FRAKEFAMIDE
FRAKEFAMIDE Basic information
- Product Name:
- FRAKEFAMIDE
- Synonyms:
-
- FRAKEFAMIDE
- L-Tyrosyl-D-alanyl-L-(4-fluoro)phenylalanyl-L-phenylalanylamide
- L-Phenylalaninamide, L-tyrosyl-D-alanyl-4-fluoro-L-phenylalanyl-
- CAS:
- 188196-22-7
- MF:
- C30H34FN5O5
- MW:
- 563.62
- Mol File:
- 188196-22-7.mol
FRAKEFAMIDE Chemical Properties
- 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
FRAKEFAMIDE Usage And Synthesis
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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