About: Frakefamide

An Entity of Type: chemical substance, from Named Graph: http://dbpedia.org, within Data Space: dbpedia.org

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.

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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. (en)
dbo:casNumber
  • 188196-22-7
dbo:fdaUniiCode
  • DM32B4GU70
dbo:pubchem
  • 9829352
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  • None (en)
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  • 30 (xsd:integer)
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  • 188196 (xsd:integer)
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  • 9829352 (xsd:integer)
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  • C[C@H]NC[C@H]N (en)
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  • GTPHQORJKFJIRB-JTQLPTLWSA-N (en)
dbp:synonyms
  • L-Tyrosyl-D-alanyl-4-fluoro-L-phenylalanyl-L-phenylalaninamide (en)
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  • DM32B4GU70 (en)
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rdfs:comment
  • 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. (en)
rdfs:label
  • Frakefamide (en)
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