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1. Marker protein and target for may represent a novel chemosensitizing 5. G. Balboni et al. Highly selective
antigen-specific immunotherapy in agent for treating cancer, and may also fluorescent analogue of the potent *elta-
patients with malignant melanoma. be used for reducing tolerance to opioid receptor antagonist Dmt-Tic. J
2. Therapeutics and diagnostics for morphine, the drug of choice in most Med Chem. 2004 Dec 16:47(26):6541–
melanin-related disorders. hospitals around the world, thereby 6546.
Development Status: Early stage. increasing its effectiveness. Also Patent Status:
Inventors: William J. Pavan and Stacie disclosed are compounds produced 1. U.S. Patent No. 6,753,317 issued 22
K. Loftus (NHGRI). through derivatization of Dmt-Tic Jun 2004 (HHS Reference No. E–103–
Publications: Stacie K. Loftus, Denise reference compounds with lysine, 2000/0–US–02).
M. Larson, Laura L. Baxter, Anthony resulting in an unexpected and broad 2. U.S. Patent No. 6,916,905 issued 12
Antonellis, Yidong Chen, Xufeng Wu, range of delta-and/or mu-opioid Jul 2005 (HHS Reference No. E–103–
Yuan Jiang, Michael Bittner, John A. receptor modulation. The inventors 2000/1–US–01).
Hammer III, and William J. Pavan. have also prepared symmetric and 3. U.S. Patent Application No. 10/
Mutation of melanosome protein RAB38 asymmetric Dmt-Tic di-peptides that are 280,752 filed 16 Nov 2005 (HHS
in chocolate mice. Proc Natl Acad Sci potent dual delta- and mu-opioid Reference No. E–103–2000/2–US–02).
U.S.A. 2002 Apr 2;99(7):4471–4476. receptor antagonists and that can pass 4. U.S. Provisional Application No.
Patent Status: through the gastrointestinal and blood- 60/834,438 filed 31 Jul 2006 (HHS
1. U.S. National Stage Application No. brain barriers. Finally, the inventors Reference No. E–103–2000/3–US–01).
10/501,611 filed 20 Nov 2005, claiming have prepared various fluorescent Dmt- 5. PCT Application No. PCT/US06/
priority to 18 Jan 2002 (HHS Reference Tic analogs that are useful for study of 33560 filed 30 Aug 2006 (HHS
No. E–315–2001/0–US–07). delta- and mu-opioid receptor structure Reference No. E–305–2005/0–PCT–02).
2. Foreign counterparts pending in and function. Licensing Status: Available for
Australia, Canada, Europe, and Japan. Applications: exclusive or nonexclusive licensing.
Licensing Status: Available for 1. Potential opiate, food, and alcohol Licensing Contact: Tara L. Kirby, PhD;
exclusive or non-exclusive licensing. addiction therapeutics. 301/435–4426; tarak@mail.nih.gov.
Licensing Contact: Tara L. Kirby, 2. Potential therapeutics for pain Dated: April 17, 2007.
Ph.D; 301/435–4426; treatment.
tarak@mail.nih.gov. 3. Potential therapeutics for cancer. Steven M. Ferguson,
4. Tools for screening ligand binding Director, Division of Technology Development
Novel Dmt-Tic Analogues Specific for activity and differentiating between and Transfer, Office of Technology Transfer,
Delta- and Mu-Opioid Receptors delta- and mu-opioid receptors. National Institutes of Health.
Description of Technology: Opioid Market: [FR Doc. E7–7933 Filed 4–25–07; 8:45 am]
receptor modulators, used historically 1. In 2004, approximately 22 million BILLING CODE 4140–01–P
for pain control, have more recently Americans over the age of 12 required
been shown to possess broader treatment for alcohol or illicit drug
therapeutic potential in areas such as abuse and addiction; 13 million of these DEPARTMENT OF HOMELAND
opiate and alcohol abuse, neurological were classified as alcoholics. SECURITY
disease or injury, neuropeptide or 2. Approximately 50 million
neurotransmitter imbalance, and Americans suffer from pain, and an Coast Guard
immune system dysfunction. estimated 1.5 billion people suffer from
[USCG–2007–27858]
Furthermore, their interaction with key moderate to severe pain worldwide.
reward pathways presents interesting 3. Two-thirds of the U.S. population National Boating Safety Advisory
avenues for exploration in the treatment is overweight, with a quarter designated Council; Vacancies
of food as an addictive substance, due as obese (9 million of whom are
to the fact that obesity is a major health children); the number of overweight AGENCY: Coast Guard, DHS.
problem in the U.S. Also, evidence of Americans doubled between 1980–1999 ACTION: Request for applications.
modulatory interactions between delta- and is predicted to increase 20% by
2013 to 140 million. SUMMARY: The Coast Guard seeks
and mu-opioid receptors has spurred applications for membership on the
Development Status: In vitro data are
interest in new opioid ligands National Boating Safety Advisory
available.
possessing mixed and dual specificity Inventors: Lawrence H. Lazarus Council (NBSAC). NBSAC advises the
for these receptors. These bifunctional (NIEHS) et al. Coast Guard on matters related to
compounds are particularly promising Publications: recreational boating safety.
for treatment of addiction and treatment 1. G. Balboni et al. Effect of lysine at DATES: Application forms should reach
of pain with the elimination of drug C-terminus of the Dmt-Tic opioid
tolerance. us on or before August 17, 2007.
pharmacophore. J Med Chem. 2006 Sep
The inventors have developed a wide ADDRESSES: You may request an
7;49(18):5610–5617.
variety of highly selective Dmt-Tic 2. T Lovekamp et al. Inhibition of application form by writing to
analogues with potential therapeutic human multidrug resistance P- Commandant, Office of Boating Safety
applications. These analogues include glycoprotein 1 by analogues of a potent (CG–3PCB–1), U.S. Coast Guard, 2100
specific agonists and antagonists of the delta-opioid antagonist. Brain Res. 2001 Second Street, SW., Washington, DC
delta- and mu-opioid receptors and May 25;902(1):131–134. 20593–0001; by calling 202–372–1062;
combinations thereof. 3. T Li et al. Potent Dmt-Tic or by faxing 202–372–1932. Send your
Some disclosed analogues are di- and pharmacophoric delta- and mu-opioid application in written form to the above
tri-peptidic derivatives of the Dmt-Tic receptor antagonists. J Med Chem. 2005 street address. This notice and the
rwilkins on PROD1PC63 with NOTICES
pharmacophore; in addition to opioid Dec 15;48(25):8035–8044. application form are also available on
receptor specificity, two of these 4. T Li et al. Transformation of a mu- the Internet at: http://
derivatives have been shown to inhibit opioid agonist into biologically potent www.uscgboating.org/nbsac/nbsac.htm.
the activity of human multidrug mu-opioid antagonists. Bioorg Med FOR FURTHER INFORMATION CONTACT: Mr.
resistance glycoprotein 1 (hMDR1) and Chem. 2007 Feb 1;15(3):1237–1251. Jeff Ludwig, Executive Secretary of
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Federal Register / Vol. 72, No. 80 / Thursday, April 26, 2007 / Notices 20863
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