188196-22-7

Name	FRAKEFAMIDE
CAS	188196-22-7
Molecular Formula	C30H34FN5O5
MDL Number	MFCD09838485
Molecular Weight	563.62
MOL File	188196-22-7.mol

Synonyms

FRAKEFAMIDE L-Tyrosyl-D-alanyl-L-(4-fluoro)phenylalanyl-L-phenylalanylamide

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Chemical Properties

Boiling point	973.0±65.0 °C(Predicted)
density	1.295±0.06 g/cm3(Predicted)
pka	9.97±0.15(Predicted)

Hazard Information

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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