary:


- (11C)mGlu1 is a new drug that helps to show where a protein, mGluR1, is found in the brain. The drug contains a small amount of radioactivity that can be detected by imaging studies like positron emission tomography (PET) scans. By looking at the mGluR1 receptors, researchers hope to better understand how they are involved in general health, brain disorders, and addiction.


  • To test how (11C)mGlu1 is distributed in the brain and body.
  • To measure how mGluR1 receptors display (11C)mGlu1 during imaging studies.


- Healthy volunteers between 18 and 50 years of age.


  • Participants will be screened with a medical history, physical exam, and blood and urine tests. This study requires four visits to the NIH Clinical Center.
  • Participants will have an initial evaluation, a magnetic resonance imaging (MRI) scan, a PET scan, and a final blood sample after the PET scan, all at different visits.
  • The MRI and PET scans will focus on the brain. Participants will receive (11C)mGlu1, and have scans to see how it shows up in the brain.
  • Some participants will have whole body imaging studies to see how (11C)mGlu1 shows up in the body.

Condition or disease Intervention/treatment Phase
Dosimetry Pharmacokinetics Drug: [11C]LY2428703 Phase 1

Detailed Description:

Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors that respond to glutamate by activating proteins inside nerve cells that affect cell metabolism, thereby fine-tuning the signals sent between cells to maintain balance in neuronal activity. mGluR receptor subtype 1 (mGluR1s) are located in several brain regions, including the cerebellum, hippocampus, olfactory bulb, and basal ganglia. mGluR1 activation stimulates phospholipase C, resulting in phosphoinositide hydrolysis and increased intracellular Ca(2+) levels. Detailed study of mGluR1s has heretofore been hindered by the lack of high affinity and of selective ligands for this receptor subtype.

The present protocol will use a new PET ligand [C(11)]mGlu1 to 1) perform kinetic brain imaging to quantify mGluR1 binding parameters in brain and determine the reliability and reproducibility of these measures in 15 healthy volunteers (Phase 1); and 2) if the tracer proves successful in Phase 1, we will estimate radiation-absorbed doses of [C(11)]mGlu1 in healthy human subjects by performing whole body imaging (Phase 2).

Successful development of a PET ligand to image mGlurR1 would have a strong impact on clinical management of brain disorders characterized by disruptions in glutamatergic transmission, including anxiety and stress disorders, drug addiction, epilepsy, Huntington s disease, and Parkinson s disease.

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 3 participants
Allocation: Non-Randomized
Intervention Model: Single Group Assignment
Masking: None (Open Label)
Primary Purpose: Diagnostic
Official Title: PET Imaging of Brain mGlu1 Receptors Using [11]LY2428703
Study Start Date : July 29, 2011
Actual Primary Completion Date : November 27, 2012
Actual Study Completion Date : November 27, 2012

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 50 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes
  • Healthy volunteers subjects aged 18 50 with medical history/physical exam, electrocardiogram (ECG), and laboratory tests within normal limits within 60 days of the PET scan.


  • <TAB>Lifetime psychiatric illness or severe systemic disease based on history and physical exam.
  • <TAB>Serious medical illness likely to modify brain anatomy and/or physiology (seizure disorders, past brain surgery, etc.)
  • <TAB>High blood pressure, as demonstrated by at least two resting measurements above 140/100, separated by at least 30 min.
  • <TAB>Any current substance or alcohol abuse, with the exception of nicotine.
  • <TAB>Positive urine toxicology screen
  • <TAB>Radiation exposure from participation in other research protocols or clinical care in the last year such that the additional radiation exposure from this protocol would exceed annual limits.
  • <TAB>Pregnancy or breastfeeding.
  • <TAB>Claustrophobia (Part 1 only).
  • <TAB>metallic (ferromagnetic) implants, including pacemakers or other implanted electrical devices, brain stimulators, some types of dental implants, aneurysm clips (metal clips on the wall of a large artery), metallic prostheses (including metal pins and rods, heart valves, and cochlear implants), permanent eyeliner, implanted delivery pump, shrapnel fragments, and possible small metal fragments in the eye (Part 1 only).
  • <TAB>Unable to lie flat on back for up to 2.5 hours.
  • <TAB>Positive HIV test.
  • <TAB>Inability to provide informed consent

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT01420952

United States, Maryland
National Institutes of Health Clinical Center, 9000 Rockville Pike
Bethesda, Maryland, United States, 20892
Sponsors and Collaborators
National Institute of Mental Health (NIMH)
Principal Investigator: Robert B Innis, M.D. National Institute of Mental Health (NIMH)