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Frakefamide

Opioid agonist peptide compound

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Frakefamide (INN) is a synthetic, fluorinated linear tetrapeptide with the amino acid sequence Tyr-D-Ala-(p-F)Phe-Phe-NH2 which acts as a peripherally-specific, selective μ-opioid receptor agonist. Despite its inability to penetrate the blood-brain-barrier and enter the central nervous system, frakefamide has potent analgesic effects and, unlike centrally-acting opioids like morphine, does not produce respiratory depression, indicating that its antinociceptive effects are mediated by peripheral μ-opioid receptors. It was under development for the treatment of pain by AstraZeneca and Shire but was shelved after phase II clinical trials.

References

(March 2005). "A novel molecule (frakefamide) with peripheral opioid properties: the effects on resting ventilation compared with morphine and placebo". Anesthesia and Analgesia.
(30 November 2009). "Meyler's Side Effects of Analgesics and Anti-Inflammatory Drugs". Elsevier.
(January 2006). "A novel molecule with peripheral opioid properties: the effects on hypercarbic and hypoxic ventilation at steady-state compared with morphine and placebo". Anesthesia and Analgesia.
(15 April 2012). "Practical Process Research and Development: A Guide for Organic Chemists". Academic Press.
(13 May 2003). "Pain: Current Understanding, Emerging Therapies, And Novel Approaches To Drug Discovery". CRC Press.

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analgesics 4-fluorophenyl-compounds opioid-peptides peripherally-selective-drugs tetrapeptides

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