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Radiotracers for Imaging Cannabinoid Sub-Type1 (CB1) Receptor

National Institutes of Health (NIH)
Novel radiolabeled compounds for imaging cannabinoid sub-type 1 receptors in brains of mammals using PET or SPECT.

Full description

The present invention relates to novel radiolabeled compounds for imaging cannabinoid sub-type 1 (CB1) receptors in brains of mammals, particularly humans, using positron emission tomography (PET) or single photon emission computed tomography (SPECT). These radioligands can be used in clinical research, diagnostics, or drug discovery and development, in that, they permit understanding of the role of CB1 receptors in neuropsychiatric disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, multiple sclerosis, depression, mood disorder, anxiety, schizophrenia, drug addiction, alcohol disorder, obesity and anorexia.

 

Applications:

  • In vivo imaging of CB1 receptor in mammals, particularly humans
  • Diagnostic imaging of CB1 receptors in subjects having a neurological, neuropsychiatric, neurodegenerative or other condition and treatment
  • Pharmaceutical composition
  • Diagnostic kits

 

Advantages:

The principal radioligand under the claim is effective for imaging CB1 receptors in vivo with PET.

 

Development Status:

Primary radioligand has been evaluated in non-human primates with PET.

 

Market:

Radioligands may be useful for performing drug occupancy studies of CB1 receptors, and for neuropsychiatric studies and investigations with imaging techniques (e.g., PET or SPECT).

 

Relevant Publications:

  • SR Donohue, C Halldin, VW Pike.  Synthesis and structure–activity relationships (SARs) of 1,5-diarylpyrazole cannabinoid  type-1 (CB1) receptor ligands for potential use in molecular imaging.  Bioorg Med Chem. 2006 Jun 1;14(11):3712-3720.  [PubMed abs]
  • SR Donohue, VW Pike, SJ Finnema, P Truong, J Andersson, B Gulyás, C Halldin.  Discovery and labeling of high affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.  J Med Chem., in  press.

 

 

Patent information

U.S. Provisional Application No. 61/052,581 filed 12 May 2008 (HHS Reference No. E-155-2008/0-US-01)

Inventors:

Victor W. Pike (NIMH), Sean R. Donohue (NIMH), et al.

Type of business relationship sought

Licensees Sought:

Available for exclusive or non-exclusive licensing.

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