Instructional Specialist, Senior

Iman Daryaei

Method of Synthesizing 18F Radiolabeled Biomolecular Agents

Small Molecule Mixed Agonist/Antagonist for Opioid Receptors for Anti-Addiction and/or Pain TherapyThis invention provides compositions and method of pain treatment using a mixture of an opioid receptor agonist in combination with an adrenoreceptor modulator compound.  The opioid receptor agonist may be a clinically-used drug, and the adrenoreceptor modulator compound is a novel small molecule.  Proof-of-concept testing in animals has shown analgesic effect without reward behavior.

Background:
Opioids continue to be widely used for pain treatment. However, constant opioid treatment is accompanied with serious undesirable effects including drowsiness and mental clouding, nausea and emesis, constipation and in many cases dependence and addiction. Continuous use of opioid therapy also develops analgesic tolerance and hyperalgesia in many patients. These unwanted effects significantly diminish the patients’ quality of life. The mechanisms for these side effects are still largely unclear.  However, one particular side effect, namely addiction, is a cause for great concern in pain treatment using opioids.

Prescription opioids can be highly addictive and are widely misused. It has been estimated that the total economic cost of opioid misuse in the United States is $78.5 billion per year. The opioid crisis has been exacerbated by over-prescription of opioid pain-relievers for the treatment of pain. Due at least in part due to over-prescription and additive nature of opioids, some who experience chronic pain may suffer undertreatment. In fact, in many parts of the developing world, access to opioids even for acute pain and/or cancer pain can be restricted due to concerns over addiction and overdose. Even in the United States, some patients can suffer from an undertreatment of pain. For example, patients with cognitive impairment and the elderly can be especially susceptible to the central nervous system effects of traditional opioids such as morphine and in some cases are not prescribed enough to meet their pain management needs.

Applications:
· Pain treatment
· Anti-addiction therapy

Advantages:
· Improve pain management
· Reduce risk of addiction

KMap

Chemistry & Biochemistry - Science