| Identification | Back Directory | [Name]
FRAKEFAMIDE | [CAS]
188196-22-7 | [Synonyms]
FRAKEFAMIDE
L-Tyrosyl-D-alanyl-L-(4-fluoro)phenylalanyl-L-phenylalanylamide | [Molecular Formula]
C30H34FN5O5 | [MDL Number]
MFCD09838485 | [MOL File]
188196-22-7.mol | [Molecular Weight]
563.62 |
| Chemical Properties | Back Directory | [Boiling point ]
973.0±65.0 °C(Predicted) | [density ]
1.295±0.06 g/cm3(Predicted) | [pka]
9.97±0.15(Predicted) | [Sequence]
Tyr-Ala-Phe(4-F)-Phe-NH2 |
| Hazard Information | Back Directory | [Uses]
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system[1][2]. | [in vivo]
Frakefamide (LEF576) yields a dose dependent increase in morphine appropriate responding to 50% at the highest dose tested (10 μmol/kg) after infusion durations of 2 min, whereas after 15 min infusions a maximum of 25% morphine appropriate responding was occasioned at 17.5 μmol/kg[1][2]. | [References]
[1] Modalen AO, et al. A novel molecule (frakefamide) with peripheral opioid properties: the effects on resting ventilation compared with morphine and placebo. Anesth Analg. 2005 Mar;100(3):713-7. DOI:10.1213/01.ANE.0000145011.75545.C5
[2] Swedberg MD, et al. Drug discrimination: A versatile tool for characterization of CNS safety pharmacology and potential for drug abuse. J Pharmacol Toxicol Methods. 2016 Sep-Oct;81:295-305. DOI:10.1016/j.vascn.2016.05.011 |
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