frakefamide

Names

[ Name ]:
frakefamide

[Synonym ]:
L-Phenylalaninamide, 4-fluoro-L-phenylalanyl-N-[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)-1-oxopropyl]amino]-1-oxopropyl]-
4-Fluoro-L-phenylalanyl-N-[(2R)-2-(L-tyrosylamino)propanoyl]-L-phenylalaninamide
frakefamide

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor

Signaling Pathways >> Neuronal Signaling >> Opioid Receptor

Research Areas >> Neurological Disease

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
897.9±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₀H₃₄FN₅O₅

[ Molecular Weight ]:
563.620

[ Flash Point ]:
496.8±34.3 °C

[ Exact Mass ]:
563.254395

[ LogP ]:
1.45

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.610

Related Compounds

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