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Radiotracers for Imaging Cannabinoid Sub-Type1 (CB1) Receptor

Description of Invention:
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).

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

Patent Status:
DHHS Reference No. E-155-2008/0 --
U.S. Provisional Application No. 61/052,581 filed 12 May 2008

Relevant Publication:
  1. 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]
  2. 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. 2008 Sep 25;51(18):5608-5616. [PubMed abs]


Licensing Status:
Available for exclusive or non-exclusive licensing.


Portfolios:
Devices/Instrumentation
Central Nervous System

Central Nervous System -Research Materials-Other
Devices/Instrumentation-Diagnostics-Imaging
Central Nervous System -Research Materials
Devices/Instrumentation-Diagnostics

For Additional Information Please Contact:
RC Tang JD, LLM
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301/435-5031
Email: tangrc@mail.nih.gov
Fax: 301/402-0220


Web Ref: 1801

Updated: 8/08

 

 
 
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