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Preclinical, Journal: Non-addictive orally-active kappa opioid agonists for the treatment of peripheral pain in rats. (Pubmed Central) - Jan 15, 2020
Further, derivatives of the tetra-peptide D-Phe-D-Phe-D-Nle-D-Arg-NH, such as CR665, exhibit high peripheral to central selectivity in analgesic models when administered intravenously (i.v.); however, they are inactive when administered orally...PERSPECTIVE: This article presents data supporting the analgesic properties of an orally available, peripherally-restricted, kappa-opioid agonist for peripheral pain. A potential out-patient pharmaceutical that acts as efficacious as morphine in alleviating peripheral pain, while failing to produce undesired CNS-mediated effects, could help reduce the current health care burden associated with prescription opioids.
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