Fluorinated MU-Opioid Receptor Agonists

Summary: 
Investigators at the National Institute on Drug Abuse seek co-development partners and/or licensees for collection of mu opioid receptor (MOR) agonists as alternatives for existing compounds.

Description of Technology: 
Although existing opioids are excellent analgesics and useful as positron emission tomography (PET) radiotracers, they come with debilitating side effects. These include addiction, respiratory distress, hyperalgesia, and constipation. Therefore, there is a need for alternatives with lower adverse effects.

Intralipid as a Contrast Agent to Enhance Subsurface Blood Flow Imaging

This technology includes a blood flow imaging method that allows for a higher density of smaller particles to be detected. Current imaging methods that are based on Doppler measurements are limited by the discontinuity in the capillary flow in the space between red blood cells. The core technology is to use a scattering agent to enhance capillary flow or microcirculation. This technology has been tested for optical coherence Doppler tomography, but can be expended to any Doppler based flow imaging techniques such as laser speckle imaging.

Interleukin-27 Producing B-Cell Population and Uses Thereof

Summary: 
The National Eye Institute (NEI) seeks research co-development partners and/or licensees to advance the production and uses of interleukin-27 (IL-27) producing B-regulatory cell (i27-Breg) therapy for immune related autoimmune disorders. These disorders include but are not limited, to age-related macular degeneration (AMD), graft-versus-host disease (GVHD), multiple sclerosis (MS) and transplant rejection.

P2Y14 Receptor Antagonists for the Treatment of Inflammatory Diseases, Including Pulmonary and Renal Conditions and Chronic Pain

This technology includes the development of selective P2Y14R antagonists for the treatment of asthma, sterile inflammation of the kidney, diabetes, and neurodegeneration. The P2Y14 receptor (P2Y14R) is a target for the treatment of inflammatory diseases, including pulmonary and renal conditions. Selective P2Y14R antagonists have demonstrated efficacy in animal models of asthma, pain, diabetes, and acute kidney injury. However, the prototypical antagonist is not optimal for in vivo administration, as it displays a low oral bioavailability.

Selective A3 Adenosine Receptor Agonists for the Treatment of Chronic Neuropathic Pain and Other Conditions

This technology includes the creation and use of A3 adenosine receptor (A3AR)-selective agonists for treating chemotherapy-induced peripheral neuropathy, chronic neuropathic pain, rheumatoid arthritis, psoriasis, and other conditions. A3 receptors for adenosine are found in most cells and endogenous activation of the A3 receptors can result in apoptosis, thereby relieving the inflammation or targeting a tumor. A3AR agonists have been a promising strategy for the treatment of various diseases.

A3 Adenosine Receptor Positive Allosteric Modulators

Selective A3AR agonists are sought as potential agents for treating inflammatory diseases,
chronic pain, cancer and non-alcoholic steatohepatitis (NASH). NIDDK investigators have invented 
new chemical composition as positive allosteric modulators (PAMs) of the A3AR. These chemical 
compounds contain sterically constrained, bridged modifications and cycloalkyl rings of various 
sizes, as well as modifications of the 4-arylamino group. The compounds have added 

Nanobody–Antiviral Peptide Conjugates for Potent HIV Entry Inhibition

This technology includes a new class of nanobody–antiviral peptide conjugates that block HIV from infecting human CD4⁺ T-cells, positioning them for future therapeutic and prophylactic use. Nanobodies—single-domain antibody fragments—guide the drug to the virus’s docking site and impede receptor binding, while the linked peptide halts the membrane-fusion step, creating a one-two punch against viral entry.

Novel Small Molecule Agonists of the Relaxin Receptor as Potential Therapy for Heart Failure and Fibrosis

The present invention is directed to novel small molecule agonists of the mammalian relaxin family receptor 1 (RXFP1), including human RXFP1. Activation of RXFP1 induces: 1) vasodilation due to up-regulation of the endothelin system; 2) extracellular matrix remodeling; 3) moderation of inflammation by reducing levels of inflammatory cytokines; and 4) angiogenesis. Small molecule agonists of RXFP1 may be useful in treating acute heart failure (AHF), scleroderma, fibrosis, other conditions associated with the biology of relaxin, and in improving reproductive health and wound healing.