Dopamine D3 Receptor Agonist Compounds, Methods of Preparation, Intermediates Thereof, and their Methods of Use

Due to the large degree of homology among dopamine D2-like receptors, discovering ligands capable of discriminating between the D2, D3, and D4 receptor subtypes remains a significant challenge. The development of subtype-selective pharmaceutical small molecules to activate (agonists) signals regulated by D2-like receptors has been especially difficult. 

Novel Biased Potent Opioid-Like Agonists as Improved Medications to Treat Chronic and Acute Pain

There are no analgesics to ameliorate chronic pain without adverse side-effects (e.g., respiratory depression, gastrointestinal effects, tolerance, dependence), thus forcing patients into a difficult choice of negative impacts on quality of life. Most of the analgesics used for chronic and acute pain are drugs such as oxycodone, morphine, oxymorphone, and codeine. All of these opioids have been subject to misuse; prescription drug abuse is a severe problem worldwide, causing high mortality and greatly increased emergency room visits.

Analogues of Modafinil for treating sleep and attention disorders

Modafinil has attracted attention for the treatment of cognitive dysfunction in disorders such as attention-deficit/hyperactivity disorder (ADHD) as well as cocaine and methamphetamine dependence.  However, modafinil has relatively low affinity for binding to the dopamine transporter (DAT) to block dopamine reuptake, and is water-insoluble, thus requiring large doses to achieve pharmacological effects.

Methods of making and using dopamine receptor selective antagonists/partial agonists

Dopamine is a major neurotransmitter in the central nervous system and among other functions is directly related to the rewarding effects of drugs of abuse.  Dopamine signaling is mediated by D1, D2, D3, D4 and D5 receptors.  The dopamine D3 receptor is a known target to treat a variety of neuropsychiatric disorders, including substance use disorders (e.g. cocaine and opioid), schizophrenia and depression.

Systems and Devices for Training and Imaging an Awake Test Animal

Typical MRI imaging sessions can last over 45 minutes and depend on the subject remaining still during the procedure for accurate imaging. In particular, animals being imaged, such as rodents (rats) in an awakened state, are not readily compliant with the restricted movement required when being imaged. Current techniques for imaging awake animals focus on training them with full body restraints and head fixation using a bite bar and/or ear bars.

A Protocol to Enhance Therapeutic Effects of Transcranial Magnetic Stimulation and the Methods to Realize It

Summary: 

The National Institute on Drug Abuse (NIDA) seeks research co-development partners and/or licensees for a high-powered electronic device and coil that delivers Transcranial Magnetic Stimulation (TMS) pulses as well as the software that controls the device for treating treatment resistant depression, substance use disorders and other CNS disorders.

Description of Technology: 

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.