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Frakefamide (INN) is a synthetic, fluorina … 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.as shelved after phase II clinical trials.
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| rdfs:comment |
Frakefamide (INN) is a synthetic, fluorina … 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.as shelved after phase II clinical trials.
|
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Frakefamide
|
