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Species-Independent A3 Adenosine Receptor Agonists

Posted Jul 31 2008 5:00pm

Description of Invention:
The A3 adenosine receptor (A3AR) subtype has been linked with helping protect the heart from ischemia, controlling inflammation, and regulating cell proliferation. Agonists of the human A3AR subtype have been described; however, they lack selectivity for the corresponding receptor of the mouse. This poses a problem for clinical development because animal model testing is important for pre-clinical validation of drug function. Consequently, a novel agonist was made that is selective for the mouse A3AR while retaining selectivity for the human receptor. This innovation should facilitate moving A3 agonists into the clinical phase of drug development with confidence.

This invention claims species-independent agonists of A3AR, specifically (N)-methanocarba adenine nucleosides. In addition, it describes pharmaceutical compositions comprising such nucleosides, and methods of use such as administering an effective amount to a mammal.

  • cardiac arrhythmias or ischemia
  • inflammation
  • stroke
  • diabetes
  • asthma
  • cancer

Development Status:
Research quantities of compounds have been synthesized and tested for receptor selectivity.

Kenneth A Jacobson (NIDDK)
Artem Melman (NIDDK)

Patent Status:
HHS, Reference No. E-140-2008/0
PCT, Application No. PCT/US09/38026 filed 24 Mar 2009

Relevant Publication:
  1. A Melman et al. Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-2819. [ PubMed abs ]

Licensing Status:
Available for licensing.

Internal Medicine
Internal Medicine - Diagnostics
Internal Medicine - Therapeutics
Ophthalmology - Therapeutics

For Additional Information Please Contact:
Steven Standley Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4074
Fax: 301-402-0220

Ref No: 1796

Updated: 08/2008

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