Frakefamide 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

563.62

C₃₀H₃₄FN₅O₅

188196-22-7

Tyr-Ala-Phe(4-F)-Phe-NH2

YA-Phe(4-F)-Phe-NH2

O=C(N[C@H](C(N)=O)CC1=CC=CC=C1)[C@@H](NC([C@@H](C)NC([C@@H](N)CC(C=C2)=CC=C2O)=O)=O)CC(C=C3)=CC=C3F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]