Adel Nefzi, a researcher at the FIU Center for Translational Science, received a $1,000,000 grant from the National Institute on Drug Abuse of the National Institutes of Health to continue the support of his research in synthesis and in vitro and in vivo screening of fused and tethered heterocyclic peptidomimetics for the discover of new analgesics with decreased side effects.
Dr. Nefzi and his collaborators expect to find structurally diverse, orally active, metabolically stable peripheral restricted opioid peptidomimetics agonists with improved analgesic efficacy while having significantly fewer liabilities of clinical use.
While opioids, such as morphine, have been used extensively for the treatment of severe pain, their clinical use poses serious consequences including respiratory depression and abuse liability for both individuals and society. There is an unmet need for the development of powerful pain relievers with fewer side effects. Given that many of the liabilities of opioid analgesics stem from the effects of the analgesics crossing the blood brain barrier, there is renewed interest in developing peripherally-restricted opioids. Preliminary results from the Nefzi Laboratory, along with his collaborators, suggest the possibility of identifying a new class of metabolically stable peripheral-restricted opioid agonists with improved analgesic efficacy while having significantly fewer liabilities of clinical use.